The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
Databases containing information about PROTEINS such as AMINO ACID SEQUENCE; PROTEIN CONFORMATION; and other properties.
A family of enzymes that catalyze the conversion of ATP and a protein to ADP and a phosphoprotein.
A process that includes the determination of AMINO ACID SEQUENCE of a protein (or peptide, oligopeptide or peptide fragment) and the information analysis of the sequence.
The procedures involved in combining separately developed modules, components, or subsystems so that they work together as a complete system. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.
Protein kinases that catalyze the PHOSPHORYLATION of TYROSINE residues in proteins with ATP or other nucleotides as phosphate donors.
A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
An isoflavonoid derived from soy products. It inhibits PROTEIN-TYROSINE KINASE and topoisomerase-II (DNA TOPOISOMERASES, TYPE II); activity and is used as an antineoplastic and antitumor agent. Experimentally, it has been shown to induce G2 PHASE arrest in human and murine cell lines and inhibits PROTEIN-TYROSINE KINASE.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
A family of synthetic protein tyrosine kinase inhibitors. They selectively inhibit receptor autophosphorylation and are used to study receptor function.
Non-receptor tyrosine kinases encoded by the C-ABL GENES. They are distributed in both the cytoplasm and the nucleus. c-Abl plays a role in normal HEMATOPOIESIS especially of the myeloid lineage. Oncogenic transformation of c-abl arises when specific N-terminal amino acids are deleted, releasing the kinase from negative regulation.
A replication-defective strain of Murine leukemia virus (LEUKEMIA VIRUS, MURINE) capable of transforming lymphoid cells and producing a rapidly progressing lymphoid leukemia after superinfection with FRIEND MURINE LEUKEMIA VIRUS; MOLONEY MURINE LEUKEMIA VIRUS; or RAUSCHER VIRUS.
Transforming proteins encoded by the abl oncogenes. Oncogenic transformation of c-abl to v-abl occurs by insertional activation that results in deletions of specific N-terminal amino acids.
Species of GAMMARETROVIRUS, containing many well-defined strains, producing leukemia in mice. Disease is commonly induced by injecting filtrates of propagable tumors into newborn mice.
Retrovirus-associated DNA sequences (abl) originally isolated from the Abelson murine leukemia virus (Ab-MuLV). The proto-oncogene abl (c-abl) codes for a protein that is a member of the tyrosine kinase family. The human c-abl gene is located at 9q34.1 on the long arm of chromosome 9. It is activated by translocation to bcr on chromosome 22 in chronic myelogenous leukemia.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Catalytically active enzymes that are formed by the combination of an apoenzyme (APOENZYMES) and its appropriate cofactors and prosthetic groups.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
Individual's rights to obtain and use information collected or generated by others.
A subspecialty of internal medicine concerned with the study of the physiology and diseases of the digestive system and related structures (esophagus, liver, gallbladder, and pancreas).
The lower part of the SPINAL CORD consisting of the lumbar, sacral, and coccygeal nerve roots.
The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)
A publication issued at stated, more or less regular, intervals.
A quantitative measure of the frequency on average with which articles in a journal have been cited in a given period of time.
The evaluation by experts of the quality and pertinence of research or research proposals of other experts in the same field. Peer review is used by editors in deciding which submissions warrant publication, by granting agencies to determine which proposals should be funded, and by academic institutions in tenure decisions.

Intracellular signalling: PDK1--a kinase at the hub of things. (1/15539)

Phosphoinositide-dependent kinase 1 (PDK1) is at the hub of many signalling pathways, activating PKB and PKC isoenzymes, as well as p70 S6 kinase and perhaps PKA. PDK1 action is determined by colocalization with substrate and by target site availability, features that may enable it to operate in both resting and stimulated cells.  (+info)

PKCdelta acts as a growth and tumor suppressor in rat colonic epithelial cells. (2/15539)

We have analysed the expression of three calcium-independent isoforms of protein kinase C (PKC), PKCdelta, PKCepsilon and PKCzeta, in an in vitro model of colon carcinogenesis consisting of the nontumorigenic rat colonic epithelial cell line D/WT, and a derivative src-transformed line D/src. While PKCzeta and PKCepsilon showed similar protein levels, PKCdelta was markedly decreased in D/src cells when compared to the D/WT line. To assess whether down-regulation of PKCdelta was causally involved in the neoplastic phenotype in D/src cells, we prepared a kinase-defective mutant of PKCdelta. Stable transfection of this sequence caused morphological and growth changes characteristic of partial transformation in D/WT cells. Moreover, to test whether PKCdelta was involved in growth control and transformation in this model, we overexpressed PKCdelta in D/src cells. Transfected cells underwent marked growth and morphological modifications toward the D/WT phenotype. In a late stage in culture, transfected cells ceased to proliferate, rounded up and degenerated into multinucleated, giant-like cells. We conclude that PKCdelta can reverse the transformed phenotype and act as a suppressor of cell growth in D/src cells. Moreover, our data show that downregulation of this isoenzyme of PKC may cooperate in the neoplastic transformation induced by the src oncogene in D/WT cells.  (+info)

Activation of IkappaB kinase beta by protein kinase C isoforms. (3/15539)

The atypical protein kinase C (PKC) isotypes (lambda/iotaPKC and zetaPKC) have been shown to be critically involved in important cell functions such as proliferation and survival. Previous studies have demonstrated that the atypical PKCs are stimulated by tumor necrosis factor alpha (TNF-alpha) and are required for the activation of NF-kappaB by this cytokine through a mechanism that most probably involves the phosphorylation of IkappaB. The inability of these PKC isotypes to directly phosphorylate IkappaB led to the hypothesis that zetaPKC may use a putative IkappaB kinase to functionally inactivate IkappaB. Recently several groups have molecularly characterized and cloned two IkappaB kinases (IKKalpha and IKKbeta) which phosphorylate the residues in the IkappaB molecule that serve to target it for ubiquitination and degradation. In this study we have addressed the possibility that different PKCs may control NF-kappaB through the activation of the IKKs. We report here that alphaPKC as well as the atypical PKCs bind to the IKKs in vitro and in vivo. In addition, overexpression of zetaPKC positively modulates IKKbeta activity but not that of IKKalpha, whereas the transfection of a zetaPKC dominant negative mutant severely impairs the activation of IKKbeta but not IKKalpha in TNF-alpha-stimulated cells. We also show that cell stimulation with phorbol 12-myristate 13-acetate activates IKKbeta, which is entirely dependent on the activity of alphaPKC but not that of the atypical isoforms. In contrast, the inhibition of alphaPKC does not affect the activation of IKKbeta by TNF-alpha. Interestingly, recombinant active zetaPKC and alphaPKC are able to stimulate in vitro the activity of IKKbeta but not that of IKKalpha. In addition, evidence is presented here that recombinant zetaPKC directly phosphorylates IKKbeta in vitro, involving Ser177 and Ser181. Collectively, these results demonstrate a critical role for the PKC isoforms in the NF-kappaB pathway at the level of IKKbeta activation and IkappaB degradation.  (+info)

Promoter and exon-intron structure of the protein kinase C gene from the marine sponge Geodia cydonium: evolutionary considerations and promoter activity. (4/15539)

We report the gene structure of a key signaling molecule from a marine sponge, Geodia cydonium. The selected gene, which codes for a classical protein kinase C (cPKC), comprises 13 exons and 12 introns; the introns are, in contrast to those found in cPKC from higher Metazoa, small in size ranging from 93 nt to 359 nt. The complete gene has a length of 4229 nt and contains exons which encode the characteristic putative regulatory and catalytic domains of metazoan cPKCs. While in the regulatory domain only one intron is in phase 0, in the catalytic domain most introns are phase 0 introns, suggesting that the latter only rarely undergo module duplication. The 5'-flanking sequence of the sponge cPKC gene contains a TATA-box like motif which is located 35-26 nt upstream from the start of the longest sequenced cDNA. This 5'-flanking sequence was analyzed for promoter activity. The longest fragment (538 nt) was able to drive the expression of luciferase in transient transfections of NIH 3T3 fibroblasts; the strong activity of the sponge promoter was found to be half the one displayed by the SV40 reference promoter. Deletion analysis demonstrates that the AP4 site and the GC box which is most adjacent to the TATA box are the crucial elements for maximal promoter activity. The activity of the promoter is not changed in 3T3 cells which are kept serum starved or in the presence of a phorbol ester. In conclusion, these data present the phylogenetically oldest cPKC gene which contains in the 5'-flanking region a promoter functional in the heterologous mammalian cell system.  (+info)

Phosphorylation by protein kinase C decreases catalytic activity of avian phospholipase C-beta. (5/15539)

The potential role of protein kinase C (PKC)-promoted phosphorylation has been examined in the G-protein-regulated inositol lipid signalling pathway. Incubation of [32P]Pi-labelled turkey erythrocytes with either the P2Y1 receptor agonist 2-methylthioadenosine triphosphate (2MeSATP) or with PMA resulted in a marked increase in incorporation of 32P into the G-protein-activated phospholipase C PLC-betaT. Purified PLC-betaT also was phosphorylated by PKC in vitro to a stoichiometry (mean+/-S. E.M.) of 1.06+/-0.2 mol of phosphate/mol of PLC-betaT. Phosphorylation by PKC was isoenzyme-specific because, under identical conditions, mammalian PLC-beta2 also was phosphorylated to a stoichiometry near unity, whereas mammalian PLC-beta1 was not phosphorylated by PKC. The effects of PKC-promoted phosphorylation on enzyme activity were assessed by reconstituting purified PLC-betaT with turkey erythrocyte membranes devoid of endogenous PLC activity. Phosphorylation resulted in a decrease in basal activity, AlF4(-)-stimulated activity, and activity stimulated by 2MeSATP plus guanosine 5'-[gamma-thio]triphosphate in the reconstituted membranes. The decreases in enzyme activities were proportional to the extent of PKC-promoted phosphorylation. Catalytic activity assessed by using mixed detergent/phospholipid micelles also was decreased by up to 60% by phosphorylation. The effect of phosphorylation on Gqalpha-stimulated PLC-betaT in reconstitution experiments with purified proteins was not greater than that observed on basal activity alone. Taken together, these results illustrate that PKC phosphorylates PLC-betaT in vivo and to a physiologically relevant stoichiometry in vitro. Phosphorylation is accompanied by a concomitant loss of enzyme activity, reflected as a decrease in overall catalytic activity rather than as a specific modification of G-protein-regulated activity.  (+info)

Dephosphorylation of the catenins p120 and p100 in endothelial cells in response to inflammatory stimuli. (6/15539)

Inflammatory mediators such as histamine and thrombin increase the tight-junction permeability of endothelial cells. Tight-junction permeability may be independently controlled, but is dependent on the adherens junction, where adhesion is achieved through homotypic interaction of cadherins, which in turn are associated with cytoplasmic proteins, the catenins. p120, also termed p120(cas)/p120(ctn), and its splice variant, p100, are catenins. p120, originally discovered as a substrate of the tyrosine kinase Src, is also a target for a protein kinase C-stimulated pathway in epithelial cells, causing its serine/threonine dephosphorylation. The present study shows that pharmacological activation of protein kinase C stimulated a similar pathway in endothelial cells. Activation of receptors for agents such as histamine (H1), thrombin and lysophosphatidic acid in the endothelial cells also caused serine/threonine dephosphorylation of p120 and p100, suggesting physiological relevance. However, protein kinase C inhibitors, although blocking the effect of pharmacological activation of protein kinase C, did not block the effects due to receptor activation. Calcium mobilization and the myosin-light-chain-kinase pathway do not participate in p120/p100 signalling. In conclusion, endothelial cells possess protein kinase C-dependent and -independent pathways regulating p120/p100 serine/threonine phosphorylation. These data describe a new connection between inflammatory agents, receptor-stimulated signalling and pathways potentially influencing intercellular adhesion in endothelial cells.  (+info)

Salmonella typhimurium and lipopolysaccharide stimulate extracellularly regulated kinase activation in macrophages by a mechanism involving phosphatidylinositol 3-kinase and phospholipase D as novel intermediates. (7/15539)

Activation of the extracellularly regulated kinase (ERK) pathway is part of the early biochemical events that follow lipopolysaccharide (LPS) treatment of macrophages or their infection by virulent and attenuated Salmonella strains. Phagocytosis as well as the secretion of invasion-associated proteins is dispensable for ERK activation by the pathogen. Furthermore, the pathways used by Salmonella and LPS to stimulate ERK are identical, suggesting that kinase activation might be solely mediated by LPS. Both stimuli activate ERK by a mechanism involving herbimycin-dependent tyrosine kinase(s) and phosphatidylinositol 3-kinase. Phospholipase D activation and stimulation of protein kinase C appear to be intermediates in this novel pathway of MEK/ERK activation.  (+info)

Role of iron in Nramp1-mediated inhibition of mycobacterial growth. (8/15539)

Innate resistance to mycobacterial growth is mediated by a gene, Nramp1. We have previously reported that Nramp1 mRNA from macrophages of Mycobacterium bovis BCG-resistant (Bcgr) mice is more stable than Nramp1 mRNA from macrophages of BCG-susceptible (Bcgs) mice. Based on these observations and on reports that show that the closely related Nramp2 gene is a metal ion transporter, we evaluated the effect of iron on the growth of Mycobacterium avium within macrophages as well as on the stability of Nramp1 mRNA. The addition of iron to macrophages from Bcgs mice resulted in a stimulation of mycobacterial growth. In contrast, iron increased the capacity of macrophages from Bcgr mice to control the growth of M. avium. When we treated recombinant gamma interferon (IFN-gamma)-activated macrophages with iron, we found that iron abrogated the growth inhibitory effect of IFN-gamma-activated macrophages from Bcgs mice but that it did not affect the capacity of macrophages from Bcgr mice to control microbial growth. A more detailed examination of the effect of iron on microbial growth showed that the addition of small quantities of iron to resident macrophages from Bcgr mice stimulated antimicrobial activity within a very narrow dose range. The effect of iron on the growth inhibitory activity of macrophages from Bcgr mice was abrogated by the addition of catalase or mannitol to the culture medium. These results are consistent with an Fe(II)-mediated stimulation of the Fenton/Haber-Weiss reaction and hydroxyl radical-mediated inhibition of mycobacterial growth.  (+info)

Dive into the research topics of p21(ras) function is important for T cell antigen receptor and protein kinase C regulation of nuclear factor of activated T cells. Together they form a unique fingerprint. ...
K04166 AGTR1; angiotensin II receptor type 1 K04634 GNAQ; guanine nucleotide-binding protein G(q) subunit alpha K04635 GNA11; guanine nucleotide-binding protein subunit alpha-11 K05858 PLCB; phosphatidylinositol phospholipase C, beta [EC:] K05858 PLCB; phosphatidylinositol phospholipase C, beta [EC:] K05858 PLCB; phosphatidylinositol phospholipase C, beta [EC:] K05858 PLCB; phosphatidylinositol phospholipase C, beta [EC:] K04958 ITPR1; inositol 1,4,5-triphosphate receptor type 1 K04959 ITPR2; inositol 1,4,5-triphosphate receptor type 2 K04960 ITPR3; inositol 1,4,5-triphosphate receptor type 3 K02677 PRKCA; classical protein kinase C alpha type [EC:] K19662 PRKCB; classical protein kinase C beta type [EC:] K19663 PRKCG; classical protein kinase C gamma type [EC:] K18050 PRKCE; novel protein kinase C epsilon type [EC:] K06070 PKD; protein kinase D [EC:] K06070 PKD; protein kinase D [EC:] K06070 PKD; protein ...
TY - JOUR. T1 - Selectivity of connexin 43 channels is regulated through protein kinase C-dependent phosphorylation. AU - Ek-Vitorin, Jose F.. AU - King, Timothy J.. AU - Heyman, Nathanael S.. AU - Lampe, Paul D.. AU - Burt, Janis M.. PY - 2006/6. Y1 - 2006/6. N2 - Coordinated contractile activation of the heart and resistance to ischemic injury depend, in part, on the intercellular communication mediated by Cx43-composed gap junctions. The function of these junctions is regulated at multiple levels (assembly to degradation) through phosphorylation at specific sites in the carboxyl terminus (CT) of the Cx43 protein. We show here that the selective permeability of Cx43 junctions is regulated through protein kinase C (PKC)-dependent phosphorylation at serine 368 (S368). Selective permeability was measured in several Cx43-expressing cell lines as the rate constant for intercellular dye diffusion relative to junctional conductance. The selective permeability of Cx43 junctions under control ...
Complement factor C3, recently found to contain covalently bound phosphate, was phosphorylated in vitro by cyclic AMP-dependent protein kinase (protein kinase A) and Ca2+-activated, phospholipid-dependent protein kinase (protein kinase C). Both protein kinases phosphorylated the same serine residue(s) located in the C3a portion of the alpha-chain. In addition, protein kinase C phosphorylated the beta-chain to a lesser extent. Protein kinase A gave a maximal incorporation of 1 mol of phosphate/mol of C3 while that value with protein kinase C was 1.5 mol of phosphate/mol of C3. The velocity in pmol of [32P]phosphate/(min x unit kinase) was 20 times higher for protein kinase C than for protein kinase A although a 10 times lower ratio of protein kinase to C3 was used in the former case. The apparent Kmfor C3 was 2.6 µM when protein kinase C was used. The phosphorylated C3 was found to be more resistant to partial degradation by trypsin than unphosphorylated C3. It was also found that ...
TY - JOUR. T1 - Identification of a nuclear protein binding element within the rat brain protein kinase C γ promoter that is related to the developmental control of this gene. AU - Chen, Kuang Hua. AU - Widen, Steven. AU - Wilson, Samuel H.. AU - Huang, Kuo Ping. PY - 1993/7/5. Y1 - 1993/7/5. N2 - Protein kinase C γ (PKC γ) is a brain-specific isozyme expressed at a high level in the adult but not in the fetal or newborn rat. At least seventeen nuclear protein binding sites within the 5-flanking region extending from -1612 to +243 had been identified by DNase I footprinting analysis and gel mobility shift assays. Among them, one site, GAATTAATAGG, at -669 to -679 is protected from DNase I digestion by nuclear protein from newborn but not from the adult rat brain. The levels of this binding protein, as determined by gel mobility shift assay, were found inversely related to the levels of PKC γ in rat brain at different stages of development. These results suggest that this particular binding ...
TY - JOUR. T1 - A role for protein kinase C-mediated phosphorylation in eliciting glucagon desensitization in rat hepatocytes. AU - Savage, A.. AU - Zeng, L.. AU - Houslay, M. D.. PY - 1995/4/1. Y1 - 1995/4/1. N2 - An immobilized hepatocyte preparation was used to show that both vasopressin and glucagon could desensitize the ability of glucagon to increase intracellular cyclic AMP concentrations. This process was not dependent on any influx of extracellular Ca2+ and was not mediated by any rise in the intracellular level of Ca2+. The protein kinase C-selective inhibitors chelerythrine, staurosporine and calphostin C acted as potent inhibitors of the desensitization process but with various degrees of selectivity regarding their ability to inhibit the desensitizing actions of glucagon and vasopressin. The protein phosphatase inhibitor okadaic acid was just as potent as vasopressin and glucagon in causing desensitization. Treatment of hepatocyte membranes with alkaline phosphatase restored to near ...
We previously established a cell line from a patient with acute myelomonocytic leukemia with eosinophilia (M4E0), ME-1. ME-1 cells are responsive to colony-stimulating factors (CSFs) such as interleukin-3 (IL-3), IL-4, and granulocyte-macrophage CSF (GM-CSF), and exhibit monocyte-macrophage differentiation. We isolated three subclones, ME-F1 from ME-1, and ME-F2 and ME-F3 from two sublines of ME-1. These subclones had different morphologic, cytochemical, phenotypic, and cytogenetic features. They represented different monocytic-lineage differentiation stages and exhibited different responses to IL-3, GM- CSF, and especially IL-4. IL-3, GM-CSF, and IL-4 enhanced proliferation and differentiation to macrophage-like cells in the ME-F1 subclone. However, they enhanced only proliferation of ME-F2 cells and only differentiation to macrophage-like cells in the ME-F3 subclone. To elucidate possible differences in signal transduction mechanisms in ME- F1, ME-F2, and ME-F3 cells following stimulation by ...
|strong|Mouse anti Human protein kinase C zeta antibody|/strong| recognizes the protein kinase C (PKC) zeta type also known as PKC2.|br||br|Protein kinase C zeta is a member of the PKC family of serin…
TY - JOUR. T1 - Modulation of chemosensitivity in human colon carcinoma cells by downregulating Protein Kinase Cα expression. AU - Chakrabarty, Subhas. AU - Huang, Shuang. PY - 1996/7/1. Y1 - 1996/7/1. N2 - Protein kinase C (PKC) is thought to play a role in tumor progression and drug resistance of colon carcinomas. Specifically, the PKCα isoform has been implicated in drug resistance and responsiveness of colon carcinoma cells to growth factors. Therefore, in this study we determined the effect of downregulating PKCα expression by transfecting human colon carcinoma cells with an antisense PKCα expression vector and then determined the sensitivity of these cells to the anticancer drugs mitomycin C (MMC), 5-fluorouracil (5-FU) and vincristine (Vin). Transiently transfecting the human colon carcinoma cell lines Moser, SW480 and HT29 with antisense PKCα expression vector (but not antisense PKCβ expression vector) consistently increased the sensitivity of these cells to MMC, 5-FU and VIN by ...
TY - JOUR. T1 - Differential effects of protein kinase C inhibitors on chemokine production in human synovial fibroblasts. AU - Jordan, Nicola J.. AU - Watson, Malcolm L.. AU - Yoshimura, Teizo. AU - Westwick, John. PY - 1996. Y1 - 1996. N2 - 1. Rheumatoid arthritis is associated with the accumulation and activation of selected populations of inflammatory cells within the arthritic joint. One putative signal for this process is the production, by resident cells, of a group of inflammatory mediators known as the chemokines. 2. The chemokines interleukin-8 (IL-8), monocyte chemotactic protein-1 (MCP-1) and RANTES (regulated on activation normal T-cell expressed and presumably secreted) are target-cell specific chemoattractants produced by synovial fibroblasts in response to stimulation with interleukin-1α (IL-1α) or tumour necrosis factor α (TNFα). The signalling pathways involved in their production are not well defined. We therefore used four different protein kinase C inhibitors to ...
TY - JOUR. T1 - Protein kinase C regulates the tonic but not the phasic component of contraction in guinea-pig ileum. AU - Sasaguri, T.. AU - Watson, S. P.. PY - 1989/1/1. Y1 - 1989/1/1. N2 - We have investigated the effect of phorbol esters and the down-regulation of protein kinase C on contraction of guinea-pig ileum longitudinal smooth muscle to carbachol and high K+. Phorbol 12,13-dibutyrate (PDBu) enhanced the phasic component and inhibited or enhanced, respectively, the tonic component of contraction to carbachol and high K+. In contrast, 4α-phorbol, which does not activate protein kinase C, had no effect on these responses. Exposure to phorbol 12-myristate 13-acetate (PMA; 1 μM) for up to 8 h induced a time-dependent loss of [3H]-PDBu binding sites, consistent with the down-regulation of protein kinase C by this treatment. The phasic component of contraction to carbachol or high K+ was unaffected following the down-regulation of protein kinase C. The tonic component of contraction to ...
using yeast to study the role of ceramide pathway in the regulation of mammalian protein kinase c isoforms dissertação de mestrado em genetica molecul
Protein kinase C regulates the activity of a diverse group of cellular proteins including membrane ion channel proteins. Although protein kinase C and its substrate protein have been identified in both membrane and cytosolic fractions in the heart, the physiological role of this kinase in the regulation of cardiac function remains unknown. We examined the physiological role of protein kinase C by stimulating its activity with 12-deoxyphorbol 13 isobutyrate 20 acetate (DPBA) in human trabeculae carneae. This resulted in decreased peak isometric twitch force and peak intracellular sarcoplasmic reticulum calcium release as detected with aequorin. Furthermore, in the presence of DPBA, steady-state force-[Ca2+] relations were shifted to higher intracellular calcium concentrations, and the Hill coefficient was reduced, indicating a decrease in responsiveness of the myofilaments to calcium and a change in cooperativity among thin filament proteins, respectively. Thus, DPBA affects not only ...
wp-content/uploads/2018/08/johns_hopkins_medicine_logo-300-x-156-300x156.jpg 0 0 admin /wp-content/uploads/2018/08/johns_hopkins_medicine_logo-300-x-156-300x156.jpg admin2014-08-08 15:04:382018-08-11 11:48:32Phosphorylation of protein kinase C sites Ser42/44 decreases Ca(2+)-sensitivity and blunts enhanced length-dependent activation in response to protein kinase A in human cardiomyocytes ...
Effects of pentoxifylline and protein kinase C inhibitor on phorbol ester-induced intercellular adhesion molecule-1 expression in brain microvascular endothelial cells.
TY - JOUR. T1 - Inhibition of the spontaneous rate of contraction of neonatal cardiac myocytes by protein kinase C isozymes. T2 - A putative role for the ε isozyme. AU - Johnson, John A. AU - Mochly-Rosen, Daria. PY - 1995/1/1. Y1 - 1995/1/1. N2 - Protein kinase C (PKC) enzymes regulate numerous cardiac functions. In the present study, we determined the effects of the PKC-activating drug 4-β phorbol 12-myristate 13-acetate (4-β PMA) on the rate of contraction and correlated these changes with the distribution and levels of α-, β-, δ-, ε-, and ζ-PKC isozymes by using neonatal rat cardiac myocytes in culture. Treatment with 0.3 to 100 nmol/L 4-β PMA caused negative chronotropic effects on contraction. This effect was maximal at a concentration of 3 nmol/L 4-β PMA and correlated with redistribution of the α- and ε-PKC isozymes from the cytosolic to the particulate cell fraction. After a 1-hour treatment with 100 nmol/L PMA, the α- and β-PKC isozymes and an 80-kD ζ- like PKC isozyme ...
TY - JOUR. T1 - Isolation and characterization of two new Drosophila protein kinase C genes, including one specifically expressed in photoreceptor cells. AU - Schaeffer, Eric. AU - Smith, Dean. AU - Mardon, Graeme. AU - Quinn, William. AU - Zuker, Charles. PY - 1989/5/5. Y1 - 1989/5/5. N2 - We have isolated and characterized two new protein kinase C (PKC) genes from D. melanogaster. One, dPKC98F, maps to chromosome region 98F and displays over 60% amino acid sequence identity with members of a recently described PKC-related subfamily in mammals. The other, dPKC53E(ey), maps to region 53E 4-7 on the second chromosome and lies within 50 kb of a PKC gene previously characterized (dPKC). While dPKC98F transcripts are expressed throughout development, expression of the two genes mapping at cytogenetic location 53E is primarily in adults. dPKC98F and the previously reported 53E gene are transcribed predominantly in brain tissue. In contrast, dPKC53E(ey) is transcribed only in photoreceptor cells. We ...
We found that removal of Ca2+ and inhibition of PKC prevented high Pi-induced O2·− production (Figures 3A and 3B), indicating a role for mechanosensitive Ca2+ signaling and PKC-dependent pathways in high Pi-induced upregulation of NAD(P)H oxidase activity. This idea is consistent with the findings that high Pi elicited significantly greater increases in smooth muscle [Ca2+]i than normal levels of Pi (Figure 4). The important role of Ca2+ signaling is also supported by the finding that administration of a Ca2+ ionophore resulted in significantly increased arterial O2·− production (Figure 3C). Further, pharmacological activation of PKC2 elicited substantial increases in arterial NAD(P)H oxidase-derived O2·− generation (Figure 3C). Because removal of Ca2+ during high-pressure treatment prevented endothelial dysfunction (Figure 1) and increases in O2·− production in high Pi-exposed arteries (Figure 3A) and phorbol ester-stimulated O2·− generation in normotensive arteries could also be ...
This investigation deals with the molecular mechanism of anti-human immunodeficiency virus type 1 (HIV-1) action of pentoxifylline (PTX) [1-(5′-oxohexyl)-3,7-dimethylxanthine] a drug widely used for the treatment of conditions involving defective regional microcirculation. The inhibition by PTX of protein kinase C (PKC) or cAMP-dependent protein kinase (PKA)-mediated activation by phorbol ester (PMA) and tumor necrosis factor alpha (TNF-α) of HIV-1-LTR-regulated reporter gene expression was studied in human CD4+ T lymphocytes (Jurkat) and human embryo kidney cells (293-27-2). A protein kinase C is involved in activation of NF-κB in whole cells, identified by using inhibitors specific for PKC- or PKA-catalyzed NF-κB activation in whole cell and cell-free systems. PTX inhibited PKC- or PKA-catalyzed activation of NF-κB in cytoplasmic extracts from unstimulated Jurkat or 293-27-2 cells, but not interaction of preactivated NF-κB with its motifs. Calphostin C, a specific inhibitor of PKC, inhibited NF
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TY - JOUR. T1 - Photoactivated inhibition of superoxide generation and protein kinase C activity in neutrophils by blepharismin, a protozoan photodynamically active pigment. AU - Watanabe, Yoshiya. AU - E-ige, Keisuke. AU - Kobuchi, Hirotsugu. AU - Kato, Yoji. AU - Matsuoka, Tatsuomi. AU - Utsumi, Toshihiko. AU - Yoshioka, Tamotsu. AU - Horton, Alan A.. AU - Utsumi, Kozo. PY - 1995/2/14. Y1 - 1995/2/14. N2 - Blepharismin is an endogenous photosensitizing pigment found in the protozoan Blepharisma. This pigment inhibited the generation of Superoxide anion (O2-) in neutrophils not only via a diacylglycerol-induced protein kinase C (PKC)-dependent reaction but also by an arachidonate-induced PKC-independent reaction. The inhibition was light and concentration dependent for both reactions. Light-activated inhibition was strong at wavelengths between 520 and 570nm but not above 610nm. PKC activity in neutrophils and from rat brain was inhibited by blepharismin in a light- and concentration dependent ...
TY - JOUR. T1 - Differential effects of protein kinase C on the levels of epithelial Na+ channel subunit proteins. AU - Stockand, James D. AU - Hui-Fang, B.. AU - Schenck, J.. AU - Malik, B.. AU - Middleton, P.. AU - Schlanger, L. E.. AU - Eaton, D. C.. PY - 2000/8/18. Y1 - 2000/8/18. N2 - Regulation of epithelial Na+ channel (ENaC) subunit levels by protein kinase C (PKC) was investigated in A6 cells. PKC activation altered ENaC subunit levels, differentially decreasing the levels of both β and γ, but not αENaC. Temporal regulation of β and γENaC by PKC differed; γENaC decreased with a time constant of3.7 ± 1.0 h, whereas βENaC decreased in 13.9 ±3.0h. Activation of PKC also resulted in a decrease in trans-epithelial Na+ reabsorption for up to 48h. PMA activation of PKC resulted in negative feedback inhibition of PKC protein levels beginning within 4h. Both β and γENaC levels, as well as transport tended toward pretreatment values after 48 h of PMA treatment. PKC inhibitors ...
TY - JOUR. T1 - Synthesis and protein kinase C binding activity of benzolactam-V7. AU - Ma, Dawei. AU - Wang, Guoqiang. AU - Wang, Shaomeng. AU - Kozikowski, Alan P.. AU - Lewin, Nancy E.. AU - Blumberg, Peter M.. PY - 1999/5/17. Y1 - 1999/5/17. N2 - Benzolactam-V7 (3a), a simplified analogues of (-)-indolactam-V with twist-form conformation, was synthesized and evaluated as a new protein kinase C modulator. Both 3a and its-7-substituted analogue 3c showed weak binding activity to displace PDBU binding from recombinant PKCα.. AB - Benzolactam-V7 (3a), a simplified analogues of (-)-indolactam-V with twist-form conformation, was synthesized and evaluated as a new protein kinase C modulator. Both 3a and its-7-substituted analogue 3c showed weak binding activity to displace PDBU binding from recombinant PKCα.. UR - UR - U2 - ...
TY - JOUR. T1 - Role of Ras in signal transduction from the nerve growth factor receptor. T2 - Relationship to protein kinase C, calcium and cyclic AMP. AU - Szeberenyi, J.. AU - Erhardt, P.. AU - Cai, H.. AU - Cooper, G. M.. PY - 1992/1/1. Y1 - 1992/1/1. N2 - A dominant inhibitory ras mutant (Ha-ras Asn-17) has been used to investigate the role of Ras in nerve growth factor (NGF)-mediated signal transduction in PC12 cells. Expression of Ha-Ras Asn-17 blocks neuronal differentiation of these cells in response to NGF treatment. The Ha-Ras Asn-17 block was bypassed by treatment with NGF plus dibutyryl cAMP or NGF plus the Ca2+ ionophore ionomycin, but not by NGF plus 12-O-tetradecanoyl phorbol acetate (TPA). Direct stimulation of the cAMP or Ca2+ pathways thus appeared to act synergistically with a Ras-independent NGF signaling pathway. This Ras-independent pathway was also distinct from protein kinase C, since its activity was not affected by protein kinase C down-regulation. It thus appears that ...
Protein Kinase C Theta Type (nPKC Theta or PRKCQ or EC - Pipeline Review, H1 2017 Size and Share Published in 2017-05-30 Available for US$ 3500 at
Correlation between endogenous membrane PKC activity and proliferation versus differentiation of normal and HPV16 transformed rat myoblast (L 6 cells): Histochem.J.
Catalytic domain of the Protein Serine/Threonine Kinase, Classical Protein Kinase C. Serine/Threonine Kinases (STKs), Classical (or Conventional) Protein Kinase C (cPKC) subfamily, catalytic (c) domain. STKs catalyze the transfer of the gamma-phosphoryl group from ATP to serine/threonine residues on protein substrates. The cPKC subfamily is part of a larger superfamily that includes the catalytic domains of other protein STKs, protein tyrosine kinases, RIO kinases, aminoglycoside phosphotransferase, choline kinase, and phosphoinositide 3-kinase (PI3K). PKCs are classified into three groups (classical, atypical, and novel) depending on their mode of activation and the structural characteristics of their regulatory domain. PKCs undergo three phosphorylations in order to take mature forms. In addition, cPKCs depend on calcium, DAG (1,2-diacylglycerol), and in most cases, phosphatidylserine (PS) for activation. cPKCs contain a calcium-binding C2 region in their regulatory domain. There are four cPKC ...
The activity of calcium-, phospholipid-dependent protein kinase (PKc) was measured in (a) total extracts, (b) crude membrane, and (c) cytosolic fractions of chick embryo myogenic cells differentiating in culture. Total PKc activity slowly declines during the course of terminal myogenesis in contrast to the activity of cAMP-dependent protein kinase, which was also measured in the same cells. Myogenic cells at day 1 of culture possess high particulate and low soluble PKc activity. A dramatic decline of particulate PKc activity occurs during myogenic cell differentiation and is accompanied, through day 4, by a striking rise of the soluble activity. The difference in the subcellular distribution of PKc between replicating myoblasts and myotubes is confirmed by phosphorylation studies conducted in intact cells. These studies demonstrate that four polypeptides whose phosphorylation is stimulated by the tumor promoter 12-O-tetradecanoyl phorbol 13-acetate in myotubes, are spontaneously phosphorylated ...
TY - JOUR. T1 - NMDA receptor blockade prevents the increase in protein kinase C substrate (protein F1) phosphorylation produced by long-term potentiation. AU - Linden, David J.. AU - Wong, Ka L.. AU - Sheu, Fwu Shan. AU - Routtenberg, Aryeh. PY - 1988/8/16. Y1 - 1988/8/16. N2 - Recent evidence has implicated activation of the N-methyl-d-aspartate (NMDA) class of glutamate receptor in the initiation of hippocampal long-term potentiation (LTP), an electrophysiological model of information storage in the brain. A separate line of evidence has suggested that activation of protein kinase C (PKC) and the consequent phosphorylation of it substrates is necessary for the maintenance of the LTP response. To determine if PKC activation is a consequence of NMDA receptor activation during LTP, we applied the NMDA receptor antagonist drug, dl-aminophosphonovalerate (APV) both immediately prior to and following high frequency stimulation, resulting in successful and unsuccessful blockade of LTP initiation, ...
Octadecadienoic acids (linoleic acid and linolelaidic acid) and the diacylglycerol, 1-oleoyl-2-acetyl-rac-glycerol (OAG) concentration-dependently induced activation of gel-filtered human platelets, i.e. aggregation and phosphorylation of 20 kDa and 47 kDa peptides. In contrast, octadecenoic acids (oleic and elaidic acid) and octadecanoic (stearic) acid were inactive. Octadecadienoic acid-induced platelet activation was suppressed by the protein kinase C inhibitor, polymyxin B, but not by the cyclooxygenase inhibitor, indomethacin. OAG-induced activation was potentiated by octadecadienoic acids present at non-stimulatory concentrations. Our data suggest that octadecadienoic acids and diacylglycerol synergistically induce platelet activation via protein kinase C. Furthermore, linolelaidic acid may provide a useful experimental tool to study fatty acid regulation of protein kinase C in intact cells. ...
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TY - JOUR. T1 - Functional mapping of the promoter region of the GNB2L1 human gene coding for RACK1 scaffold protein. AU - Del Vecchio, Igor. AU - Zuccotti, Annalisa. AU - Pisano, Federica. AU - Canneva, Fabio. AU - Lenzken, Silvia C.. AU - Rousset, Francoise. AU - Corsini, Emanuela. AU - Govoni, Stefano. AU - Racchi, Marco. PY - 2009/2/1. Y1 - 2009/2/1. N2 - RACK1 (Receptor for Activated C Kinase 1) is a scaffold protein for different kinases and membrane receptors. Previously, we characterized an age-dependent decline of RACK1 protein expression which could be counteracted with DHEA (dehydroepiandrosterone) [Corsini, E., et al. 2002. In vivo dehydroepiandrosterone restores age-associated defects in the protein kinase C signal transduction pathway and related functional responses. J. Immunol. 168, 1753-1758. and Corsini, E., et al. 2005. Age-related decline in RACK-1 expression in human leukocytes is correlated to plasma levels of dehydroepiandrosterone. J. Leukoc. Biol. 77, 247-256.]. ...
Translocation of PKC isoforms has been implicated in mechanisms involved in heart failure, 22myocardial hypertrophy, 23and preconditioning. PKC isoforms are activated by phosphorylating enzymes such as G proteins and are modified in enzyme activity by phospholipids, diacylglycerol, increased Ca2+, nitric oxide, and superoxide anions. This is followed by translocation in an isoform-specific and cytoskeleton-mediated manner to subcellular targets, which can be directly visualized by immunohistochemical methods. Only 10 min of ischemia 24or brief administrations of pharmacologic agents 11,25may elicit significant PKC translocation. Recent evidence indicates that translocation is dependent on PKC binding to a family of proteins called receptors of activated C kinase. 26These anchoring proteins are highly specific, and each PKC isoenzyme can bind to only one receptor of activated C kinase. Thus, different PKC isoforms may be linked to distinctive aspects of myocardial function, and this functional ...
The N-methyl-D-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, which plays crucial roles in synaptic plasticity and development. We have recently shown that potentiation of NMDA receptor function by protein kinase C (PKC) appears to be mediated via activation of non-receptor tyrosine kinases. The aim of this study was to test whether this effect could be mediated by direct tyrosine phosphorylation of the NR2A or NR2B subunits of the receptor. Following treatment of rat hippocampal CA1 mini-slices with 500 nM phorbol 12-myristate 13-acetate (PMA) for 15 min, samples were homogenized, immunoprecipitated with anti-NR2A or NR2B antibodies and the resulting pellets subjected to Western blotting with antiphosphotyrosine antibody. An increase in tyrosine phosphorylation of both NR2A (76 +/- 11% above control) and NR2B (41 +/- 11%) was observed. This increase was blocked by pretreatment with the selective PKC inhibitor chelerythrine, with the tyrosine kinase inhibitor Lavendustin A or with the
TY - JOUR. T1 - Unique functions for protein kinase D1 and protein kinase D2 in mammalian cells. AU - Matthews, Sharon A.. AU - Navarro, Maria N.. AU - Sinclair, Linda V.. AU - Emslie, Elizabeth. AU - Feijoo-Carnero, Carmen. AU - Cantrell, Doreen A.. PY - 2010/11/15. Y1 - 2010/11/15. N2 - Mammalian PKD (protein kinase D) isoforms have been implicated in the regulation of diverse biological processes in response to diacylglycerol and PKC (protein kinase C) signalling. To compare the functions of PKD1 and PKD2 in vivo, we generated mice deficient in either PKD1 or PKD2 enzymatic activity, via homozygous expression of PKD1(S744A/S7484) or PKD2(S707A/S711A) knockin alleles. We also examined PKD2-deficient mice generated using gene-trap technology. We demonstrate that, unlike PKD I, PKD2 catalytic activity is dispensable for normal embryogenesis. We also show that PKD2 is the major PKD isoform expressed in lymphoid tissues, but that PKD2 catalytic activity is not essential for the development of ...
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TY - JOUR. T1 - Chromatinized Protein Kinase C-theta: Can It Escape the Clutches of NF-kB?. AU - Sutcliffe, Elissa. AU - Li, Jasmine. AU - Zafar, Anjum. AU - Hardy, Kristine. AU - Ghildyal, Reena. AU - Norris, Nicole. AU - Lim, Chloe (Pek Siew). AU - Milburn, Peter. AU - Casarotto, Marco. AU - Denyer, Gareth. AU - Rao, Sudha. PY - 2012. Y1 - 2012. N2 - We recently provided the first description of a nuclear mechanism used by Protein Kinase C-theta (PKC-θ) to mediate T cell gene expression. In this mode, PKC-θ tethers to chromatin to form an active nuclear complex by interacting with proteins including RNA polymerase II, the histone kinase MSK-1, the demethylase LSD1, and the adaptor molecule 14-3-3ζ at regulatory regions of inducible immune response genes. Moreover, our genome-wide analysis identified many novel PKC-θ target genes and microRNAs implicated in T cell development, differentiation, apoptosis, and proliferation. We have expanded our ChIP-on-chip analysis and have now identified a ...
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We have provided clear evidence that insulin activation of all three signaling components, Viz., IRS-1-dependent PI 3-Kinase, atypical protein kinase C (aPKC) and PKB/Akt is defective in diabetic muscle. These defects are best seen when insulin activation is conducted at both half-maximal and maximal stimulation. Moreover, whereas previous studies had shown that treatment with metformin (Met) alone improves aPKC activation, or that treatment with thiazolidinedione (TZD) alone produces increases in activation of IRS-1/PI3K and aPKC when evaluated at maximal insulin stimulation, we have recently found that combined treatment with Met plus TZD for 6 weeks provokes marked increases in insulin effects on all three signaling factors at both half-maximal and maximal insulin stimulation. This work is being prepared for submission for publication.. We have also evaluated the improvement in insulin signaling in diabetic muscle 4 hours after acute endurance (one-legged) exercise and found that the ...
FIG. 3. Expression of PKC-α, -βI, and -βII isoforms in membrane and cytosolic fractions of DRG in experimental animals. Western blot analysis showed a single band of each isoform in all groups (A). Compared with nondiabetic littermate control mice (Lm) and transgenic mice (Tg), densitometric analysis disclosed reduced expression of membrane α isoform in both diabetic littermate mice (LmDM) and diabetic transgenic mice (TgDM), and the change in diabetic transgenic mice was more severe than in diabetic littermate mice (B). By contrast, cytosolic fraction of α isoform was contrariwise increased to a similar extent in both diabetic transgenic mice and diabetic littermate mice. Treatment with an ARI (fidarestat) corrected these changes in both diabetic groups (LmDM+ARI and TgDM+ARI). There was no change in βI expression in either membrane or cytosolic fraction among all groups. On the other hand, membrane βII expression tended to be elevated in diabetic littermate mice, and the increase was ...
We have isolated and characterized two new protein kinase C (PKC) genes from D. melanogaster. One, dPKC98F, maps to chromosome region 98F and displays over 60% amino acid sequence identity with members of a recently described PKC-related subfamily in mammals. The other, dPKC53E(ey), maps to region …
Protein kinase C has been in the spotlight since the discovery two decades ago that it is activated by the lipid second messenger diacylglycerol. Despite protein kinase Cs enduring stage presence, the regulation and specific roles of its isozymes in defined cellular processes are still under intens …
|p|GF 109203X is a potent and selective inhibitor of protein kinase C [1].|/p||p| Protein kinase C (PKC) is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of serine and threon
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The acetylcholine analogue carbachol rapidly activated mitogen-activated protein kinase (MAPK), and caused tyrosine phosphorylation of the adapter protein p52 Shc and the epidermalgrowth factor (EGF) receptor, in human embryonic kidney cells stably expressing m3 muscarinic receptors. The protein kinase C (PKC) inhibitor GF109203X caused a significant partial inhibition of m3 receptor-mediated activation of MAPK. The PKC-independent MAPK activity elicited by carbachol in the presence of GF109203X was reproducibly abolished by AG1478, an inhibitor of EGF-receptor tyrosine kinase activity, and by the Src tyrosine kinase inhibitor PP1. In a subset of these experiments, GF109203X concomitantly increased carbachol-induced tyrosine phosphorylation of p52 Shc and the EGF receptor. In co-stimulation experiments, carbachol and EGF activated MAPK in a non-additive fashion; moreover, EGF-induced association of Shc with the phosphorylated EGF receptor was inhibited by carbachol. This effect of carbachol was ...
Protein kinase C, commonly abbreviated to PKC (EC, is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins, or a member of this family. PKC enzymes in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca2+). Hence PKC enzymes play important roles in several signal transduction cascades. The PKC family consists of fifteen isozymes in humans. They are divided into three subfamilies, based on their second messenger requirements: conventional (or classical), novel, and atypical. Conventional (c)PKCs contain the isoforms α, βI, βII, and γ. These require Ca2+, DAG, and a phospholipid such as phosphatidylserine for activation. Novel (n)PKCs include the δ, ε, η, and θ isoforms, and require DAG, but do not require Ca2+ for activation. Thus, conventional and novel PKCs are ...
Treatment of intact NIH 3T3 cells with 12-O-tetradecanoylphorbol-13-acetate (TPA) causes a rapid redistribution (stabilization) of protein kinase C to the particulate fraction. Part of the enzyme activity stabilized to the membrane fraction in response to TPA can be recovered associated with nuclear-cytoskeletal components. An apparently pure nuclear fraction prepared from NIH 3T3 cells was found to contain 25-30% of the total membrane-associated protein kinase C activity when isolated in the presence of Ca2+. In untreated control cells, most of this activity found with the nuclear fraction can be extracted by chelators. Phorbol easter (TPA) treatment of NIH 3T3 cells induces the tight association of protein kinase C to the nucleus; this tightly bound activity is not dissociable by chelators and can be recovered only by solubilization with detergent. Nuclei purified from untreated human promyelocytic leukemic HL-60 cells contain higher amounts of chelator-stable, detergent-extractable protein ...
TY - JOUR. T1 - Decrease in cytosolic calcium/phospholipid-dependent protein kinase activity following phorbol ester treatment of EL4 thymoma cells. AU - Kraft, A. S.. AU - Anderson, W. B.. AU - Cooper, H. L.. AU - Sando, J. J.. N1 - Copyright: Copyright 2004 Elsevier B.V., All rights reserved.. PY - 1982. Y1 - 1982. UR - UR - M3 - Article. C2 - 7142138. AN - SCOPUS:0020356002. VL - 257. SP - 13193. EP - 13196. JO - Journal of Biological Chemistry. JF - Journal of Biological Chemistry. SN - 0021-9258. IS - 22. ER - ...
MARCKS (myristoylated alanine-rich protein kinase C substrate), Authors: Atsuhiro Tanabe, Maho Saito. Published in: Atlas Genet Cytogenet Oncol Haematol.
Phorbol ester-sensitive EL4 murine thymoma cells respond to phorbol 12-myristate 13-acetate with activation of ERK mitogen-activated protein kinases, synthesis of interleukin-2, and death, whereas phorbol ester-resistant variants of this cell line do not exhibit these responses. Additional aspects of the resistant phenotype were examined, using a newly-established resistant cell line. Phorbol ester induced morphological changes, ERK activation, calcium-dependent activation of the c-Jun N-terminal kinase (JNK), interleukin-2 synthesis, and growth inhibition in sensitive but not resistant cells. A series of protein kinase C activators caused membrane translocation of protein kinase Cs (PKCs) alpha, eta, and theta in both cell lines. While PKC eta was expressed at higher levels in sensitive than in resistant cells, overexpression of PKC eta did not restore phorbol ester-induced ERK activation to resistant cells. In sensitive cells, PKC activators had similar effects on cell viability and ERK ...
Looking for online definition of Protein-kinase C-related kinase 2 in the Medical Dictionary? Protein-kinase C-related kinase 2 explanation free. What is Protein-kinase C-related kinase 2? Meaning of Protein-kinase C-related kinase 2 medical term. What does Protein-kinase C-related kinase 2 mean?
Ludwig, L.M.; Weihrauch, D.; Kersten, J.R.; Pagel, P.S.; Warltier, D.C., 2004: Protein kinase C translocation and Src protein tyrosine kinase activation mediate isoflurane-induced preconditioning in vivo: potential downstream targets of mitochondrial adenosine triphosphate-sensitive potassium channels and reactive oxygen species
As the colonic epithelium is physiologically exposed to butyrate and to activators of protein kinase C, we examined the effect of the protein kinase C signalling pathway on butyrate-induced expression of markers of differentiation. Activators and inhibitors of protein kinase C were used in combination with butyrate and effects on the expression of markers of differentiation examined in colon cancer cell lines. When the protein kinase C activator phorbol myristate acetate (100 nM) was added for 24 h prior to the addition of 2 mM butyrate, there was a synergistic increase in alkaline phosphatase activity (154 ± 11% above that for butyrate alone, P = 0.003) in a concentration- and time-dependent manner. Butyrate-induced expression of carcinoembryonic antigen and interleukin-8, dome formation and cell turnover were also markedly augmented by pre-treatment with phorbol myristate acetate. A similar effect was observed with propionate or acetate (but not other differentiating agents), when phorbol ...
Protein kinase C is the Ca{dollar}\sp{lcub}2+{rcub}{dollar}/phospholipid-dependent enzyme that serves as the receptor for, and is directly activated by, the tumour-promoting phorbol esters. To examine the involvement of protein kinase C in the regulation of the organization or function of the actin-containing microfilaments, the activity of the enzyme towards two distinct groups of proteins that are thought to be involved in microfilament regulation has been investigated. For these studies, protein kinase C was partially purified from bovine brain or was more extensively purified from rat brain. Two proteins that are localized in certain areas of microfilament-membrane attachment (focal contacts), vinculin and talin, were identified as in vitro substrates for protein kinase C. Purified protein kinase C also phosphorylated chicken gizzard myosin light chain kinase and different forms of caldesmon, proteins that are involved in the regulation of contractile events. Chicken gizzard caldesmon and chicken
Protein kinase C beta II (PKCβII) has been implicated in diabetic nephropathy (DN). Mesangial cell (MC) hypertrophy is a pathologic feature of DN. PKCβII...
TY - JOUR. T1 - Protein kinase C effects on nerve function, perfusion, Na+,K+-ATPase activity and glutathione content in diabetic rats. AU - Cameron, Norman E. AU - Cotter, M A AU - Jack, A M AU - Basso, M D AU - Hohman, T C PY - 1999. Y1 - 1999. N2 - Aims/hypothesis. Increased protein kinase C activity has been linked to diabetic vascular complications in the retina and kidney, which were attenuated by protein kinase C antagonist treatment. Neuropathy has a vascular component, therefore, the aim was to assess whether treatment with WAY151003 or chelerythrine, inhibitors of protein kinase C regulatory and catalytic domains respectively, could correct nerve blood flow, conduction velocity, Na+,K+-ATPase, and glutathione deficits in diabetic rats.Methods. Diabetes was induced by streptozotocin. Sciatic nerve conduction velocity was measured in vivo and sciatic endoneurial perfusion was monitored by microelectrode polarography and hydrogen clearance. Glutathione content and Na+,K+-ATPase activity ...
TY - JOUR. T1 - Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. AU - Rizvi, Mujahid A.. AU - Ghias, Kulsoom. AU - Davies, Katharine M.. AU - Ma, Chunguang. AU - Weinberg, Frank. AU - Munshi, Hidayatullah G.. AU - Krett, Nancy L.. AU - Rosen, Steven T.. N1 - Copyright: Copyright 2008 Elsevier B.V., All rights reserved.. PY - 2006/7. Y1 - 2006/7. N2 - Enzastaurin (LY317615), an acyclic bisindolylmaleimide, is an oral inhibitor of the protein kinase Cβ isozyme. The objective of this study was to assess the efficacy of enzastaurin in inducing apoptosis in multiple myeloma (MM) cell lines and to investigate possible mechanisms of apoptosis. Cell proliferation assays were done on a variety of MM cell lines with unique characteristics (dexamethasone sensitive, dexamethasone resistant, chemotherapy sensitive, and melphalan resistant). The dexamethasone-sensitive MM.1S cell line was used to further assess the effect ...
Atypical protein kinase C (PKC) isoforms play essential roles in lots of neural processes including synaptic plasticity and neurodegenerative diseases. the appearance of atypical PKCs in phrenic electric MRS 2578 motor neurons offers a construction within which to assess their function in respiratory electric motor control including book types of respiratory plasticity recognized to occur in this area. 2000 Provided their function in synaptic plasticity we questioned whether atypical PKCs can be found in the phrenic electric motor nucleus an integral site for respiratory electric motor plasticity (Mitchell proteins expression thats diminished as well as non-existent (e.g. Sanders and Ridyard 2000 Cell lifestyle circumstances change from the surroundings potentially resulting in altered proteins appearance. The strength of labeling within phrenic electric motor neurons described right here shows that atypical PKC isoforms possess the to be engaged in essential neuron-specific functions like the ...
RESULTS: Pterostilbene possessed comparable antioxidant properties as resveratrol in cell free system. Computational methods were used to establish the molecular characteristics of stilbene derivatives. The values of electronic parameters suggest a slight enhancement of electron donor properties of pterostilbene compared to resveratrol. Phosphorylation and thus activation of protein kinase C alpha/beta II in activated neutrophils was not decreased by pterostilbene. Pterostilbene in concentrations of 10-100 μM was found to inhibit the activity of human caspase-3 purified enzyme and did not influence cell viability significantly ...
TY - JOUR. T1 - Expression of amyloid beta peptide in human platelets. T2 - Pivotal role of the phospholipase Cγ2-protein kinase C pathway in platelet activation. AU - Shen, Ming Yi. AU - Hsiao, George. AU - Fong, Tsorng Han. AU - Chou, Duen Suey. AU - Sheu, Joen Rong. PY - 2008/2. Y1 - 2008/2. N2 - The amyloid β peptide (Aβ), a mediator of neuronal and vascular degeneration in the pathogenesis of Alzheimers disease and cerebral amyloid angiopathy may have peripheral actions. Platelets are enriched with Aβ and have been shown to enhance platelet actions. However, the detailed signaling pathways through which Aβ activates platelets have not been previously explored. In this study, we examined the intra-platelet Aβ distribution using a gold labeling technique and noted that Aβ was predominantly localized in the cytoplasm of resting platelets. A marked increase in Aβ-gold labeling in an open canalicular system was observed in collagen-activated platelets. Exogenous Aβ (2-10 μM) ...
BACKGROUND: Titin is a giant protein crucial for the assembly and elasticity of the sarcomere. Recently, titin has been linked to signal transduction through its kinase domain, which has been proposed to sense mechanical load. We developed a knockout in which expression of M-line-deficient titin can be induced in adult mice and investigated the role of the titin kinase region in cardiac function. METHODS AND RESULTS: Isolated heart experiments revealed that in titin M-line-deficient mice, the contractile response to beta-adrenergic agonists and extracellular calcium is reduced. However, the Ca(2+) sensitivity and cooperativity of activation of skinned cardiac muscle were unchanged. In knockout mice, calcium transients showed a reduced rate of calcium uptake, and expression analysis showed reduced levels of calmodulin, phospholamban, and SERCA2. Ultimately, knockout mice developed cardiac hypertrophy and heart failure, which involves protein kinase C signal transduction but not the ...
TY - JOUR. T1 - Amelioration of denervation-induced atrophy by clenbuterol is associated with increased PKC-alpha activity. AU - Sneddon, Alan Arthur. AU - Delday, Margaret Inkster. AU - Maltin, Charlotte. PY - 2000/7. Y1 - 2000/7. N2 - Rat soleus muscle was denervated for 3 or 7 days, and total membrane protein kinase C (PKC) activity and translocation and immunocytochemical localization of PKC isoforms were examined. Dietary administration of clenbuterol concomitant with denervation ameliorated the atrophic response and was associated with increased membrane PKC activity at both 3 (140%) and 7 (190%) days. Of the five PKC isoforms (alpha, epsilon, theta, zeta, and mu) detected in soleus muscle by Western immunoblotting, clenbuterol treatment affected only the PKC-alpha and PKC-theta forms. PKC-alpha was translocated to the membrane fraction upon denervation, and the presence of clenbuterol increased membrane-bound PKC-alpha and active PKC-alpha as assayed by Ser(657) phosphorylation. PKC-theta ...
Sugita M., Kuwata H., Kudo I., Hara S.. Protein kinase C (PKC) is a family of serine/threonine kinases involved in various signal transduction pathways. We investigated the roles of PKC in the regulation of group IIA secreted phospholipase A(2) (sPLA(2)-IIA) expression in cytokine-stimulated rat fibroblastic 3Y1 cells. Here we show that the induction of sPLA(2)-IIA by proinflammatory cytokines was under the control of both classical cPKCalpha and atypical aPKClambda/iota pathways by using PKC inhibitors, a PKC activator, and PKC knockdowns. Treatment of 3Y1 cells with PKC selective inhibitors having broad specificity, such as chelerythrine chloride and GF109203X, blocked IL-1beta/TNFalpha-dependent induction of sPLA(2)-IIA protein in a dose-dependent manner. Treatment with the PKC activator phorbol 12-myristate 13-acetate (PMA), which activates cPKC and novel nPKC isoforms, markedly attenuated the cytokine-dependent induction of sPLA(2)-IIA expression. In comparison, 24-h pretreatment with PMA, ...
1. Huang KP, Huang FL, Jager T, Li J, Reymann KG, Balschun D. Neurogranin/RC3 enhances long-term potentiation and learning by promoting calcium-mediated signaling. J Neurosci. 2004;24:10660-10669 2. Baudier J, Deloulme JC, Van Dorsselaer A, Black D, Matthes HW. Purification and characterization of a brain-specific protein kinase C substrate, neurogranin (p17). Identification of a consensus amino acid sequence between neurogranin and neuromodulin (GAP43) that corresponds to the protein kinase C phosphorylation site and the calmodulin-binding domain. J Biol Chem. 1991;266:229-237 3. Sheu FS, Mahoney CW, Seki K, Huang KP. Nitric oxide modification of rat brain neurogranin affects its phosphorylation by protein kinase C and affinity for calmodulin. J Biol Chem. 1996;271:22407-22413 4. Cohen RW, Margulies JE, Coulter PM 2nd, Watson JB. Functional consequences of expression of the neuron-specific, protein kinase C substrate RC3 (neurogranin) in Xenopus oocytes. Brain Res. 1993;627:147-152 5. Yang HM, ...
Global Markets Directs, Protein Kinase C Epsilon Type (nPKC Epsilon or PRKCE or EC - Pipeline Review, provides in depth analysis on Protein Kinase C Epsilon Type (nPKC Epsilon or PRKCE or EC targeted pipeline therapeutics.
TY - JOUR. T1 - Phase I trial of high-dose tamoxifen in combination with cisplatin in patients with lung cancer and other advanced malignancies. AU - Perez, Edith A.. AU - Gandara, David R.. AU - Edelman, Martin J.. AU - ODonnell, Robert. AU - Lauder, Ignacio J.. AU - DeGregorio, Michael. PY - 2003/3/18. Y1 - 2003/3/18. N2 - Background. Tamoxifen has been reported to enhance the antitumor activity of cisplatin in preclinical models by modulation of protein kinase C signal transduction and apoptosis-related pathways. Methods. We conducted a phase I study of high-dose oral tamoxifen in combination with intravenous cisplatin, with two objectives: 1) to determine tolerability, and 2) to determine the daily tamoxifen dose required to achieve serum levels equivalent to in vitro concentrations reported to enhance cisplatin cytotoxicity in preclinical models. Tamoxifen was administered days one through seven at escalating daily doses of 160mg/m2 (n = 5), 200mg/m2 (n = 6), and 250 mg/m2 (n = 4) by ...
The Ca2+-insensitive protein kinase C (PKC) isoforms ε, η, δ and ζ are possible direct downstream targets of phosphatidylinositol 3-kinase (PI3-K), and might therefore be involved in insulin signalling. Although isoform-specific changes in PKC expression have been reported for skeletal muscle and liver in insulin-resistant states, little is known about these isoforms in adipocytes. Therefore we studied (1) expression and subcellular localization of these isoforms in murine adipocytes, (2) translocation of specific isoforms to membranes in response to treatment with insulin and phorbol 12-myristate 13-acetate (PMA) and (3) regulation of expression in insulin-resistant states. The PKC isoforms ε, η, δ and ζ are expressed in adipocytes. Immunoreactivity for all isoforms is higher in the membranes than in the cytosol, but subcellular fractionation by differential centrifugation shows an isoform-specific distribution within the membrane fractions. PMA treatment of adipocytes induces ...
Previous studies have shown that activators of protein kinase C (C kinase) produce synaptic potentiation in the hippocampus. For example, the C kinase activator phorbol dibutyrate has been shown to increase transmitter release in the hippocampus. In addition, a role for C kinase in long-term potentiation has been proposed. A common assumption in such studies has been that substrates for C kinase were responsible for producing these forms of synaptic potentiation. However, we have recently shown that phorbol dibutyrate increased the phosphorylated of synapsin II (formerly protein III, Browning et al., 1987) in chromaffin cells (Haycock et al., 1988). Synapsin II is a synaptic vesicle-associated phosphoprotein that is a very poor substrate for C kinase but an excellent substrate for cAMP-dependent and Ca2+/calmodulin-dependent protein kinase. We felt, therefore, that activation of C kinase might lead to activation of a kinase cascade. Thus effects of C kinase activation might be produced via the
TY - JOUR. T1 - The min K channel underlies the cardiac potassium current I(Ks) and mediates species-specific responses to protein kinase C. AU - Varnum, M. D.. AU - Busch, A. E.. AU - Bond, C. T.. AU - Maylie, J.. AU - Adelman, J. P.. PY - 1993. Y1 - 1993. N2 - A clone encoding the guinea pig (gp) min K potassium channel was isolated and expressed in Xenopus oocytes. The currents, gpI(sK), exhibit many of the electrophysiological and pharmacological properties characteristic of gpI(Ks), the slow component of the delayed rectifier potassium conductance in guinea pig cardiac myocytes. Depolarizing commands evoke outward potassium currents that activate slowly, with time constants on the order of seconds. The currents are blocked by the class III antiarrhythmic compound clofilium but not by the sotalol derivative E4031 or low concentrations of lanthanum. Like I(Ks) in guinea pig myocytes, gpI(sK) is modulated by stimulation of protein kinase A and protein kinase C (PKC). In contrast to rat and ...
TY - JOUR. T1 - Phosphorylation of MYPT1 by protein kinase C attenuates interaction with PP1 catalytic subunit and the 20 kDa light chain of myosin. AU - Tóth, Attila. AU - Kiss, Enikö. AU - Gergely, P.. AU - Walsh, Michael P.. AU - Hartshorne, David J.. AU - Erdődi, F.. PY - 2000/11/3. Y1 - 2000/11/3. N2 - The effect of phosphorylation in the N-terminal region of myosin phosphatase target subunit 1 (MYPT1) on the interactions with protein phosphatase 1 catalytic subunit (PP1c) and with phosphorylated 20 kDa myosin light chain (P-MLC20) was studied. Protein kinase C (PKC) phosphorylated threonine-34 (1 mol/mol), the residue preceding the consensus PP1c-binding motif (35KVKF38) in MYPT11-38, but this did not affect binding of the peptide to PP1c. PKC incorporated 2 mol P(i) into MYPT11-296 suggesting a second site of phosphorylation within the ankyrin repeats (residues 40-296). This phosphorylation diminished the stimulatory effect of MYPT11-296 on the P-MLC20 phosphatase activity of PP1c. ...
This study demonstrates that different PKC isoforms are differentially expressed in particular cellular components of ovarian follicles of pre-pubertal, pubertal and adult mouse ovaries.. Data obtained from H-Score evaluation of immunohistochemistry findings revealed that PKCα expression was more apparent in oocytes of all follicles in pre-pubertal, pubertal and adult ovaries, though it was also expressed in granulosa cells. Interestingly, in adult and pre-pubertal ovaries, intense immunostaining of PKCα in oocytes was statistically significant in primordial (PND60, PND7 and PND1), primary (PND60, PND7 and PND1) and secondary follicles (PND60 and PND7), whereas in PND21 ovaries only oocytes of primordial follicles had significantly higher immunostaining level of PKCα. These findings support the idea that PKCα expression in oocytes of larger follicles may have low significance due to granulosa-oocyte interactions during initiation of hormone dependent follicular growth [27],[28]. PKCα ...
We isolated a group of genes that are rapidly and transiently induced in 3T3 cells by tetradecanoyl phorbol acetate (TPA). These genes are called TIS genes (for TPA-inducible sequences). Epidermal growth factor (EGF), fibroblast growth factor (FGF), and TPA activated TIS gene expression with similar induction kinetics. TPA pretreatment to deplete protein kinase C activity did not abolish the subsequent induction of TIS gene expression by epidermal growth factor or fibroblast growth factor; both peptide mitogens can activate TIS genes through a protein kinase C-independent pathway(s). We also analyzed TIS gene expression in three TPA-nonproliferative variants (3T3-TNR2, 3T3-TNR9, and A31T6E12A). The results indicate that (i) modulation of a TPA-responsive sodium-potassium-chloride transport system is not necessary for TIS gene induction either by TPA or by other mitogens and (ii) TIS gene induction is not sufficient to guarantee a proliferative response to mitogenic stimulation. ...
TY - JOUR. T1 - Monoclonal antibody analysis of phosphatidylserine and protein kinase C localizations in developing rat cerebellum. AU - Miyazawa, Atsuo. AU - Inoue, Hiroko. AU - Yoshioka, Tohru. AU - Horikoshi, Tetsuro. AU - Yanagisawa, Keiji. AU - Umeda, Masato. AU - Inoue, Keizo. PY - 1992/10. Y1 - 1992/10. N2 - Understanding the topographical relationships between phosphatidylserine (PS) and protein kinase C (PKC) within neurons can provide clues about the mechanism of translocation and activation of PKC. For this purpose we applied monoclonal antibodies (Abs) of PS and PKC to sections of developing rat cerebellum. The anti-PKC Ab immunohistochemical pattern showed homogeneous staining of Purkinje cells over various postnatal ages, whereas the anti-PS Ab staining showed a heterogeneous localization over these ages. Purkinje cells did not stain well between postnatal day 14 (PND 14) and PND 21, suggesting that the PS was lost from the membrane during preparation of the sections during this ...
Human UC11 astrocytoma cells were used to investigate the role of protein kinase C (PKC) and other kinases in neurokinin (NK)1 receptor desensitization. The selective NK1 receptor agonist [Sar9,Met(O2)11]-substance P stimulated a biphasic accumulation of [3H]inositol phosphates ([3H]IPs) in the presence of 10 mM LiCl in cells that had been prelabeled with [3H]inositol. An initial rapid phase of [3H]IP accumulation during the first 1 min was followed by a slower sustained phase for up to 90 min. These results demonstrate that the human NK1 receptor desensitizes rapidly but only partially. The selective PKC inhibitor Ro31-8220 did not prevent rapid NK1 receptor desensitization but after a longer incubation significantly potentiated human NK1 receptor agonist-stimulated accumulation of [3H]IPs. These results suggest that, although PKC does not mediate the process of rapid desensitization, it does have an inhibitory role at later times. This conclusion is supported by studies with staurosporine, ...
Dynamic changes of glycolipid domains within the plasma membranes of cultured rat cerebellar granule cells have been investigated. For this purpose, a pyrene-labelled derivative of G(M1) ganglioside has been incorporated in the cell plasma membrane, and the rate of excimer formation, directly related to the formation of domains, has been studied by a fluorescence imaging technique (excimer-formation imaging). Fluorescence imaging showed that upon addition of 100 μM glutamate, indirectly inducing the activation of protein kinase C (PKC), glycolipid concentration within domains increases in cell bodies. Comparable effects were exerted by the addition of PMA, directly inducing the activation of PKC. On the contrary, the phorbol ester was not effective in the presence of the specific PKC inhibitor, bisindolylmaleimide. These results suggest that glycolipid-enriched domains are dynamic supramolecular structures affected by membrane-associated events, such as PKC activation. Dynamic changes of ...
0033] In embodiments in which it is desirous to inhibit Hh pathway signaling, a cell is contacted with an aPKC iota antagonist. By an aPKC iota antagonist, it is meant an agent that reduces, suppresses or inhibits aPKC iota activity. In other words, an aPKC iota antagonist antagonizes the activating effect of aPKC iota on the Hh signaling pathway. In some embodiments, the aPKC iota antagonist is a polypeptide or peptide. For example, the antagonist may be a peptide that competes with natural substrates for access to the active site of aPKC iota, i.e. a pseudosubstrate inhibitor, or PSI. In some instance, the PSI is a PSI that is specific for atypical PKCs, i.e. it is specific for aPKC iota and aPKC zeta. In some instances, it is specific for aPKC iota. In some instances, the PSI is a peptide that consists or consists essentially of the sequence SIYRRGARRWRKLY (SEQ ID NO:4), for example a SIYRRGARRWRKLY peptide that has been myristoylated (to make it cell permeable). By consisting essentially ...
BioAssay record AID 163866 submitted by ChEMBL: Inhibition of [3H]- PDBu binding to peptide D of mouse skin Protein kinase C eta (inactive).
2 Department of Radiation Oncology, University Hospital Zurich, CH-8091 Zurich, Switzerland [S. R., C. G., S. B., M. P.]; Laboratory for Biochemistry, Federal Institute of Technology, 8091 Zurich, Switzerland [S. R., K. W.]; Novartis Pharma Inc., 4002 Basel, Switzerland [D. F.]; and Cold Spring Harbor Laboratory, Cold Spring Harbor, New York 11724 [M. S. S., S. W. L.] Abstract. Caspases are a family of cysteine proteases that constitute the apoptotic cell death machinery. We report the importance of the cytochrome c-mediated caspase-9 death pathway for radiosensitization by the protein kinase C (PKC) inhibitors staurosporine (STP) and PKC-412. In our genetically defined tumor cells, treatment with low doses of STP or the conventional PKC-specific inhibitor PKC-412 in combination with irradiation (5 Gy) potently reduced viability, enhanced mitochondrial cytochrome c release into the cytosol, and specifically stimulated the initiator caspase-9. Whereas treatment with each agent alone had a minimal ...
TY - JOUR. T1 - NF-κB/RelA transactivation is required for atypical protein kinase Cl-mediated cell survival. AU - Lu, Ying. AU - Jamieson, Lee. AU - Brasier, Allan R.. AU - Fields, Alan P.. PY - 2001/8/9. Y1 - 2001/8/9. N2 - In chronic myelogenous leukemia (CML), the oncogene bcr-abl encodes a dysregulated tyrosine kinase that inhibits apoptosis. We showed previously that human erythroleukemia K562 cells are resistant to antineoplastic drug (taxol)-induced apoptosis through the atypical protein kinase C iota isozyme (PKCl), a kinase downstream of Bcr-Abl. The mechanism(s) by which PKCl mediates cell survival to taxol is unknown. Here we demonstrate that PKCl requires the transcription factor nuclear factor-κB (NF-κB) to confer cell survival. At apoptosis-inducing concentrations, taxol weakly induces IκBα proteolysis and NF-κB translocation in K562 cells, but potently induces its transcriptional activity. Inhibition of NF-κB activity (by blocking IκBα degradation) significantly ...
c-Abl and Atm have been implicated in cell responses to DNA damage and oxidative stress. However, the molecular mechanisms by which they regulate oxidative stress response remain unclear. In this report, we show that deficiency of c-Abl and deficiency of ATM differentially altered cell responses to oxidative stress by induction of antioxidant protein peroxiredoxin I (Prx I) via Nrf2 and cell death, both of which required protein kinase C (PKC) δ activation and were mediated by reactive oxygen species. c-abl-/- osteoblasts displayed enhanced Prx I induction, elevated Nrf2 levels, and hypersusceptibility to arsenate, which were reinstated by reconstitution of c-Abl; Atm-/- osteoblasts showed the opposite. These phenotypes correlated with increased PKC δ expression in c-abl-/- osteoblasts and decreased PKC δ expression in Atm-/- cells, respectively. The enhanced responses of c-abl-/- osteoblasts could be mimicked by overexpression of PKC δ in normal cells and impeded by inhibition of PKC δ, and
sn-1,2-Didecanoylglycerol, a synthetic lipid second messenger and model diacylglycerol, was evaluated as a complete skin tumor promoter in CD-1 mice. In addition, sn-1,2-dioctanoylglycerol, sn-1,2-didecanoylglycerol, the second stage tumor promoter mezerein, and the complete tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) were examined for their ability to stimulate epidermal protein kinase C activity in vitro. All four compounds stimulated epidermal protein kinase C activity utilizing lysine-rich histone as the phosphate acceptor substrate. sn-1,2-Dioctanoylglycerol and sn-1,2-didecanoylglycerol stimulated epidermal protein kinase C activity to a maximum velocity similar to that obtained when the enzyme was stimulated with TPA; however, about 1000 times greater concentration of the sn-1,2-diacylglycerols was required. sn-1,2-Didecanoylglycerol was evaluated as a complete skin tumor promoter in CD-1 mice utilizing a dosing regimen demonstrated to produce epidermal hyperplasia. Mice ...
Insulin stimulated protein synthesis in L6 myoblasts but did not increase the labelling of DAG or the release of phosphocholine from phosphatidylcholine. The DAG lipase inhibitor, RHC 80267, more than doubled the amount of label appearing in DAG but did not stimulate protein synthesis. Even in the presence of the DAG lipase inhibitor insulin failed to have any effect on DAG labelling, and conversely RHC 80267 did not modify the insulin-induced increase in protein synthesis. These results suggest that endogenous DAG production is not involved in the stimulation of protein synthesis by insulin. However, exogenous diacylglycerols (1-oleoyl-2-acetyl glycerol and 1-stearoyl-2-arachidonoyl glycerol) both stimulated protein synthesis in L6 myoblasts. The efficacy of the former (arachidonatefree) DAG suggested that their action was by activation of protein kinase C rather than by arachidonate release and prostaglandin formation. Ibuprofen, an inhibitor of cyclo-oxygenase failed to block the effects of ...
TY - JOUR. T1 - PDK1 in apical signaling endosomes participates in the rescue of the polarity complex atypical PKC by intermediate filaments in intestinal epithelia. AU - Mashukova, Anastasia. AU - Forteza, Radia. AU - Wald, Flavia A.. AU - Salas, Pedro J. PY - 2012/5/1. Y1 - 2012/5/1. N2 - Phosphorylation of the activation domain of protein kinase C (PKC) isoforms is essential to start a conformational change that results in an active catalytic domain. This activation is necessary not only for newly synthesized molecules, but also for kinase molecules that become dephosphorylated and need to be refolded and rephosphorylated. This rescuemechanism is responsible for the maintenance of the steady-state levels of atypical PKC (aPKC [PKCι/λ and ζ]) and is blocked in inflammation. Although there is consensus that phosphoinositide-dependent protein kinase 1 (PDK1) is the activating kinase for newly synthesized molecules, it is unclear what kinase performs that function during the rescue and where ...
1. The involvement of phospholipase D (PLD) in the 5-hydroxytryptamine 5-HT1B/5-HT1D-signalling pathway was assessed in the rabbit isolated mesenteric artery. 2. RT-PCR analysis of mesenteric smooth muscle cells revealed a strong signal corresponding to mRNA transcript for the 5-HT1B receptor. The PCR fragment corresponded to the known sequence for the 5-HT1B receptor. No signal corresponding to 5-HT1D mRNA was detected. 3. Neither 5-HT (3 microM) nor KCl (45 mM) individually stimulated any significant increase in the smooth muscle concentration of [33P]-PtdBut to reflect PLD activity. However, in the presence of KCl (45 mM), 5-HT evoked a concentration-dependent increase in [33P]-PtdBut, to a maximum of 84% with 5-HT (3 microM). 4. [33P]-PtdBut accumulation evoked by 5-HT in the presence of KCl was abolished in nominally calcium-free Krebs-Henseleit Buffer (KHB) or with the selective protein kinase C inhibitor, Ro-31 8220 (10 microM, 20 min). 5. 5-HT (3 microM) in the presence of KCl (45 mM) failed to
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Objective: An increase in intracellular calcium concentration ([Ca2+]i) leads to augmentation of late sodium current (late INa) by activating Ca2+-calmodulin-dependent protein kinase II (CaMK-II). The objective of this study was to confirm our hypothesis that both CaMK-II and protein kinase C (PKC) are the signaling molecules whose activation result in increased late INa in the presence of an increased [Ca2+]i.. Methods: Whole-cell and open-cell patch clamp techniques were used to record late INa in rabbit ventricular myocytes dialyzed with pipette solutions containing various concentrations (0.1, 0.3 and 0.6 μM) of [Ca2+]i in the absence and presence of CaMK-II (KN-93), PKC (bisindolylmaleimide, Bim) and MAPK (U0126) inhibitors in the bath solution.. Results: Increases in [Ca2+]i from 0.1 to 0.6 μM resulted in an augmentation of late INa from 0.30 ± 0.03 to 0.45 ± 0.03 pA/pF (n=8-10, p,0.01) in a concentration dependent manner, which was associated with an increase in mean Na+ channel open ...
Pro-apoptotic protein kinase C delta is associated with intranuclear inclusions in a transgenic model of Huntingtons disease.: In order to investigate any effe
In this paper, we have shown that specific isoforms of PKC are pivotal intracellular mediators of signals that regulate the production of rod photoreceptors in the postnatal mouse retina. The complete lack of rods detected in the presence of PKC inhibitors suggests that this enzyme may play this key role for the wide variety of other signals that can elicit rod production.. To provide access to factors that might modulate rod photoreceptor formation, we made use of a well-characterized explant culture system that we developed and have used in many studies of retinal development (Sparrow et al., 1990; Zhao et al., 1995; Zhang et al. 2002, 2004, 2005). These cultures maintain excellent cell viability, tissue lamination, and cell differentiation. In a microarray analysis of gene expression in vivo and in explant cultures, we did, however, find that expression of some genes is delayed by 1-2 d (Liu et al., 2008). This is apparent in the low levels of opsin expression in 4 d explant cultures from P1 ...
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine: A specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.
TY - JOUR. T1 - Rottlerin inhibits tonicity-dependent expression and action of TonEBP in a PKCδ-independent fashion. AU - Zhao, Hongyu. AU - Tian, Wei. AU - Cohen, David M.. PY - 2002. Y1 - 2002. N2 - Novel protein kinase C (PKC) isoforms PKCδ and PKCε have recently been implicated in signaling by hypertonic stress. We investigated the role of the putative PKCδ inhibitor rottlerin on tonicity-dependent gene regulation. In the renal medullary mIMCD3 cell line, rottlerin blocked tonicity-dependent transcription of a tonicity enhancer (TonE)-driven luciferase reporter gene, as well as tonicity-dependent transcription of the physiological tonicity effector gene aldose reductase, but not urea-dependent transcription. Consistent with these data, rottlerin inhibited tonicity-dependent expression of TonE binding protein (TonEBP) at the mRNA and protein levels. Another inhibitor of both novel and conventional PKC isoforms, GF-109203X, suppressed TonEBP-dependent transcription but failed to influence ...
Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by the second messenger diacylglycerol. PKC family members phosphorylate a wide variety of protein targets and are known to be involved in diverse cellular signaling pathways. PKC family members also serve as major receptors for phorbol esters, a class of tumor promoters. Each member of the PKC family has a specific expression profile and is believed to play a distinct role. The protein encoded by this gene is one of the PKC family members. It is a calcium-independent and phospholipid-dependent protein kinase. This kinase is important for T-cell activation. It is required for the activation of the transcription factors NF-kappaB and AP-1, and may link the T cell receptor (TCR) signaling complex to the activation of the transcription factors.[6]. ...
Protein kinase Cepsilon (PKCε) exerts a well-known cardio-protective activity in ischemia-reperfusion injury and plays a pivotal role in stem cell proliferation and differentiation. Although many studies have been performed on physiological and morphological effects of PKCε mis-expression in cardiomyocytes, molecular information on the role of PKCε on early cardiac gene expression are still lacking. We addressed the molecular role of PKCε in cardiac cells using mouse cardiomyocytes and rat bone marrow mesenchymal stem cells. We show that PKCε is modulated in cardiac differentiation producing an opposite regulation of the cardiac genes NK2 transcription factor related, locus 5 (nkx2.5) and GATA binding protein 4 (gata4) both in vivo and in vitro. Phospho-extracellular regulated mitogen-activated protein kinase 1/2 (p-ERK1/2) levels increase in PKCε over-expressing cells, while pkcε siRNAs produce a decrease in p-ERK1/2. Indeed, pharmacological inhibition of ERK1/2 rescues the expression ...
Protein kinase C activation[edit]. PIP2 cleavage to IP3 and DAG initiates intracellular calcium release and PKC activation. ... "Protein Kinase C as the Receptor for the Phorbol Ester Tumor Promoters: Sixth Rhoads Memorial Award Lecture". Cancer Research. ... whereas DAG is a physiological activator of protein kinase C (PKC). The production of DAG in the membrane facilitates ... Diacylglycerol can be phosphorylated to phosphatidic acid by diacylglycerol kinase. Insulin resistance[edit]. Activation of PKC ...
The active site is a region on an enzyme which a particular protein or substrate can bind to. The active site will only allow ... "Functional Design of Proteins". Molecular Cell Biology. 4th edition. W. H. Freeman. ...
COX-2 up-regulation has also been linked to the phosphorylation and activation of the E3 ubiquitin ligase HDM2, a protein that ...
Protein kinase *Tyrosine kinase *Janus kinase. Hydrolase (EC 3). *3.1 Phosphodiesterase. *Acetylcholinesterase ...
1.7% in typical proteins) and is sensitive to oxidation. RI is also rich in leucine (21.5%, compared to 9% in typical proteins ... The affinity of RI for ribonucleases is among the highest for any protein-protein interaction; the dissociation constant of the ... It is a major cellular protein, comprising ~0.1% of all cellular protein by weight, and appears to play an important role in ... Ribonuclease inhibitor (RI) is a large (~450 residues, ~49 kDa), acidic (pI ~4.7), leucine-rich repeat protein that forms ...
Click on genes, proteins and metabolites below to link to respective articles. [§ 1] ... Monitoring liver enzymes and creatine kinase is especially prudent in those on high-dose statins or in those on statin/fibrate ... Decreasing of specific protein prenylation[edit]. Statins, by inhibiting the HMG CoA reductase pathway, simultaneously inhibit ... The sterol response elements then facilitate increased transcription of various other proteins, most notably, LDL receptor. The ...
Protein kinase *Tyrosine-kinase *Janus kinase. Hydrolase (EC 3). *3.1 Phosphodiesterase. *Acetylcholinesterase ...
Protein kinase *Tyrosine-kinase *Janus kinase. Hydrolase (EC 3). *3.1 Phosphodiesterase. *Acetylcholinesterase ...
Protein kinases can also be inhibited by competition at the binding sites where the kinases interact with their substrate ... As a consequence, if two protein kinase inhibitors both bind in the active site with similar affinity, but only one has to ... For example, some protein kinase inhibitors have chemical structures that are similar to adenosine triphosphate, one of the ... Bogoyevitch, MA; Barr, RK; Ketterman, AJ (2005). "Peptide inhibitors of protein kinases-discovery, characterisation and use". ...
It competes with proteins to bind to trypsin and therefore renders it unavailable to bind with proteins for the digestion ... 2001). The serpins are an expanding superfamily of structurally similar but functionally diverse proteins. JBC papers in press. ... A trypsin inhibitor (TI) is a protein and a type of serine protease inhibitor (serpin) that reduces the biological activity of ... Trypsinogen is an inactive form of trypsin, its inactive form ensures protein aspects of the body, such as the pancreas and ...
... and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles. ...
Norbury C (1995). "Cdk2 protein kinase (vertebrates)". In Hardie DG, Hanks S (eds.). Protein kinase factsBook. Boston: Academic ... CDK interacting protein/Kinase inhibitory protein) family and the INK4a/ARF (Inhibitor of Kinase 4/Alternative Reading Frame) ... Nigg EA (June 1995). "Cyclin-dependent protein kinases: key regulators of the eukaryotic cell cycle". BioEssays. 17 (6): 471-80 ... Originally, a green fluorescent protein, mAG, was fused to hGem(1/110) and an orange fluorescent protein (mKO2) was fused to ...
kinase activity. • protein binding. • ATP binding. • protein serine/threonine kinase activity. • protein kinase activity. ... Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by the second ... Dephospho-(reductase kinase) kinase (EC *AMP-activated protein kinase α *PRKAA1 ... "Complex formation and cooperation of protein kinase C theta and Akt1/protein kinase B alpha in the NF-kappa B transactivation ...
... protein tyrosine kinases and protein serine/threonine kinases. Dual-specificity kinases are subclass of the tyrosine kinases. ... PIKKs have four domains at the protein level, which distinguish them from other protein kinases. From the N-terminus to the C- ... mTOR is a kinase within the family of phosphatidylinositol-3 kinase-related kinases (PIKKs), which is a family of serine/ ... threonine protein kinases, with a sequence similarity to the family of lipid kinases, PI3Ks. These kinases have different ...
Tyrosine-protein kinase 6-also known as BRK (breast tumor kinase)-is a cytoplasmic non-receptor protein kinase which may ... "PTK6 protein tyrosine kinase 6". National Center for Biotechnology Information (NCBI). 4 June 2020. Mitchell, P J; Sara E A; ... Tyrosine-protein kinase 6 is an enzyme that in humans is encoded by the PTK6 gene. ... Lee ST, Strunk KM, Spritz RA (December 1993). "A survey of protein tyrosine kinase mRNAs expressed in normal human melanocytes ...
... belongs to the serine/threonine-specific protein kinase family and therefore has the protein kinase domain in positions ... Serine/threonine-protein kinase RIO1 is an enzyme that in humans is encode by the RIOK1 gene. RIOK1 is an atypical protein, ... The protein Kinase RIO1 highest expression is in testicles, in addition the RNA that encodes this protein has low tissue ... 6:7,389,496-7,418,037) Effects on modified protein - protein degradation, triggered by K411-m1; protein stabilization, ...
... in tyrosine-protein kinase receptors; and in the programmed cell death protein 1 (PD1). Immunoglobulin V-set, subgroup InterPro ... V-set domains are found in diverse protein families, including immunoglobulin light and heavy chains; in several T-cell ...
DAG activates a family of serine/threonine protein kinases, collectively known as protein kinase C (PKC). Phorbol esters can ... Phorbol esters can directly stimulate protein kinase C, PKC. The N-terminal region of PKC, known as C1, has been shown Phorbol ... Kikkawa U, Nishizuka Y, Igarashi K, Fujii T, Ono Y, Kuno T, Tanaka C (1989). "Phorbol ester binding to protein kinase C ... "The protein kinase C family". Eur. J. Biochem. 208 (3): 547-557. doi:10.1111/j.1432-1033.1992.tb17219.x. PMID 1396661. ...
Mitogen-activated protein kinase 4 is a member of the mitogen-activated protein kinase family. Tyrosine kinase growth factor ... Mitogen-activated protein kinase 4 is an enzyme that in humans is encoded by the MAPK4 gene. ... Li L, Wysk M, Gonzalez FA, Davis RJ (February 1994). "Genomic loci of human mitogen-activated protein kinases". Oncogene. 9 (2 ... "Entrez Gene: MAPK4 mitogen-activated protein kinase 4". Petersen M, Brodersen P, Naested H, Andreasson E, Lindhart U, Johansen ...
Allende JE, Allende CC (1995). "Protein kinases. 4. Protein kinase CK2: an enzyme with multiple substrates and a puzzling ... "Characterization of protein interaction among subunits of protein kinase CKII in vivo and in vitro". Mol. Cells. 8 (1): 43-8. ... a novel pleckstrin homology domain-containing protein that interacts with protein kinase CK2". J. Biol. Chem. 275 (19): 14295- ... Faust M, Montenarh M (2001). "Subcellular localization of protein kinase CK2. A key to its function?". Cell Tissue Res. 301 (3 ...
protein kinase activity. • kinase activity. • protein binding. • protein tyrosine kinase activity. • ATP binding. • protein ... Dual specificity mitogen-activated protein kinase kinase 6 also known as MAP kinase kinase 6 (MAPKK 6) or MAPK/ERK kinase 6 is ... "Human mitogen-activated protein kinase kinase kinase mediates the stress-induced activation of mitogen-activated protein kinase ... protein serine/threonine kinase activity. • identical protein binding. • MAP kinase kinase activity. ...
protein tyrosine kinase activity. • nucleotide binding. • MAP kinase kinase activity. • protein kinase activity. • protein ... protein serine/threonine kinase activator activity. • protein binding. • protein serine/threonine/tyrosine kinase activity. • ... This protein kinase lies upstream of MAP kinases and stimulates the enzymatic activity of MAP kinases upon activation by a wide ... Dephospho-(reductase kinase) kinase (EC *AMP-activated protein kinase α *PRKAA1 ...
protein kinase activity. • kinase activity. • protein binding. • protein tyrosine kinase activity. • ATP binding. • Ras guanyl- ... membrane protein proteolysis. • phosphorylation. • transmembrane receptor protein tyrosine kinase signaling pathway. • positive ... transmembrane receptor protein tyrosine kinase activity. • receptor tyrosine kinase. • transmembrane signaling receptor ... "The Ret receptor protein tyrosine kinase associates with the SH2-containing adapter protein Grb10". J. Biol. Chem. 270 (37): ...
protein kinase activity. • kinase activity. • protein binding. • transmembrane receptor protein tyrosine kinase activity. • ... protein tyrosine kinase collagen receptor activity. • protein tyrosine kinase activity. • ATP binding. • collagen binding. ... transmembrane receptor protein tyrosine kinase signaling pathway. • regulation of bone mineralization. • positive regulation of ... protein phosphorylation. • cell adhesion. • positive regulation of osteoblast differentiation. • chondrocyte proliferation. • ...
The product of this gene belongs to the serine/threonine protein kinase family and to the Ca2+/calmodulin-dependent protein ... "Entrez Gene: CAMK2B calcium/calmodulin-dependent protein kinase (CaM kinase) II beta". Walikonis RS, Oguni A, Khorosheva EM, ... "KN-93 inhibition of G protein signaling is independent of the ability of Ca2+/calmodulin-dependent protein kinase II to ... Calcium/calmodulin-dependent protein kinase type II beta chain is an enzyme that in humans is encoded by the CAMK2B gene. ...
It shows protein kinase C inhibitor activity. Foeniculoside I is a glucoside of cis-miyabenol C. Mattivi, F.; Vrhovsek, U.; ... "Naturally Occurring Protein Kinase C Inhibitors; II. Isolation of Oligomeric Stilbenes from Caragana sinica". Planta Medica. 61 ...
Non-receptor tyrosine-protein kinase TYK2. Protein-tyrosine phosphatases PTPN3 and PTPN4, enzymes that appear to act at ... Focal-adhesion kinases (FAKs), cytoplasmic protein tyrosine kinases involved in signalling through integrins. Janus tyrosine ... Ezrin, moesin, and radixin are highly related proteins (ERM protein family), but the other proteins in which the FERM domain is ... In molecular biology, the FERM domain (F for 4.1 protein, E for ezrin, R for radixin and M for moesin) is a widespread protein ...
The protein possesses tyrosine kinase activity. The primary single chain precursor protein is post-translationally cleaved to ... c-Met, also called tyrosine-protein kinase Met or hepatocyte growth factor receptor (HGFR), is a protein that in humans is ... Furge KA, Zhang YW, Vande Woude GF (November 2000). "Met receptor tyrosine kinase: enhanced signaling through adapter proteins ... The limitations of kinase inhibitors include the facts that they only inhibit kinase-dependent MET activation, and that none of ...
Protein kinase LYK5, also known as LYK5 or STRADα, is a human protein and also denotes the gene encoding it. Endogenous LKB1 ... "Entrez Gene: LYK5 protein kinase LYK5". Baas AF, Boudeau J, Sapkota GP, Smit L, Medema R, Morrice NA, Alessi DR, Clevers HC ( ... "LKB1 is a master kinase that activates 13 kinases of the AMPK subfamily, including MARK/PAR-1". EMBO J. 23 (4): 833-43. doi: ... STRADα stabilizes LKB1 protein both in vivo and in vitro, and is capable of eliciting multiple axons in mouse embryonic ...
Protein KaiA enhances the phosphorylation of protein KaiC by binding to the A loop of the CII domain to promote auto-kinase ... KaiC encodes for the KaiC protein which interacts with the KaiA and KaiB proteins in a post-translational oscillator (PTO). The ... Variations in the C-terminal region of each of their proteins suggest functional divergence between the Kai clock proteins, ... lysed S. elongatus and isolated KaiABC proteins. In test tubes containing only KaiABC proteins and ATP, in vitro ...
1985). "Amino terminal myristylation of the protein kinase p60src, a retroviral transforming protein". Science. 227 (4685): 427 ... 1990). "Myristoylation of gag proteins of HIV-1 plays an important role in virus assembly". AIDS Res. Hum. Retroviruses. 6 (6 ... Tashiro A, Shoji S, Kubota Y (1990). "Antimyristoylation of the gag proteins in the human immunodeficiency virus-infected cells ... Zhou W, Resh MD (1997). "Differential membrane binding of the human immunodeficiency virus type 1 matrix protein". J. Virol. 70 ...
ER Translocon complex.[2] Many protein complexes are involved in protein synthesis. The actual production takes place in the ... Sec61 is the protein-conducting channel and the OST adds sugar moieties to the nascent protein. ... Oligosaccharyltransferase or OST (EC is a membrane protein complex that transfers a 14-sugar oligosaccharide from ... Yeast OST is composed of eight different membrane-spanning proteins in three subcomplexes (one of them is OST4).[7][8] These ...
Kumar S, Sieghart W, Morrow AL (2002). "Association of protein kinase C with GABA(A) receptors containing alpha1 and alpha4 ... This membrane protein-related article is a stub. You can help Wikipedia by expanding it.. *v ... Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.[5][6] ... GABRA4+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) ...
A protein kinase drifting around on the outer chloroplast membrane can use ATP to add a phosphate group to the Toc34 protein, ... It can be regulated through phosphorylation, but by a different protein kinase than the one that phosphorylates Toc34.[41] Its ... Protein targeting and importEdit. See also: Protein targeting. The movement of so many chloroplast genes to the nucleus means ... Protein synthesisEdit. See also: Transcription and translation. Protein synthesis within chloroplasts relies on an RNA ...
The CD20 proteins are sticking out of the cell membrane, and rituximab, the Y-shaped antibody, is binding to the CD20 proteins. ... Tyrosine-kinase inhibitors ("-nib"). Receptor tyrosine kinase. *ErbB: HER1/EGFR (Brigatinib. *Erlotinib ... The antibody binds to the cell surface protein CD20. CD20 is widely expressed on B cells, from early pre-B cells to later in ... In contrast, when the B cell lacked this asymmetric protein cluster, it was killed only 40% of the time.[36][37] ...
negative regulation of protein kinase activity. • cytokine-mediated signaling pathway. • negative regulation of JAK-STAT ... protein kinase inhibitor activity. • collagen binding. • extracellular matrix structural constituent conferring compression ... a newly discovered member of the leucine-rich repeat protein family". The Journal of Biological Chemistry. 276 (15): 12212-21. ... a novel member of the leucine-rich repeat protein family closely related to decorin and biglycan". The Journal of Biological ...
"The neuropeptide substance P activates p38 mitogen-activated protein kinase resulting in IL-6 expression independently from NF- ... "Metalloproteinases and transforming growth factor-alpha mediate substance P-induced mitogen-activated protein kinase activation ... "Substance P induces rapid and transient membrane blebbing in U373MG cells in a p21-activated kinase-dependent manner". PLOS ... "Inhibitor of apoptosis proteins (IAPs) and their antagonists regulate spontaneous and tumor necrosis factor (TNF)-induced ...
Like lapatinib and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth ... Binding proteins: IGFBP (1, 2, 3, 4, 5, 6, 7). *Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1) ... Phase II results for breast cancer that over-expresses the protein human epidermal growth factor receptor 2 (Her2-positive ... Afatinib is not only active against EGFR mutations targeted by first generation tyrosine-kinase inhibitors (TKIs) like ...
Mijelin protein nula • Osteonektin • Protein C • Protein S • Proteoglikan • Serum amiloid P komponenta • Sialoglikoprotein ( ... and c-Jun NH2-terminal kinase.". J. Biol. Chem. 274 (23): 15978-81. PMID 10347144. doi:10.1074/jbc.274.23.15978. CS1 održavanje ... Faktor aktivacije B-ćelija, (BAFF) koji je takođe poznat kao faktor nekroze tumora ligand superfamilija član 13B, je protein ... On je izražen kao transmembranski protein na različitim ćelijskim tipovima, kao što su monociti, dendritske ćelije i ćelije ...
Vallenius T، Mäkelä TP (2003). "Clik1: a novel kinase targeted to actin stress fibers by the CLP-36 PDZ-LIM protein.". J. Cell ... "Towards a proteome-scale map of the human protein-protein interaction network.". Nature. 437 (7062): 1173-8. PMID 16189514. doi ... Wang H، Harrison-Shostak DC، Lemasters JJ، Herman B (1996). "Cloning of a rat cDNA encoding a novel LIM domain protein with ... Vallenius T، Luukko K، Mäkelä TP (2000). "CLP-36 PDZ-LIM protein associates with nonmuscle alpha-actinin-1 and alpha-actinin-4 ...
... quercetin is a non-specific protein kinase enzyme inhibitor.[17][20] Quercetin has also been reported to have estrogenic ( ... Quercetin also activates or inhibits the activities of a number of proteins.[22] For example, ... quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER).[26][27] ... "The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells ...
... mitogen-activated protein kinase) cascade that is itself a kinase. RSK2 phosphorylates cellular proteins (including histone H3 ... Mutations in the RPS6KA3 gene can result in expression of an RSK2 protein (ribosomal S6 kinase 2) with reduced or absent kinase ... The protein RSK2 which is encoded by the RPS6KA3 gene is a kinase which phosphorylates some substrates like CREB and histone H3 ... Mutations in the RPS6KA3 disturb the function of the protein, but it is unclear how a lack of this protein causes the signs and ...
protein binding. • enzyme binding. • receptor binding. • lipid binding. • RNA polymerase II transcription factor activity, ... In vitro phosphorylation by casein kinase II". The Journal of Biological Chemistry. 269 (49): 31034-40. PMID 7983041.. ... The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found ... identical protein binding. • RNA polymerase II transcription factor activity, sequence-specific DNA binding. • transcriptional ...
The encoded protein is a type 1A regulatory subunit of protein kinase A. Inactivating germline mutations of this gene are found ... transition in the second codon position of the 74th codon in the protein) mutation in the PRKAR1A gene confirming the diagnosis ...
Fig 2. Schematic diagram of a GABAA receptor protein ((α1)2(β2)2(γ2)) which illustrates the five combined subunits that form ... Bcr-Abl tyrosine-kinase inhibitors. *Cannabinoid receptor antagonists. *CCR5 receptor antagonists. *Neurokinin 1 receptor ... The synaptic anchoring protein Gephyrin is indirectly linked to the GABAA receptors. ... molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. ...
... binding to cAMP-dependent protein kinase (PKA).[111] Moclobemide is chemically unrelated to irreversible MAOI antidepressants ... The elimination half-life is around 2 hours.[8][118] It is moderately bound to plasma proteins, especially albumin.[8] However ...
Adducin binds with high affinity to Ca(2+)/calmodulin and is a substrate for protein kinases A and C. Alternative splicing ... Matsuoka Y, Li X, Bennett V (1998). "Adducin is an in vivo substrate for protein kinase C: phosphorylation in the MARCKS- ... Definition of the calmodulin-binding domain and sites of phosphorylation by protein kinases A and C". J. Biol. Chem. 271 (41): ... Alpha-adducin is a protein that in humans is encoded by the ADD1 gene. Adducins are a family of cytoskeleton proteins encoded ...
positive regulation of protein kinase activity. • T cell activation involved in immune response. • cellular protein metabolic ... protein processing. • protein maturation. • myeloid dendritic cell differentiation. • autophagy. • protein glycosylation. • ... negative regulation of protein kinase activity. • cell fate specification. • skeletal system morphogenesis. • regulation of ... positive regulation of protein phosphorylation. • positive regulation of MAP kinase activity. • positive regulation of ...
protein C-terminus binding. • protein binding. • four-way junction DNA binding. • identical protein binding. • ... Lin HR, Ting NS, Qin J, Lee WH (Sep 2003). "M phase-specific phosphorylation of BRCA2 by Polo-like kinase 1 correlates with the ... This protein can interact with the ssDNA-binding protein RPA, BRCA2, PALB2[10] and RAD52. ... Protein domains in homologous recombination-related proteins are conserved across the three main groups of life: archaea, ...
"Human tyrosine kinase 2 deficiency reveals its requisite roles in multiple cytokine signals involved in innate and acquired ... Genetic disorder, protein biosynthesis: Transcription factor/coregulator deficiencies. (1) Basic domains. 1.2. *Feingold ...
1992). "The lymphocyte-specific tyrosine protein kinase p56lck is endocytosed in Jurkat cells stimulated via CD2.". J. Immunol. ... to the transmembrane protein GP41 of HIV-1 inhibits distinct lymphocyte activation pathways dependent on protein kinase C and ... Wilkins A, Yang W, Yang J (2003). "Structural biology of the cell adhesion protein CD2: from molecular recognition to protein ... 1990). "Immunoregulatory effect of a synthetic peptide corresponding to a region of protein p24 of HIV.". Folia Biol. (Praha) ...
Perets T, Blumenstein Y, Shistik E, Lotan I, Dascal N (Apr 1996). "A potential site of functional modulation by protein kinase ... Calcium channel, voltage-dependent, L type, alpha 1C subunit (also known as Cav1.2) is a protein that in humans is encoded by ... Click on genes, proteins and metabolites below to link to respective Wikipedia articles. [§ 1] ... protein binding. • alpha-actinin binding. • voltage-gated calcium channel activity. • voltage-gated calcium channel activity ...
TANGO6: encoding protein Transport and Golgi organization protein 6 homolog. *TAO2: encoding Serine/threonine-protein kinase ... UNKL: encoding protein RING finger protein unkempt-like. *VAT1L: encoding protein Vesicle amine transport protein 1 homolog (T ... LINC00273 encoding protein Long intergenic non-protein coding RNA 273. *LOC124220: encoding protein Zymogen granule protein 16 ... SHCBP1: encoding protein SHC SH2 domain-binding protein 1. *SLZ1: encoding protein SLX1 structure-specific endonuclease subunit ...
"The Drosophila Clock Gene double-time Encodes a Protein Closely Related to Human Casein Kinase Iε" (PDF). Cell. 94 (1): 97-107 ... In 1998, Jeff Price from the Young lab discovered a kinase called doubletime(Casein kinase 1) that phosphorylates PER on ... Young's lab is also attributed with the discovery of the timeless and doubletime genes, which makes proteins that are also ... Period and Timeless proteins bind together to form a stabilized dimer, which allows the two to enter the nucleus. ...
... who believed that transcription was activated by protein-DNA and protein-protein interactions on largely naked DNA templates, ... The mitotic kinase aurora B phosphorylates histone H3 at serine 10, triggering a cascade of changes that mediate mitotic ... Nuclear protein Ataxia-Telangiectasia (NPAT), also known as nuclear protein coactivator of histone transcription, is a ... The first step of chromatin structure duplication is the synthesis of histone proteins: H1, H2A, H2B, H3, H4. These proteins ...
This bacterial protein complex is a machine for folding other proteins, which get trapped within the shell. Fatty acid synthase ... Arias-Palomo E, Recuero-Checa MA, Bustelo XR, Llorca O (December 2007). "3D structure of Syk kinase determined by single- ... Proteins in vitreous ice usually adopt a random distribution of orientations (or viewing angles), allowing a fairly isotropic ... Important information on protein synthesis, ligand binding and RNA interaction can be obtained using this novel technique at ...
Kelly CJ, Stenton SR, Lashen H. Insulin-like growth factor binding protein-1 in PCOS: a systematic review and meta-analysis. ... of 17α-Hydroxylase Activity Is Mediated by Phosphatidyl Inositol 3-Kinase But Not Extracellular Signal-Regulated Kinase-1/2 in ...
Cyclin-T2 is a protein that in humans is encoded by the CCNT2 gene. The protein encoded by this gene belongs to the highly ... This cyclin and its kinase partner CDK9 were found to be subunits of the transcription elongation factor p-TEFb. The p-TEFb ... Kwak YT, Ivanov D, Guo J, Nee E, Gaynor RB (1999). "Role of the human and murine cyclin T proteins in regulating HIV-1 tat- ... Jang MK, Mochizuki K, Zhou M, Jeong HS, Brady JN, Ozato K (2005). "The bromodomain protein Brd4 is a positive regulatory ...
... and two kinases of the JNK MAP kinase pathway (MLK2 and MKK7). He then determined that CNK1 acts together with these four ... It was already known that other Ga proteins could induce Rho activation (i.e. Ga13 activates p115 Rho GEF, which in turn ... In 1993, Alan Hall was awarded the Feldberg Foundation Prize for his work on the role GTP-binding proteins played on signal ... In 1986, Hall helped uncover properties of the human p21 protein, which is encoded by N-ras. GTPase activity of different ...
MAP kinase kinase kinase (MAP3K or MKKK). *MAP kinase kinase kinases *MAP3K1 ... A mitogen-activated protein kinase (MAPK or MAP kinase) is a type of protein kinase that is specific to the amino acids serine ... Dephospho-(reductase kinase) kinase (EC *AMP-activated protein kinase α *PRKAA1 ... is performed by members of the Ste7 protein kinase family, also known as MAP2 kinases. MAP2 kinases in turn, are also activated ...
... protein kinases are implicated in a broad variety of diseases, including cancers and neurodegenerative conditions, and offer ... Assays for Mitogen-Activated Protein Kinase (MARK) Subtypes and MARK Activating Protein Kinase-2 (MAPKAP K-2) Using a Common ... Analysis of Protein Kinase Subcellular Localization by Visualization of GFP Fusion Proteins ... In Protein Kinase Protocols, a panel of highly skilled laboratory investigators describe both basic and more sophisticated ...
Protein kinase C (PKC). is actually a family of protein kinases consisting of ~10 isozymes. They are divided into three ... Dephospho-(reductase kinase) kinase (EC *AMP-activated protein kinase α *PRKAA1 ... A serine/threonine protein kinase (EC is a kinase enzyme that phosphorylates the OH group of serine or threonine ( ... Protein Kinase B, also known as AKT kinase. The v-akt gene was identified as the oncogene of retrovirus AKT8. The gene codes ...
Norway rat protein-coding gene Mapk1. Represented by 134 ESTs from 65 cDNA libraries. Corresponds to reference sequence NM_ ... Protein sequence * * Protein/EST matches (ProtEST) * * Protein/protein matches (BLink) * mitogen-activated protein kinase 1. C ... Protein sequence * * Protein/EST matches (ProtEST) * * Protein/protein matches (BLink) * mitogen-activated protein kinase 1. X ... Protein sequence * * Protein/EST matches (ProtEST) * * Protein/protein matches (BLink) * mitogen-activated protein kinase 8. C ...
Lambda/iota protein kinase C-interacting protein; Lambda-interacting protein; LIP; Phosphatidylinositol 3-kinase-related kinase ... Phosphatidylinositol 3-kinase-related kinase; Phosphatidylinositol 3-kinase-related protein kinase; PI-3-kinase-related kinase ... 61E3.4; ATX; hSMG-1; KIAA0421; Lambda/iota protein kinase C-interacting protein; Lambda-interacting protein; LIP; ... Heat shock protein 90 regulates phosphatidylinositol 3-kinase-related protein kinase family proteins together with the RUVBL1/2 ...
We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their ... InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites ... Protein kinase C zeta plays a central role in activation of the p42/44 mitogen-activated protein kinase by endotoxin in ... This group represents protein kinase C (KPC), including zeta/iota types from mammals, protein kinase C-like 3 from round worms ...
Mitogen-activated protein kinase pathways.. Robinson MJ1, Cobb MH.. Author information. 1. University of Texas Southwestern ... Nearly all cell surface receptors utilize one or more of the mitogen-activated protein kinase cascades in their repertoire of ... MAP Kinase Kinase Kinase 1*. *Mammals. *Mitogen-Activated Protein Kinase Kinases*. *Protein-Serine-Threonine Kinases/metabolism ...
... and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, ... regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, ... Protein tyrosine kinase inhibitors. US20090298855 *. Jul 28, 2009. Dec 3, 2009. Critical Outcome Technologies Inc.. Protein ... The FLK family is comprised of the kinase insert domain receptor (KDR), fetal liver kinase-1 (FLK-1), fetal liver kinase-4 (FLK ...
AMP-activated protein kinase (AMPK), an energy sensor, can regulate protein and lipid metabolism responding to alterations in ...
... including the tumor suppressor protein p53, the SV40 large T antigen and several transcription factors. ... DNA-Dependent Protein Kinase (DNA-PK) phosphorylates several DNA-binding substrates in vitro, ... cAMP-Dependent Protein Kinase, Catalytic Subunit. Purified kinase for protein phosphorylation and signal transduction studies. ... Kinase-Glo® Luminescent Kinase Assays. Determines activity of purified kinases by quantifying ATP remaining after a kinase ...
mitogen-activated protein kinase;. VLCMR,. very low Ca2+, Mg2+ Ringer;. MKP-1,. MAP kinase phosphatase-1;. ΔP-MKP-1,. ... Mitogen-activated protein kinase and neural specification in Xenopus. Aarti R. Uzgare, J. Akif Uzman, Heithem M. El-Hodiri, Amy ... Mitogen-activated protein kinase and neural specification in Xenopus. Aarti R. Uzgare, J. Akif Uzman, Heithem M. El-Hodiri, Amy ... Mitogen-activated protein kinase and neural specification in Xenopus. Aarti R. Uzgare, J. Akif Uzman, Heithem M. El-Hodiri, and ...
Our data indicate that protein kinase C (PKC) is required for the proper assembly of tight junctions. Low concentrations of the ... We have now examined in detail the role of protein kinases in intercellular junction biogenesis by using a combination of ... Regulated assembly of tight junctions by protein kinase C. R O Stuart and S K Nigam ... Identity of the 330- and 65-kDa phosphoproteins remains to be determined, but the 65-kDa protein may be occludin. The mass of ...
protein kinase C, eta type. A. 157. Homo sapiens. Mutation(s): 0 Gene Names: PRKCH, PKCL, PRKCL. EC: (PDB Primary Data ... Protein kinase C eta (PKCeta) is one of several PKC isoforms found in humans. It is a novel PKC isoform in that it is activated ... Protein kinase C eta (PKCeta) is one of several PKC isoforms found in humans. It is a novel PKC isoform in that it is activated ... Structure of human protein kinase C eta (PKCeta) C2 domain and identification of phosphorylation sites.. Littler, D.R., Walker ...
View protein in PROSITE. PS00107 PROTEIN_KINASE_ATP, 1 hit. PS50011 PROTEIN_KINASE_DOM, 1 hit. PS00109 PROTEIN_KINASE_TYR, 1 ... View protein in PROSITE. PS00107 PROTEIN_KINASE_ATP, 1 hit. PS50011 PROTEIN_KINASE_DOM, 1 hit. PS00109 PROTEIN_KINASE_TYR, 1 ... IPR011009 Kinase-like_dom_sf. IPR000719 Prot_kinase_dom. IPR017441 Protein_kinase_ATP_BS. IPR001245 Ser-Thr/Tyr_kinase_cat_dom ... IPR011009 Kinase-like_dom_sf. IPR000719 Prot_kinase_dom. IPR017441 Protein_kinase_ATP_BS. IPR001245 Ser-Thr/Tyr_kinase_cat_dom ...
View protein in InterPro. IPR011009 Kinase-like_dom_sf. IPR003527 MAP_kinase_CS. IPR000719 Prot_kinase_dom. ... View protein in InterPro. IPR011009 Kinase-like_dom_sf. IPR003527 MAP_kinase_CS. IPR000719 Prot_kinase_dom. ... Kinase, Serine/threonine-protein kinaseSAAS annotation. Automatic assertion according to rulesi ... PROSITE; a protein domain and family database. More...PROSITEi. View protein in PROSITE. PS01351 MAPK, 1 hit. PS50011 PROTEIN_ ...
... is a highly specific substrate for DNA-PK, with the sequence Glu-Pro-Pro-Leu-Ser ... DNA-Dependent Protein Kinase. Purified kinase that phosphorylates several DNA-binding proteins in vitro, including p53. ... DNA-Dependent Protein Kinase. Purified kinase that phosphorylates several DNA-binding proteins in vitro, including p53. ... cAMP-Dependent Protein Kinase, Catalytic Subunit. Purified kinase for protein phosphorylation and signal transduction studies. ...
... is a truncated form of the v-AbI Protein Tyrosine Kinase, a partner in the Gag-Abl fusion protein of the Abelson murine ... 1X NEBuffer™ for Protein Kinases (PK) Incubate at 30°C 1X NEBuffer™ for Protein Kinases (PK) 50 mM Tris-HCl 10 mM MgCl2 0.1 mM ... Abl Protein Tyrosine Kinase (AbI) is a truncated form of the v-AbI Protein Tyrosine Kinase, a partner in the Gag-Abl fusion ... NEBuffer™ for Protein Kinases (PK) -20 10 X Product Categories:. Discontinued Products. * Properties & Usage Unit Definition. ...
Protein Kinase A is directed to specific sub cellular locations after tethering to Protein kinase A anchoring proteins (AKAPs ... out of 540 different protein kinase genes that make up for human kinome, only one other protein kinase, Casein kinase 2, is ... "cAMP-dependent protein kinase" redirects here. It is not to be confused with AMP-activated protein kinase or cyclin-dependent ... Protein kinase A, more precisely known as adenosine 3,5-monophosphate (cyclic AMP)-dependent protein kinase was discovered by ...
MI-1 was synthesized as protein kinases inhibitor [8]. It was tested on 32 protein kinases for determination of inhibitory ... Anti-Inflammatory Effects of Protein Kinase Inhibitor Pyrrol Derivate. Halyna M. Kuznietsova, Maryna S. Yena, Iryna P. Kotlyar ... Protein kinase inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1Н-pyrrol-2,5-dione (MI-1) (Figure 1) has been ... Indeed, protein kinases are strongly involved in pathogenesis of IBD and thereby could be the targets of anti-IBD therapy. For ...
This paper summarizes data from different studies all aimed at elucidating regulation of protein kinase B in the diabetic heart ... Protein kinase B in the diabetic heart Mol Cell Biochem. 2003 Jul;249(1-2):31-8. ... This paper summarizes data from different studies all aimed at elucidating regulation of protein kinase B in the diabetic heart ... In contrast to the above-mentioned results, the protein tyrosine phosphatase inhibitor vanadate, alone or in combination with ...
... is a serine/threonine kinase. It is a Ca 2+ /calmodulin-dependent, truncated monomer (1-325 amino acid residues) of the α ... Calmodulin-Dependent Protein Kinase II (CaMKII) is a serine/threonine kinase. It is a Ca2+/calmodulin-dependent, truncated ... 1X NEBuffer™ for Protein Kinases (PK) 50 mM Tris-HCl 10 mM MgCl2 0.1 mM EDTA 2 mM DTT 0.01% Brij 35 (pH 7.5 @ 25°C) ... 1X NEBuffer™ for Protein Kinases (PK) Supplement with 200 µM ATP, 1.2 µM and 2 µM Incubate at 30°C ...
... nounAny of a group of kinases that phosphorylate the amino acids serine, threonine, and tyrosine in certain proteins, that ... protein kinase. protein kinase. noun. Any of a group of kinases that phosphorylate the amino acids serine, threonine, and ... "protein kinase." YourDictionary, n.d. Web. 16 August 2018. ,,. ... protein kinase. (n.d.). Retrieved August 16th, 2018, from ...
... John C. Watson jcwatso at Tue Dec 30 12:32:19 EST 1997 *Previous message: Postdoctoral ... POSTDOCTORAL POSITION AT IUPUI A postdoctoral position is available to study photoregulated protein kinases from the garden pea ... Expression of the two kinases under investigation is rapidly down-regulated by light. One kinase is closely related to the blue ... Genetic, molecular, and biochemical approaches will be utilized to elucidate the roles of these kinases in the transduction of ...
PKA signaling cascade, protein kinase A signal transduction, protein kinase A signaling cascade, protein kinase A signalling ... A series of reactions, mediated by the intracellular serine/threonine kinase protein kinase A, which occurs as a result of a ... Gene Ontology Term: protein kinase A signaling. GO ID. GO:0010737 Aspect. Biological Process. Description. ...
Nearly all cell surface receptors utilize one or more of the mitogen-activated protein kinase cascades in their repertoire of ... Mitogen-activated protein kinase pathways Curr Opin Cell Biol. 1997 Apr;9(2):180-6. doi: 10.1016/s0955-0674(97)80061-0. ... Nearly all cell surface receptors utilize one or more of the mitogen-activated protein kinase cascades in their repertoire of ... Mitogen-Activated Protein Kinase Kinases* * Protein-Serine-Threonine Kinases / metabolism * Protein-Tyrosine Kinases / ...
By modeling vandetanib and PTK6 complex, researchers at LSU found that the KRAS protein to also contain a similar drug-binding ... Chemotherapeutic vandetanib bound to its main target Protein Tyrosine Kinase 6 (PTK6) in purple, which is involved in many ... Chemotherapeutic vandetanib bound to its main target Protein Tyrosine Kinase 6 (PTK6) in purple, which is involved in many ... Chemotherapeutic Vandetanib Bound to Protein Tyrosine Kinase 6 (image). Louisiana State University ...
Protein kinases and phosphatases, such as MAPKs, JAKs, cyclin-dependent kinase-9, calcium/calmodulin-dependent protein kinases ... Alterations in protein kinase A and protein kinase C levels in heart failure due to genetic cardiomyopathy. Can. J. Cardiol. ... Reciprocal modulation of mitogen-activated protein kinases and mitogen-activated protein kinase phosphatase 1 and 2 in failing ... apoptosis signaling kinase 1 [Ask1], TGF-β-activated kinase 1 [Tak1], MAPK/ERK kinase kinase 1 [MEKK1]). However, when the more ...
Compositions and methods are provided for the treatment, detection and diagnosis of diseases associated with protein kinase C ... New nucleic acid sequences are provided which encode 3 untranslated regions of human protein kinase C alpha polynucleotide ... Methods of treating conditions amenable to therapeutic intervention by modulating protein kinase C expression with an ... Compositions and methods are provided for the treatment and diagnosis of diseases associated with protein kinase C. ...
Protein kinase A (PKA) is typically activated by cAMP. Here, Bachmaier et al. show that PKA of Trypanosoma is activated by ... Protein kinase A (PKA), the main effector of cAMP in eukaryotes, is a paradigm for the mechanisms of ligand-dependent and ... domains or protein-protein interaction domains are linked to the catalytic kinase domains of the 176 identified protein kinases ... Compensatory regulation of RIalpha protein levels in protein kinase A mutant mice. J. Biol. Chem. 272, 3993-3998 (1997). ...
  • Since the consensus sequence residues of a target substrate only make contact with several key amino acids within the catalytic cleft of the kinase (usually through hydrophobic forces and ionic bonds ), a kinase is usually not specific to a single substrate, but instead can phosphorylate a whole "substrate family" which share common recognition sequences. (
  • Most kinases are inhibited by a pseudosubstrate that binds to the kinase like a real substrate but lacks the amino acid to be phosphorylated. (
  • Once released from their inhibitory Regulatory subunit, the catalytic subunits can go on to phosphorylate a huge number of other proteins in the minimal substrate context Arg-Arg-X-Ser/Thr. (
  • To phosphorylate a protein or peptide substrate to completion, the ATP concentration should be about 5-fold over the limited substrate concentration. (
  • Two C-terminal cyclic nucleotide binding (CNB) domains cooperatively bind two molecules of cAMP, resulting in a conformational change of the R subunit that releases the active catalytic kinase subunit(s) from the inhibitory pseudo-substrate or substrate site of PKAR. (
  • We will not only review the well-known members of the family, such as kinase suppressor of Ras (KSR), but also put a special focus on the function of the recently identified or less studied scaffolders, such as fibroblast growth factor receptor substrate 2, flotillin-1 and mitogen-activated protein kinase organizer 1. (
  • LC Sciences provides a comprehensive kinase analysis service utilizing high density protein kinase substrate (PKS) peptide microarrays synthesized on Paraflo microfluidic chips for proteomic scale kinase profiling, quantitative measurement of kinase kinetic activities, and drug discovery research. (
  • This study shows that Par3 conserved region 3 (CR3) forms a tight inhibitory complex with a primed aPKC kinase domain, blocking substrate access. (
  • Phosphorylation usually results in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins. (
  • The developmental expression and the cellular localization of neurogranin (formerly designated p17), a brain-specific protein kinase C (PKC) substrate, were investigated. (
  • Binding of cGMP to the regulatory domain induces a conformational change which stops the inhibition of the catalytic core by the N-terminus and allows the phosphorylation of substrate proteins. (
  • Moreover, it appears to be regulated by virtue of it being a substrate for phosphorylation by casein kinase II (protein kinase CK2). (
  • This unique conformation of the kinase-substrate complex explains the reported modulation of Haspin activity by methylation of Lys 4 of the histone H3. (
  • In transgenic mice expressing a surrogate substrate (GFPdgn), PKG activation by sildenafil increased myocardial proteasome activities and significantly decreased myocardial GFPdgn protein levels. (
  • UPS-mediated proteolysis generally involves 2 steps: targeting of the substrate protein by ubiquitination and the subsequent degradation of the ubiquitinated protein by the 26S proteasome. (
  • We have now examined in detail the role of protein kinases in intercellular junction biogenesis by using a combination of highly specific and broad-spectrum inhibitors that act by independent mechanisms. (
  • The effect of PKC inhibitors on the development of tight junctions, as measured by resistance, was paralleled by a delay in the sorting of the tight-junction protein, zona occludens 1 (ZO-1), to the tight junction. (
  • If the source of protein to be phosphorylated is a crude extract of cells or tissue, it is very important to include the appropriate protease and protein phosphatase inhibitors in the lysis buffer and to use shorter incubation time for phosphorylation. (
  • As a result, protein kinase inhibitors are important research tools to study cell functions and human diseases. (
  • ARTICLE{Davies00specificityand, author = {Stephen P. Davies and Helen Reddy and Matilde Caivano and Philip Cohen}, title = {Specificity and mechanism of action of some commonly used protein kinase inhibitors}, journal = {Biochem. (
  • The specificities of 28 commercially available compounds reported to be relatively selective inhibitors of particular serine� threonine-specific protein kinases have been examined against a large panel of protein kinases. (
  • Ro 318220 and related bisindoylmaleimides, as well as H89, HA1077 and Y 27632, were more selective inhibitors, but still inhibited two or more protein kinases with similar potency. (
  • His current research focuses on the exploration of cellular signaling pathways in cell lines with respect to the role of various protein kinases using newly characterized kinase inhibitors identified by screening small chemical compound libraries. (
  • Protein kinase C inhibitors, H-7 or sphingosine, restored the abnormal acetylcholine-induced relaxations as well as suppressed the abnormal release of prostanoids in aorta exposed to elevated glucose. (
  • We describe a streamlined mass spectrometry-based chemoproteomics workflow to examine the SAR and target profiles of a small library of kinase inhibitors that consists of the drug dasatinib and a panel of general type II inhibitors. (
  • Traxler, Protein Tyrosine Kinase Inhibitors in Cancer Treatment, Expert Opinion on Therapeutic Patents, 7(6):571-588, 1997. (
  • Researcher synthesising protein kinases as part of research to determine the selectivity of protein kinase inhibitors and their use in drug targeting. (
  • Ten protein kinase inhibitors have now been approved as anti-cancer drugs and many more are undergoing clinical trials (as of 2012). (
  • Nearly all cell surface receptors utilize one or more of the mitogen-activated protein kinase cascades in their repertoire of signal transduction mechanisms. (
  • The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent. (
  • The activators of p38 (MKK3 and MKK6), JNK (MKK4 and MKK7), and ERK (MEK1 and MEK2) define independent MAP kinase signal transduction pathways. (
  • Up to 30% of all human proteins may be modified by kinase activity, and kinases are known to regulate the majority of cellular pathways, especially those involved in signal transduction. (
  • Abstract Protein kinase C (PKC) plays a key role in a variety of signal transduction processes. (
  • Protein kinase C (PKC) is a family of serine-threonine-specific kinases, consisting of at least eight isoforms 1 that play a key role in a range of signal transduction processes. (
  • Tyrosine-specific protein kinases (EC and EC phosphorylate tyrosine amino acid residues, and like serine/threonine-specific kinases are used in signal transduction. (
  • While the catalytic domain of these kinases is highly conserved , the sequence variation that is observed in the kinome (the subset of genes in the genome that encode kinases) provides for recognition of distinct substrates. (
  • out of 540 different protein kinase genes that make up for human kinome, only one other protein kinase, Casein kinase 2 , is known to exist in a physiological tetrameric complex. (
  • A metabolic protein that nourishes cancer cells also activates tumor-promoting genes by loosening part of the packaging that entwines DNA to make up chromosomes, a team led by scientists at The University of Texas MD Anderson Cancer Center reports in the Aug. 16 issue of Cell . (
  • When the epidermal growth factor receptor (EGFR) on the cell's membrane is activated by a growth factor, the PKM2 protein moves into the cell nucleus, where it binds to the promoter regions of genes. (
  • This separates another protein called histone deacetylase 3 (HDAC3) from the promoter regions of the genes CCND1 and MYC. (
  • HuSH-29 Kinase Collection contains 512 genes cloned in pRFP-C-RS vector allowing researchers to monitor transfection. (
  • We identify 518 putative protein kinase genes, of which 71 have not previously been reported or described as kinases, and we extend or correct the protein sequences of 56 more kinases. (
  • Chromosomal mapping revealed several small clusters of kinase genes and revealed that 244 kinases map to disease loci or cancer amplicons. (
  • Protein kinases are among the largest families of genes in eukaryotes ( 2-6 ) and have been intensively studied. (
  • A complete catalog of human protein kinases will aid in the discovery of human disease genes and in the development of therapeutics. (
  • Current Cancer Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular drug targets involved in cancer, e.g. disease specific proteins, receptors, enzymes, genes. (
  • The eukaryotic protein kinase family is one of the largest gene families in all eukaryotes, counting for 2-4% of all genes. (
  • The human genome contains about 500 protein kinase genes. (
  • The Hedgehog (Hh) family of secreted proteins controls cell growth and patterning during development, in part by regulating the expression of certain target genes in local areas. (
  • The human genome contains about 500 protein kinase genes and they constitute about 2% of all human genes. (
  • cAMP-dependent protein kinase" redirects here. (
  • PKA is also known as cAMP-dependent protein kinase ( EC ). (
  • PKA is also commonly known as cAMP-dependent protein kinase, because it has traditionally been thought to be activated through release of the catalytic subunits when levels of the second messenger cAMP rise in response to a variety of signals. (
  • Hence, the synonym cAMP-dependent protein kinase is commonly used. (
  • Because MAP2 kinases display very little activity on substrates other than their cognate MAPK, classical MAPK pathways form multi-tiered, but relatively linear pathways. (
  • In comparison to the three-tiered classical MAPK pathways, some atypical MAP kinases appear to have a more ancient, two-tiered system. (
  • As key components of many cell signaling pathways, protein kinases are implicated in a broad variety of diseases, including cancers and neurodegenerative conditions, and offer considerable potential as tractable targets for therapeutic intervention. (
  • The mRNA surveillance protein hSMG-1 functions in genotoxic stress response pathways in mammalian cells. (
  • Mitogen-activated protein kinase pathways. (
  • In the 20 years since Paul Simpson initially demonstrated that neurohormonal stimulation of cultured neonatal cardiomyocytes results in cellular hypertrophy, characteristic changes in cardiac gene expression, and activation of specific kinase signaling pathways ( 1 - 3 ), protein kinases have attracted attention as candidate mediators of the cardiac biomechanical stress and trophic responses. (
  • For some of the various signaling pathways affected by antidepressant treatment, it was shown that protein phosphorylation, which represents an obligate step for most pathways, is markedly affected by long-term treatment. (
  • Protein kinases modify an estimated 30% of the human proteome and thus regulate the majority of cellular transduction pathways. (
  • Kinases regulate most cellular pathways and are responsible for the modification of nearly a third of all human proteins. (
  • Thus, the two substrates of this enzyme are ATP and a protein , whereas its two products are ADP and phosphoprotein . (
  • While serine/threonine kinases all phosphorylate serine or threonine residues in their substrates, they select specific residues to phosphorylate on the basis of residues that flank the phosphoacceptor site, which together comprise the consensus sequence . (
  • The recognition motif for phosphorylation by Abl is I/V/L Y XXP/F. Abl, like many cytosolic protein tyrosine kinases, preferentially phosphorylates sites recognized by its own SH2 domain, selects substrates with large hydrophobic amino acids at the +3 position and β-branched amino acids at the -1 position (4). (
  • His research is focused on the identification and characterization of new substrates of protein kinase CK2 from Saccharomyces cerevisiae. (
  • Antidepressant treatment activates the two kinases and increases the endogenous phosphorylation of selected substrates (microtubule-associated protein 2 and synaptotagmin). (
  • The protein kinase family is large and important, but it is only one family in a larger superfamily of homologous kinases that phosphorylate a variety of substrates and play important roles in all three superkingdoms of life. (
  • Activity of the atypical protein kinase C (aPKC) is a key output of the Par complex as phosphorylation removes substrates from the Par domain. (
  • Kinases are turned on or off by phosphorylation (sometimes by the kinase itself - cis-phosphorylation/autophosphorylation), by binding of activator proteins or inhibitor proteins, or small molecules, or by controlling their location in the cell relative to their substrates. (
  • In the absence of cAMP, inactive Protein kinase A is a holoenzyme (PKA), a heterotetramer of two identical catalytic subunits (Pka-C) and two identical regulatory subunits (Pka-R). When cAMP is present, it binds to the regulatory subunits and releases catalytic subunits from the holoenzyme, allowing phosphorylation of target substrates. (
  • Once activated, the catalytic subunits are capable of phosphorylating a large number of protein substrates, both in vitro and in vivo (Jackson, 2002 and references therein). (
  • 1997). Another p38gamma substrates that do not require PDZ domain binding interactions are the mitochondrial protein Sab (Court et al. (
  • A serine/threonine protein kinase ( EC ) is a kinase enzyme that phosphorylates the OH group of serine or threonine (which have similar sidechains). (
  • These were formerly included in EC number "", which was a general EC number for any enzyme that phosphorylates proteins while converting ATP to ADP (i.e. (
  • Mitogen-activated protein kinase kinase (also known as MAP2K , MEK , MAPKK ) is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). (
  • c-Src phosphorylates specific tyrosine residues in other tyrosine kinases. (
  • c-Src should not be confused with CSK (C-terminal Src kinase), an enzyme that phosphorylates c-Src at its C-terminus and provides negative regulation of Src's enzymatic activity. (
  • Norway rat protein-coding gene Mapk1. (
  • You can select a given mouse superfamily member and download (or forward to NCBI BLAST) FASTA formatted protein sequences of that mouse gene and its mouse, human and rat homologs, as defined in the corresponding HomoloGene Class. (
  • Compositions and methods are provided for the treatment and diagnosis of diseases associated with protein kinase C. Oligonucleotides are provided which are specifically hybridizable with a PKC gene or mRNA. (
  • Methods of treating conditions amenable to therapeutic intervention by modulating protein kinase C expression with an oligonucleotide specifically hybridizable with a PKC gene or mRNA are disclosed. (
  • Our findings establish PKM2 as a histone kinase, which directly regulates gene transcription and controls cell cycle progression and proliferation of tumor cells' Lu said. (
  • As the world's leading gene company, OriGene offers comprehensive product solutions for studying human protein kinases. (
  • This provides a starting point for comprehensive analysis of protein phosphorylation in normal and disease states, as well as a detailed view of the current state of human genome analysis through a focus on one large gene family. (
  • In humans, this protein is encoded by the gene SRPK3. (
  • In the mature nervous system, these kinases transduce signals involved in many different processes including ion fluxes, receptor modulation, cell proliferation, and gene expression ( Kheifets and Mochly-Rosen, 2007 ). (
  • The cartoon depicts the structure of the TYRO3 gene (bottom) roughly aligned with the corresponding functional protein domains (top). (
  • If indeed CALLA is a suppressor gene, whether the gene is hypermethylated or the protein is phosphorylated, the end result may be the same: No CALLA activity. (
  • Overall, our data suggest that Haspin activity affects the phosphorylation state of proteins involved in gene expression regulation and splicing. (
  • Myotonin-protein kinase (MT-PK) also known as myotonic dystrophy protein kinase (MDPK) or dystrophia myotonica protein kinase (DMPK) is an enzyme that in humans is encoded by the DMPK gene. (
  • The dmpk gene product is a Ser/Thr protein kinase homologous to the MRCK p21-activated kinases and the Rho family of kinases. (
  • The MAPK12 gene encodes a 367 amino-acid protein of about 42 kDa. (
  • Mitogen-activated protein kinase 9 is an enzyme that in humans is encoded by the MAPK9 gene . (
  • The protein encoded by this gene is a member of the MAP kinase family. (
  • This kinase targets specific transcription factors, and thus mediates immediate-early gene expression in response to various cell stimuli. (
  • This gene and MAPK8 are also known as c-Jun N-terminal kinases. (
  • pronounced "sarc", as it is short for sarcoma), is a non-receptor tyrosine kinase protein that in humans is encoded by the SRC gene. (
  • It belongs to a family of Src family kinases and is similar to the v-Src (viral Src) gene of Rous sarcoma virus. (
  • Two transcript variants encoding the same protein have been found for this gene. (
  • Broad in its range of techniques and thoroughly detailed to help ensure experimental success, Protein Kinase Protocols offers both novice and experienced investigators powerful tools for understanding the functional roles of specific protein kinases within signaling cascades and for identification and evaluation of novel therapeutic targets. (
  • Here we review recent developments in the area of these cardiotrophic kinases, highlighting the utility of animal models that are helping to identify molecular targets in the human condition. (
  • The compounds KT 5720, Rottlerin and quercetin were found to inhibit many protein kinases, sometimes much more potently than their presumed targets, and conclusions drawn from their use in cell-based experiments are likely to be erroneous. (
  • The ability to determine structure-activity relationships (SAR) and identify cellular targets from cell lysates and tissues is of great utility for kinase inhibitor drug discovery. (
  • Stringent selection criteria for target identification were applied to deduce 28 protein targets for dasatinib and 31 protein targets for our general type II kinase inhibitor in HeLa cell lysate. (
  • Additional kinase and protein targets were identified with the general type II inhibitor analogs, with small structural changes leading to divergent target profiles. (
  • Our rapid workflow profiled cellular targets for six small molecules within a week, demonstrating that an unbiased proteomics screen of cellular targets yields valuable SAR information and may be incorporated at an early stage in kinase inhibitor development. (
  • Recent advances unravelling structure-function-relationships, regulatory mechanisms and physiological roles of protein kinases, renders them attractive targets for the development of novel treatment strategies. (
  • It is thought that Ci is phosphorylated by protein kinase A (PKA) and that processing of Ci into a cleaved form involves Slimb, a protein which may specify phosphorylated targets for ubiquitin/proteosome proteolysis. (
  • A dynamic transverse enrichment of atypical protein kinase C (aPKC) shifts the balance and transiently targets activated small GTPase RhoA , myosin phosphorylation and Rab11 vesicle trafficking to longitudinal junctions. (
  • Protein kinases are key focus targets in drug discovery. (
  • Due to their substantial involvement in signaling within and between cells, protein kinases have become the second most widely studied group of potential drug targets, after G-protein-coupled receptors (GPCR). (
  • G-protein coupled receptors (GPCR) are prominent targets in drug discovery. (
  • Purdue University researchers have developed a high-throughput method for matching kinases to the proteins they phosphorylate, speeding the ability to identify multiple potential cancer drug targets. (
  • Receptor Tyrosine Kinases as Targets for Drug Intervention", DN&P 7(6):334-339, 1994. (
  • There are two main types of protein kinase, the great majority are serine/threonine kinases, which phosphorylate the hydroxyl groups of serines and threonines in their targets and the other are tyrosine kinases, although additional types exist. (
  • Serine/Threonine Kinase receptors play a role in the regulation of cell proliferation, programmed cell death ( apoptosis ), cell differentiation, and embryonic development. (
  • Protein kinase C iota type (PRKCI) is a calcium- and diacylglycerol-independent serine/ threonine-protein kinase that plays a general protective role against apoptotic stimuli, is involved in NF-kappa-B activation, cell survival, differentiation and polarity, and contributes to the regulation of microtubule dynamics in the early secretory pathway [ PMID: 10467349 , PMID: 11544035 , PMID: 11257119 ]. (
  • In the unphosphorylated structure both serines line the putative lipid-binding site and may therefore play a role in the lipid-regulation of the kinase. (
  • Protein kinase A has several functions in the cell, including regulation of glycogen , sugar , and lipid metabolism . (
  • This paper summarizes data from different studies all aimed at elucidating regulation of protein kinase B in the diabetic heart. (
  • Protein kinase A (PKA), the main effector of cAMP in eukaryotes, is a paradigm for the mechanisms of ligand-dependent and allosteric regulation in signalling. (
  • 7500 members that confers ligand-dependent allosteric regulation to a diverse range of proteins 2 . (
  • AKAP200 is a Drosophila melanogaster member of the "A Kinase Associated Protein" family of scaffolding proteins, known for their role in the spatial and temporal regulation of Protein Kinase A (PKA) in multiple signaling contexts. (
  • MAP kinases act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. (
  • The closest relatives of MAPKs are the cyclin-dependent kinases (CDKs). (
  • It is not to be confused with AMP-activated protein kinase or cyclin-dependent kinases . (
  • In the case of classical MAP kinases, the activation loop contains a characteristic TxY (threonine-x-tyrosine) motif (TEY in mammalian ERK1 and ERK2 , TDY in ERK5 , TPY in JNKs , TGY in p38 kinases ) that needs to be phosphorylated on both the threonine and the tyrosine residues in order to lock the kinase domain in a catalytically competent conformation. (
  • Abl contains 407 amino acids (residues 237-643 of the p120-gag-abl polyprotein), which include the kinase catalytic domain, SH2 domain on the N-terminus and the I237M mutation. (
  • The catalytic subunit contains the active site, a series of canonical residues found in protein kinases that bind and hydrolyse ATP and a domain to bind the regulatory subunit. (
  • The protein kinase C (PKC) family of enzymes regulates cell physiology through phosphorylation of serine and threonine residues of many proteins in most cell types. (
  • There are also protein kinases that phosphorylate other amino acids, including histidine kinases that phosphorylate histidine residues. (
  • While MAP kinases are serine/threonine-specific, they are activated by combined phosphorylation on serine/threonine and tyrosine residues. (
  • Activity of MAP kinases is restricted by a number of protein phosphatases, which remove the phosphate groups that are added to specific serine or threonine residues of the kinase and are required to maintain the kinase in an active conformation. (
  • The amino acids at positions three and five within the conserved sequence are leucine (L) residues in TYRO3 and isoleucine (I) residues in the related receptor tyrosine kinases, AXL and MERTK. (
  • 2004). Three tyrosine residues (Y681, Y685, Y686) located within the activation loop of the kinase domain of the TYRO3 receptor correspond to three tyrosine residues in the MERTK receptor kinase domain, which have been identified as sites of autophosphorylation, however, there is no direct evidence that Y681, Y685, and Y686 are autophosphorylated in the TYRO3 receptor (Linger et al. (
  • A group of enzymes that are dependent on cyclic GMP and catalyzes the phosphorylation of serine or threonine residues of proteins. (
  • The kinase domain is in an active conformation, with a fully ordered and correctly positioned aC helix, and catalytic residues in a conformation competent for catalysis. (
  • This is conducted by specialized enzymes of the STE protein kinase group. (
  • In enzymology , the term non-specific serine/threonine protein kinase describes a class of enzymes that belong to the family of transferases , specifically protein-serine/threonine kinases . (
  • These enzymes transfer phosphates to the oxygen atom of a serine or threonine sidechain in proteins . (
  • In cell biology , protein kinase A ( PKA [N 1] ) is a family of enzymes whose activity is dependent on cellular levels of cyclic AMP (cAMP). (
  • Protein kinases are enzymes that add a phosphate group to a protein or other organic molecule (phosphorylation). (
  • Mutations and dysregulation of protein kinases play causal roles in human disease, affording the possibility of developing agonists and antagonists of these enzymes for use in disease therapy ( 7-9 ). (
  • We provide unique one-stop products and services for assays of DNA, RNA, protein, enzymes, antibodies, or small molecules, as well as proven microfluidic technology and novel microarray chemistry for design of your miniaturized assay devices for diagnostics and biosensing applications. (
  • Drug compounds being developed at Purdue University could effectively target and inhibit protein kinase enzymes and secondary mutated versions that drive multiple types of cancers. (
  • Eukaryotic protein kinases are enzymes that belong to a very extensive family of proteins that share a conserved catalytic core. (
  • [4] In contrast to the classical MAP kinases, these atypical MAPKs require only a single residue in their activation loops to be phosphorylated. (
  • Diaz-Meco MT, Municio MM, Sanchez P, Lozano J, Moscat J. Lambda-interacting protein, a novel protein that specifically interacts with the zinc finger domain of the atypical protein kinase C isotype lambda/iota and stimulates its kinase activity in vitro and in vivo. (
  • This group represents protein kinase C (KPC), including zeta/iota types from mammals, protein kinase C-like 3 from round worms [ PMID: 9422779 ] and atypical protein kinase C (aPKC) from fruit flies [ PMID: 10995441 ]. (
  • Structure, expression, and properties of an atypical protein kinase C (PKC3) from Caenorhabditis elegans. (
  • Drosophila atypical protein kinase C associates with Bazooka and controls polarity of epithelia and neuroblasts. (
  • Atypical protein kinase C is involved in the evolutionarily conserved par protein complex and plays a critical role in establishing epithelia-specific junctional structures. (
  • Atypical protein kinase C{iota} is required for bronchioalveolar stem cell expansion and lung tumorigenesis. (
  • We propose that most of the so-called "atypical kinases" are not intermittently derived from protein kinases, but rather diverged early in evolution to form a distinct phyletic group. (
  • Within the atypical kinases, the aminoglycoside and choline kinase families appear to share the closest relationship. (
  • In addition, our analysis suggests that the actin-fragmin kinase, an atypical protein kinase, is more closely related to the phosphoinositide-3 kinase family than to the protein kinase family. (
  • Conversely, the α-kinases appear to be an exception to the scenario of early divergence for the atypical kinases: they apparently arose relatively recently in eukaryotes. (
  • Atypical protein kinase C (aPKC) is a key apical-basal polarity determinant and Par complex component. (
  • Protein kinase C zeta type is a calcium- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signaling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP) [ PMID: 11035106 ]. (
  • Because FGF signaling is mediated largely by the mitogen-activated protein kinase (MAPK) pathway ( 26 , 27 ), these studies suggest that MAPK may play a critical role in the specification of neural fate and anteroposterior pattern. (
  • Curcumin has anti-breast cancer activity related to the activities of protein kinases on cell signal pathway. (
  • The mitogen-activated protein kinase (MAPK) pathway is the canonical signaling pathway for many receptor tyrosine kinases, such as the Epidermal Growth Factor Receptor. (
  • Downstream of the receptors, this pathway involves the activation of a kinase cascade that culminates in a transcriptional response and affects processes, such as cell migration and adhesion. (
  • In this review, we summarize the recent advances in the research on MAPK/extracellular signal-regulated kinase (ERK) pathway scaffolders. (
  • In this study, we identify a pathway essential for rod formation that involves protein kinase C (PKC). (
  • Most studies have looked at the receptor tyrosine kinases and examples of these are platelet derived growth factor receptor (PDGFR) pathway and epidermal growth factor receptor (EGFR). (
  • A mitogen-activated protein kinase ( MAPK or MAP kinase ) is a type of protein kinase that is specific to the amino acids serine and threonine (i.e., a serine/threonine-specific protein kinase ). (
  • Any of a group of kinases that phosphorylate the amino acids serine, threonine, and tyrosine in certain proteins, that regulate essential aspects of cell growth and movement, and that can cause cancer and other diseases when dysfunctional. (
  • Most protein kinases act on the amino acids serine and threonine, while tyrosine kinases act on tyrosine, and some protein kinases act on all three. (
  • The chemical activity of a kinase involves removing a phosphate group from ATP and covalently attaching it to one of three amino acids that have a free hydroxyl group. (
  • p38gamma (MAPK12) is a Serine/Threonine protein kinase of 367 amino acids with a predicted molecular mass of 42 kDa. (
  • CK2 is a ubiquitous and highly conserved protein serine / threonine kinase that has long been considered to play a role in cell growth and proliferation. (
  • The catalytic subunits of many protein kinases are highly conserved, and several structures have been solved. (
  • The intracellular or cytoplasmic domain is responsible for the (highly conserved) kinase activity, as well as several regulatory functions. (
  • Protein kinase A, a ubiquitous, highly conserved serine-threonine kinase, is a key intracellular transducer of many hormonal and other extracellular signals. (
  • Anti-SRSF protein kinase 3 antibodies are available from several suppliers. (
  • Your search returned 107 SRSF protein kinase 3 Antibodies across 22 suppliers. (
  • Data obtained by using antibodies that detect specific isoforms of DMPK indicate that the most abundant isoform of DMPK is an 80-kDa protein expressed almost exclusively in smooth, skeletal, and cardiac muscles. (
  • Types include those acting directly as receptors ( Receptor protein serine/threonine kinase ) and Intracellular signaling peptides and proteins . (
  • Various kinases are downstream effectors of neurohormone receptors that transduce signals from the sympathetic nervous and renin-angiotensin-aldosterone systems. (
  • C-type lectin receptors activate protein kinase C δ in a Syk-dependent manner to stimulate NF-κB signaling in response to fungi. (
  • Two major factors influence activity of MAP kinases: a) signals that activate transmembrane receptors (either natural ligands or crosslinking agents) and proteins associated with them (mutations that simulate active state) b) signals that inactivate the phosphatases that restrict a given MAP kinase. (
  • 1994). Following ligand binding to the extracellular domain, the TYRO3 receptors dimerize and autophosphorylation of the tyrosine kinase domain occurs. (
  • c-Src can be activated by many transmembrane proteins that include: adhesion receptors, receptor tyrosine kinases, G-protein coupled receptors and cytokine receptors. (
  • This research topic aims to provide an overview of the key protein kinases implicated in cardiovascular disease and their regulatory mechanisms including other protein kinases, protein phosphatases, scaffold proteins and the redox system of the cell. (
  • 2005). These proteins are scaffold proteins usually targeted to the plasma membrane cytoskeleton at specialised sites such as the neuromuscular junction and gap junctions through protein-protein interactions. (
  • LY 294002 was found to inhibit casein kinase-2 with similar potency to phosphoinositide (phosphatidylinositol) 3-kinase. (
  • Protein kinase CK2 (formerly casein kinase II or 2) is known to play a critical role in the control of cell growth and cell death and is thus intimately involved in the development of cancer. (
  • also known as casein kinase II. (
  • AMP-activated protein kinase (AMPK), an energy sensor, can regulate protein and lipid metabolism responding to alterations in energy supply. (
  • Because MAPK has been shown to down-regulate Smad1, MAPK may disrupt bone morphogenetic protein 4 (BMP-4) signaling during neural specification. (
  • Migrating neurons also have intrinsic machineries to regulate cytoskeletal proteins and adhesion properties. (
  • It also appears to regulate the production and function of important structures inside muscle cells by interacting with other proteins. (
  • The possible role of protein kinase C (PKC) in regulating this critical transition was assessed in both normal oocytes isolated from small antral follicles (18-day-old B6SJLF1 mice), which have not yet developed the capacity to progress to metaphase II (MII), and also oocytes defective in their ability to exit MI despite development to the preovulatory stage (24-day-old CX8 recombinant inbred strains). (
  • Novus' bioactive proteins are fully active, fully translationally modified and biorisk-free recombinant proteins. (
  • Protein kinase C eta (PKCeta) is one of several PKC isoforms found in humans. (
  • The expected protein mass is 62 kDa, but there are 4 reported isoforms. (
  • This tandem activation loop phosphorylation (that was proposed to be either distributive or processive, dependent on cellular environment) is performed by members of the Ste7 protein kinase family, also known as MAP2 kinases . (
  • Protein phosphorylation in particular plays a significant role in a wide range of cellular processes and is a very important posttranslational modification . (
  • The R 2 homodimer is formed by an N-terminal dimerization/docking (DD) domain that also mediates sub-cellular localization via A kinase anchoring proteins (AKAPs). (
  • Protein Kinase CK2 and Cellular Function in Normal and Disease States increases knowledge of the role of CK2 in the development of cellular dysfunction and emphasizes that this protein may serve as a target of drug development for improved cancer therapy. (
  • Activation of PKG increased proteasome peptidase activities, facilitated proteasome-mediated degradation of surrogate (enhanced green fluorescence protein modified by carboxyl fusion of degron CL1) and bona fide (CryAB R120G ) misfolded proteins, and attenuated CryAB R120G overexpression-induced accumulation of ubiquitinated proteins and cellular injury. (
  • The ubiquitin-proteasome system (UPS) mediates the degradation of most intracellular proteins and regulates diverse cellular processes, including protein quality control. (
  • p38gamma (MAPK12) regulates many cellular functions by phosphorylating several proteins. (
  • MAP2 kinases in turn, are also activated by phosphorylation, by a number of different upstream serine-threonine kinases ( MAP3 kinases ). (
  • At least 125 of the 500+ human protein kinases are serine/threonine kinases (STK). (
  • Calmodulin-Dependent Protein Kinase II (CaMKII) is a serine/threonine kinase. (
  • A series of reactions, mediated by the intracellular serine/threonine kinase protein kinase A, which occurs as a result of a single trigger reaction or compound. (
  • Our standard content PKS peptide microarray includes a comprehensive list of kinases and their related experimentally verified Serine, Threonine, and Tyrosine phosphorylation sites compiled from the Phospho.ELM database. (
  • Most kinases act on both serine and threonine, others act on tyrosine, and a number (dual-specificity kinases) act on all three. (
  • Serine/threonine protein kinases (EC phosphorylate the OH group of serine or threonine (which have similar side-chains). (
  • cGMP-dependent protein kinase or Protein Kinase G (PKG) is a serine/threonine-specific protein kinase that is activated by cGMP . (
  • PKG are serine/threonine kinases that are present in a variety of eukaryotes ranging from the unicellular organism Paramecium to humans. (
  • An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. (
  • Myotonin-protein kinase is a serine-threonine kinase that is closely related to other kinases that interact with members of the Rho family of small GTPases. (
  • Dystrophia myotonica protein kinase (DMPK) is a serine/threonine kinase composed of a kinase domain and a coiled-coil domain involved in the multimerization. (
  • Using this system, we have investigated the role of cAMP protein kinase A (PKA) signaling in pigment cell differentiation. (
  • MAPKs belong to the CMGC (CDK/MAPK/GSK3/CLK) kinase group. (
  • We have investigated the activity and function of mitogen-activated protein kinase (MAPK) during neural specification in Xenopus . (
  • In recent years, it has become evident that MAPK signaling is regulated and fine-tuned by proteins that can bind to several MAPK signaling proteins simultaneously and, thereby, affect their function. (
  • These so-called MAPK scaffolding proteins are, thus, important coordinators of the signaling response in cells. (
  • Important subgroups are the kinases of the ERK subfamily, typically activated by mitogenic signals, and the stress-activated protein kinases JNK and p38. (
  • 15. A method of inhibiting the expression of human protein kinase C-α in vitro comprising contacting human cells with a therapeutically effective amount of an antisense oligonucleotide 5 to 50 nucleotides in length, said antisense oligonucleotide comprising a nucleotide sequence complementary to a portion of the sequence set forth in SEQ ID NO: 105. (
  • Assay for Immunoprecipitated Phosphoinositide 3-Kinase (PI 3 Kinase) Activity (in vitro) Immunoprecipitation assay for Phosphoinositide 3-Kinase (PI 3 Kinase) Activity (in vitro) Protocol. (
  • In silico analyses in conjunction with in vitro kinase assay were used to study kinases that potentially phosphorylate DENV NS5. (
  • Phosphorylation of NS5 RdRp was further verified by PKC in vitro kinase assay. (
  • In this review, I shall give an overview the roles of protein kinases in neuronal migration. (
  • In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2,5-dione (MI-1) on rat colon cancer model. (
  • Cloning of a novel phosphatidylinositol kinase-related kinase: characterization of the human SMG-1 RNA surveillance protein. (
  • Grimson A, O'Connor S, Newman CL, Anderson P. SMG-1 is a phosphatidylinositol kinase-related protein kinase required for nonsense-mediated mRNA Decay in Caenorhabditis elegans . (
  • The two most divergent families, α-kinases and phosphatidylinositol phosphate kinases (PIPKs), appear to have distinct evolutionary histories. (
  • Assay activity of Lck kinase expressed in a retroviral vector in rat fibroblasts. (
  • Immunoprecipitation / Kinase Assay Immunoprecipitation / Kinase Assay Protocol. (
  • Protein Kinase C Assay Protein Kinase C Assay, Newton lab. (
  • The ELISA (enzyme-linked immunosorbent assay) is a widely used application for detecting and quantifying proteins and antigens from various samples. (
  • Ever since the discovery nearly 50 years ago that reversible phosphorylation regulates the activity of glycogen phosphorylase, there has been intense interest in the role of protein phosphorylation in regulating protein function. (
  • Protein phosphorylation regulates these processes. (
  • Conclusions- PKG positively regulates proteasome activities and proteasome-mediated degradation of misfolded proteins, likely through posttranslational modifications to proteasome subunits. (
  • For example, myotonic dystrophy protein kinase has been shown to turn off (inhibit) part of a muscle protein called myosin phosphatase. (
  • Protein kinases (PKs) are key components of protein phosphorylation based signaling networks in eukaryotic cells. (
  • With the advent of DNA cloning and sequencing in the mid-1970s, it rapidly became clear that a large family of eukaryotic protein kinases exists, and the burgeoning numbers of protein kinases led to the speculation that a vertebrate genome might encode as many as 1001 protein kinases ( 1 ). (
  • Most protein kinases belong to a single superfamily containing a eukaryotic protein kinase (ePK) catalytic domain. (
  • We observed surprisingly high sequence coverage on some proteins, enabling further analyses of phosphorylation sites for several target kinases without additional sample processing. (
  • Our in silico analyses indicated that the non-structural protein 5 (NS5), especially the RNA-dependent RNA polymerase (RdRp) domain, contains conserved phosphorylation sites for protein kinase C (PKC). (
  • Each protein contains a basic and hydrophobic (BH) motif that interacts directly with phospholipids and also overlaps with aPKC phosphorylation sites. (
  • We quantified 3964 phosphorylation sites on chromatin-associated proteins and identified a Haspin protein-protein interaction network. (
  • I have started measuring in-situ Protein Kinase C activity in permeabilized cells grown in 96-well plates, based on a few references from the literature such as: Heasley L.E., J.Biol.Chem. (
  • They won the Nobel Prize in Physiology or Medicine in 1992 for their work on phosphorylation and dephosphorylation and how it relates to protein kinase A activity. (
  • Protein Kinase Protocols procedures and assays for kinase activity. (
  • Protocol applicable only to kinases whose activity is not altered by cell lysis or immunoprecipitation procedures, and do not require soluble cofactors for activity. (
  • These strategies include the interference with protein kinase activity in general or more specifically target disease-specific kinase functions by regulating spatial-temporal distribution, protein-protein interactions and their subcellular localization. (
  • Mutation of the cleavage site in Ci resulted in protein that was still phosphorylated by PKA in vivo, but whose activity was inhibited. (
  • Remarkably, even within the universal core some kinase structures display notable changes, while still retaining essential activity. (
  • It has been shown deregulation of kinase activity is a frequent cause of disease, particularly cancer. (
  • The present work is a screening of dietary phytochemicals for their ability to modulate the activity of the intracellular protein kinase A (PKA) using a novel PKA-sensitive luciferase. (
  • The p38 MAP Kinase Inhibitor X, BIRB 796, also referenced under CAS 285983-48-4, controls the biological activity of p38 MAP Kinase. (
  • Because protein kinases have profound effects on a cell, their activity is highly regulated. (
  • Activity of these protein kinases can be regulated by specific events (e.g. (
  • Recent discoveries have highlighted the importance of Haspin kinase activity for the correct positioning of the kinase Aurora B at the centromere. (
  • In particular, we validated the phosphorylation of Ser 137 of the histone variant macroH2A as a target of Haspin kinase activity. (
  • Sildenafil treatment significantly increased myocardial PKG activity and significantly reduced myocardial accumulation of CryAB R120G , ubiquitin conjugates, and aberrant protein aggregates in mice with CryAB R120G -based desmin-related cardiomyopathy. (
  • cGMP transduces many of the biological effects of NO by directly binding to and stimulating the activity of cGMP-dependent protein kinase, also known as protein kinase G (PKG). (
  • The close relationship of DMPK to the Rho-kinases has led to speculation whether DMPK activity may be regulated in vivo by small G proteins, particularly of the Rho family. (
  • In this model, transient activation of kinase activity would occur in response to G protein second messengers, while longterm activation of DMPK could be mediated by a membrane associated protease that cleaves DMPK-1 to release cytosolic DMPK-2 in a persistently activated form. (
  • SAPK3/p38gamma binds to a variety of these proteins, such as alpha1-syntrophin, SAP90/PSD95 and SAP97/hDlg , and under stress conditions is able to phosphorylate them and modulate their activity (Hasegawa et al. (
  • Protein kinases are key regulators of cell function and are known to direct the activity, localization, and function of many proteins. (
  • A protein kinase is a kinase enzyme that modifies other proteins by chemically adding phosphate groups to them (phosphorylation). (
  • A protein kinase is a kinase which selectively modifies other proteins by covalently adding phosphates to them (phosphorylation) as opposed to kinases which modify lipids, carbohydrates, or other molecules. (
  • A protein kinase activator enhances phosphorylation. (
  • Aorta treated for 10 min with 4-phorbol 12-myristate 13-acetate (PMA), a protein kinase C activator, showed decreased relaxations to the endothelium-dependent vasodilator, acetylcholine, similar to normal aorta exposed to elevated glucose (22 and 44 mM) for 6 h. (
  • Potential kinase was inhibited or activated by a specific inhibitor (or siRNA), or an activator. (
  • Wang, G., Wang, B., and Jiang, J. (1999) Protein kinase A antagonizes Hedgehog signaling by regulating both the activator and repressor forms of Cubitus interruptus. (
  • Changes were reported to be induced in the function of protein kinase C, cyclic AMP-dependent protein kinase, and calcium/calmodulin-dependent protein kinase. (
  • For two of these kinases (cyclic AMP- and calcium/calmodulin-dependent), the changes have been studied in isolated neuronal compartments (microtubules and presynaptic terminals). (
  • 11 12 Besides cAMP-dependent and Ca 2+ -calmodulin-dependent protein kinases, endothelial cells also contain PKC. (
  • In Protein Kinase Protocols, a panel of highly skilled laboratory investigators describe both basic and more sophisticated methods for the analysis of kinase-mediated signaling cascades, with emphasis on the identification of proteins according to their interactive relationships and the analysis of their functional properties. (
  • Extracellular cues such as Reelin induce intracellular signaling cascades through the protein phosphorylation. (
  • Novus provides highly purified control peptides and proteins to ensure reliable results and reproducibility. (
  • We offer Guanylate kinase Peptides and Guanylate kinase Proteins for use in common research applications: ELISA, Protein Array, SDS-Page, Western Blot. (
  • Our Guanylate kinase Peptides and Guanylate kinase Proteins can be used in a variety of model species: Human. (
  • Choose from our Guanylate kinase Peptides and Proteins. (
  • p38gamma (MAPK12), also known as Stress-activated protein kinase 3 (SAPK3) belongs to the p38 subfamily of MAPKs. (
  • A feature that makes p38gamma unique among the p38 MAPKs is its short C-terminal sequence -KETXL, an amino acid sequence ideal for binding PDZ domains in proteins. (
  • Protein phosphorylation is one of the most important molecular mechanisms by which extracellular signals produce their biological responses in cells. (
  • Molecular Dynamics of Protein Kinase-Inhibitor Complexes: A Valid. (
  • That enables them to follow and understand structure and dynamics of protein-ligand systems with extreme molecular detail on scales where motion of individual atoms can be tracked. (
  • The Gs alpha subunit of the stimulated G protein complex exchanges GDP for GTP and is released from the complex. (
  • Cloning and characterization of BCY1, a locus encoding a regulatory subunit of the cyclic AMP-dependent protein kinase in Saccharomyces cerevisiae. (
  • Four alleles of Cos1 appear to be dominant-negative mutations of a catalytic subunit of protein kinase A ( pka-C1 ) and the fifth allele, Cos1 A1 , is a gain-of-function allele of the PKA regulatory subunit pka-RII . (
  • The number of protein sequences returned does not always match the numbers of homologs shown, because the same protein sequence can be associated with multiple homologs. (
  • For mouse superfamily members not included in any HomoloGene Class, only the mouse protein sequence is returned. (
  • Note that the 'protein existence' evidence does not give information on the accuracy or correctness of the sequence(s) displayed. (
  • 10. An antisense oligonuclcotide 5 to 50 nucleotides in length comprising a nucleotide sequence which is complementary to the long mRNA transcript of human protein kinase C-α and which is not complementary to the short mRNA transcript of human protein kinase C-α. (
  • 13. A polynucleotide probe comprising a nuclcotide sequence complementary to the long mRNA transcript of human protein kinase C-α. (
  • We have catalogued the protein kinase complement of the human genome (the "kinome") using public and proprietary genomic, complementary DNA, and expressed sequence tag (EST) sequences. (
  • The near-completion of the human genome sequence now allows the identification of almost all human protein kinases. (
  • Hence, the protein kinase-like superfamily has undergone substantial structural and sequence revision over long evolutionary timescales. (
  • All three splice variants encode a transmembrane TYRO3 protein, but differ in the signal peptide sequence at the amino terminus (Biesecker et al. (
  • The conserved sequence within the kinase domain is shown. (
  • p38gamma (MAPK12) possesses at the C-terminal a sequence that binds to PDZ domain of several proteins. (
  • Select one or more mouse PIRSF members to download protein sequences or forward to NCBI BLAST. (
  • The identification of protein kinase C iota as a regulator of the Mammalian heat shock response using functional genomic screens. (
  • Phosphorylation usually alters the functional characteristics of the target protein and can act as an on/off switch for protein functions. (
  • Dr. Khalil Ahmed is a Professor at the University of Minnesota, and a Senior Research Career Scientist at Minneapolis VA Health Care System, Minneapolis, Minnesota, U.S.A. He has a long history of studies on the functional biology of protein kinase CK2 in normal and neoplastic cells. (
  • LC Sciences is a genomics and proteomics company offering innovative, customizable, and comprehensive microarray services for nucleic acid/protein profiling and functional analysis, biomarker-discovery, novel drug screening, and the custom development of diagnostic devices. (
  • Akap550 encodes a protein that has no known functional domains other than a coiled-coil Pka-RII binding site (Han, 1997). (
  • This study addresses asymmetric fate determinant localization in the developing Drosophila nervous system, specifically the control of the polarized distribution of the cell fate adapter protein Miranda . (
  • The specific localization of the protein in integrative areas of the rat brain suggests a highly specialized function of neurogranin in the CNS. (
  • Src contains at least three flexible protein domains, which, in conjunction with myristoylation, can mediate attachment to membranes and determine subcellular localization. (
  • These kinases consist of a transmembrane receptor with a tyrosine kinase domain protruding into the cytoplasm. (
  • Crystallographic structure of the leucine zipper domain of human cGMP dependent protein kinase I beta. (
  • Kinases are a class of proteins that attach phosphate groups to other proteins. (
  • You can also "Select all" mouse superfamily members to obtain their protein sequences and the protein sequences for all mouse, human and rat homologs of the mouse superfamily members. (
  • New nucleic acid sequences are provided which encode 3' untranslated regions of human protein kinase C alpha polynucleotide probes for PKC alpha are also disclosed. (
  • Kinase dysfunction is also connected to a variety of human diseases including cancer, inflammatory conditions, autoimmune disorders, and cardiac diseases. (
  • Indicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma. (
  • The OriGene True Clone collection has proven to be an excellent source of full-length human cDNAs for use in Regeneron's protein expression and target validation platforms. (
  • This kinase exists both as a membrane-associated and as a soluble form in human left ventricular samples. (
  • Just rehydrate and add cells for RNAi screening of human kinases. (
  • The Human ON-TARGET plus RTF Protein Kinase siRNA Library includes siRNA reagents directed against phylogenetically related kinases. (
  • Working in cell lines and mouse models of glioblastoma multiforme, the most lethal form of brain tumor, senior author Zhimin Lu, Ph.D., associate professor of Neuro-Oncology at MD Anderson, and colleagues show that pyruvate kinase M2 (PKM2) fuels tumor growth by influencing a histone protein. (
  • The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (
  • Xu W, Qian J, Zeng F, Li S, Guo W, Chen L, Li G, Zhang Z, Wang QJ, Deng F. Protein kinase Ds promote tumor angiogenesis through mast cell recruitment and expression of angiogenic factors in prostate cancer microenvironment. (
  • This kinase blocks the ubiquitination of tumor suppressor p53, and thus it increases the stability of p53 in nonstressed cells. (
  • Protein Kinase C (PKC) isoform PKCε has been shown to translocate to subcellular organelles including mitochondria upon activation. (