Family protein kinases. Medical search. Frequent questions

The serine/threonine kinase protein kinase D1 (PKD1) is a stress-responsive kinase and sensor for reactive oxygen species, which can initiate cell survival through NF-κB signaling. (biologists.com)

3: Both PD98059 (MAPK/ERK kinase inhibitor) and SB203580 (p38 MAPK inhibitor) attenuated FCS-induced LIF protein production and gene expression. (unboundmedicine.com)
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfiler TM service. (guidetopharmacology.org)
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. (guidetopharmacology.org)
To date, all of the kinase inhibitor drugs on the market are for use in an oncology setting. (soci.org)
The kinases are represented in complex with an ATP molecule (green, orange, blue, red) and a substrate-mimicking inhibitor (PKIA, yellow). (plos.org)
The human trabecular meshwork cells were treated with t BHP for 1 or 2 h with or without pretreatment of SB203580, an inhibitor of MAP kinase homologs. (molvis.org)
The binding site for allosteric inhibitor (amino acid) is highly conserved between human liver pyruvate kinase (hL-PYK) and the rabbit muscle isozyme (rM 1 -PYK). (figshare.com)
Consistently, LTD by dopamine + 1 S ,3 R -ACPD coapplication, as well as the two other forms of LTD (LTD by dopamine + tetani and LTD by 1S,3R-ACPD + tetani), was blocked by bath application of MAP-K kinase inhibitor PD98059. (jneurosci.org)

Mitogen-activated protein kinases (MAPKs) comprise a large family of proteins activated by a wide range of proinflammatory cytokines and environmental stress. (molvis.org)
Immunoblot analyses with anti-active mitogen-activated protein kinases (MAP-Ks) revealed that D1 receptors, D2 receptors, group I mGluRs, and group II mGluRs all contribute to MAP-K activation in prefrontal cortex, and that combined activation of dopamine receptors and mGluRs synergistically or additively activate MAP-Ks. (jneurosci.org)
Interestingly, TiO2 NPs increased the AP-1 activity via stimulating the expression of mitogen-activated protein kinases (MAPKs) family members, including extracellular signal-regulated protein kinases (ERKs), p38 kinase, and C-Jun N-terminal kinases (JNKs). (cdc.gov)

We have previously examined the specificities of 28 commercially available compounds, reported to be relatively selective inhibitors of particular serine/threonine-specific protein kinases [Davies, Reddy, Caivano and Cohen (2000) Biochem. (nih.gov)
A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase Hotspot SM platform. (guidetopharmacology.org)
In a keynote lecture, Professor Malcolm Ranson (University of Manchester / Christie Hospital) provided an insight into the clinical aspects of developing kinase inhibitors as effective medicines. (soci.org)
Additional presentations detailed kinase inhibitors, which have potential for the treatment of diseases in therapeutic areas other than cancer. (soci.org)
A screen of 72 inhibitors against 456 human kinases. (guidetomalariapharmacology.org)
Of note, the AP-1 activation induced by TiO2 NPs could be blocked by specific inhibitors (SB203580, PD98059, and SP 600125, respectively) that inhibit ERKs and p38 kinase but not JNKs. (cdc.gov)
A number of drugs and toxins have been identified as risk factors for pulmonary arterial hypertension such as fenfluramine (and other related weight-loss drugs), amphetamines, protein kinase inhibitors (such as dasatinib ), cocaine , and selective serotonin reuptake inhibitors (SSRIs). (msdmanuals.com)

Thus, PKCθ represents an additional member of the PKC family, and its predominant expression in hematopoietic cells suggests that it may play a role in signal transduction and growth regulatory pathways unique to these cells. (bgu.ac.il)
c-Src tyrosine kinase plays an important role in signal transduction pathways, where its activity is regulated by phosphorylation of the two tyrosine residues. (intechopen.com)
Mathematical modeling of signal transduction networks has previously been used to map out thermodynamical using rate equations is increasingly attracting attention as a properties of protein-folding models (6,7). (lu.se)

The method, named Predikin, identifies key conserved substrate-determining residues in the kinase catalytic domain that contact the substrate in the region of the phosphorylation site and so determine the sequence surrounding the phosphorylation site. (biomedcentral.com)
Predikin now consists of two components: (i) PredikinDB, a database of phosphorylation sites that links substrates to kinase sequences and (ii) a Perl module, which provides methods to classify protein kinases, reliably identify substrate-determining residues, generate scoring matrices and score putative phosphorylation sites in query sequences. (biomedcentral.com)
New features in Predikin include the use of SQL queries to PredikinDB to generate predictions, scoring of predictions, more reliable identification of substrate-determining residues and putative phosphorylation sites, extended options to handle protein kinase and substrate data and an improved web interface. (biomedcentral.com)
The post-translational modification of proteins by phosphorylation of serine, threonine or tyrosine residues is a ubiquitous process in cellular regulation. (biomedcentral.com)
Protein kinases, the enzymes responsible for protein phosphorylation, make up almost 2% of protein-encoding genes in the human genome [ 1 ] and an estimated 30-50% of human proteins are phosphorylated [ 2 ]. (biomedcentral.com)
Phosphorylation of the AP2 mu subunit by AAK1 mediates high affinity binding to membrane protein sorting signals. (sdbonline.org)
An in vitro phosphorylation assay demonstrated that PKA phosphorylated the recombinant protein of an active trans-sialidase. (elsevierpure.com)
Protein phosphorylation is a signalling mechanism that regulates most aspects of cellular life, and protein kinases, which carry out this post-translational modification, constitute the largest family of enzymes encoded by the human genome. (lu.se)
An overall aim of our research is to study the regulation and function of protein phosphorylation cascades with relevance to type 2 diabetes, with a particular focus on adipose tissue, since this tissue is involved in the pathogenesis of diabetes. (lu.se)

Phosphagen (guanidino) kinases are enzymes that transphosphorylate a high energy phosphoguanidino compound, like phosphocreatine (PCr) in the case of creatine kinase (CK) or phosphoarginine in the case of arginine kinase, which is used as an energy-storage and -transport metabolite, to ADP, thereby creating ATP. (nih.gov)
The symposium showcased some of the current research into this family of enzymes. (soci.org)
A plethora of connexin-associated proteins have been discovered including cytoskeletal elements enzymes adhesion molecules and signaling molecules. (liveconscience.com)

Description: In vitro inhibitory activity using the proprietary LanthaScreen Eu kinase binding assay. (guidetomalariapharmacology.org)
Western blotting assay was implemented to check the levels of phosphatidylinositol 3-kinase and protein kinase B. Results revealed that piperine induced dose reliant cytotoxicity in MCF-7 human breast cancer cells. (ijpsonline.com)
Finally, Western blotting assay predicted constant expression of phosphatidylinositol 3-kinase and protein kinase B and reduced expression of phosphorylated phosphatidylinositol 3-kinase. (ijpsonline.com)

To investigate further the potential role of mutated protein kinases in the development of TGCT and to characterize the prevalence and patterns of point mutations in these tumors, we have sequenced the coding exons and splice junctions of the annotated protein kinase family of 518 genes in a series of seven seminomas and six nonseminomas. (ox.ac.uk)
Comparative genomic hybridization and LOH analysis using SNP arrays demonstrated that the 13 TGCTs mutationally screened through the 518 protein kinase genes were uniformly aneuploid with consistent chromosomal gains on 12p, 8q, 7, and X and losses on 13q, 18q, 11q, and 4q. (ox.ac.uk)
Members of the protein kinase C (PKC) family of serine/threonine kinases play a key role in regulating the differentiation and growth of diverse cell types and, to date, the cloning of seven mammalian PKC genes encoding eight distinct isoforms has been reported. (bgu.ac.il)
Degenerate oligonucleotide primers corresponding to conserved sequence motifs, which distinguish the PKC family from other protein kinases, were employed in polymerase chain reactions (PCR) to amplify partial core sequences of putative PKC genes from a human peripheral blood lymphocyte-derived cDNA library. (bgu.ac.il)
The CASK protein is primarily found in nerve cells (neurons) in the brain, where it helps control the activity (expression) of other genes that are involved in brain development. (medlineplus.gov)
Considering the important role of activator protein-1 (AP-1) in regulating multiple genes involved in the cell proliferation and inflammation and the induction of neoplastic transformation, we aimed to evaluate the potency of TiO2 NPs (≤ 20 nm) on the activation of AP-1 signaling pathway and the generation of reactive oxygen species (ROS) in a mouse epidermal cell line, JB6 cells. (cdc.gov)

FCS also induced activation of extracellular signal-regulated kinase (ERK), p38 MAPK and c-Jun NH(2)-terminal kinase (JNK). (unboundmedicine.com)
PIK3CA (phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit a) is one of the four catalytic subunits of PI3K protein, which plays an essential role in extracellular growth signaling. (sigmaaldrich.com)

Previous work has documented activating mutations in the KIT receptor tyrosine kinase in testicular germ-cell tumors (TGCT). (ox.ac.uk)
c-Src (cellular Src), encoded by Src gene, is a non-receptor tyrosine kinase first isolated as the normal cellular homolog to the potent avian sarcoma viral transforming oncogene v-Src [ 4 ]. (intechopen.com)

Besides CK and AK, the most studied members of this family are also other phosphagen kinases with different substrate specificities, like glycocyamine kinase (GK), lombricine kinase (LK), taurocyamine kinase (TK) and hypotaurocyamine kinase (HTK). (nih.gov)
We have previously described an approach to predicting the substrate specificity of serine-threonine protein kinases. (biomedcentral.com)
How a particular protein kinase recognises its substrate protein(s) is therefore a key question. (biomedcentral.com)
Two major factors determine the formation of a protein kinase-substrate complex [ 4 ]. (biomedcentral.com)
The first, termed substrate recruitment, encompasses any process that increases the effective concentration of the protein kinase substrate. (biomedcentral.com)
The second factor, termed peptide specificity, describes the interaction between amino acid residues in the catalytic domain of the protein kinase and the substrate residues that surround the phosphorylated residue. (biomedcentral.com)
Crystal structures of protein kinases with bound substrate peptides show that substrate residues at positions -3 to +3 relative to the phosphorylated serine, threonine or tyrosine residue adopt an extended conformation and bind to a pocket in the catalytic domain of the protein kinase [ 8 ]. (biomedcentral.com)
The relative contribution of substrate recruitment and peptide specificity to protein kinase substrate specificity varies between protein kinases. (biomedcentral.com)
However, it is recognised that for many protein kinase families, particularly those that phosphorylate Ser/Thr residues, peptide specificity is the major factor that determines substrate specificity. (biomedcentral.com)
In addition, a phospho-(Ser/Thr) PKA substrate antibody detected bands on immunoblot analysis of trans-sialidase antibody precipitated proteins from parasite lysate and the media of L 6 E 9 myoblasts infected with trypomastigotes as well as from a SA85-1.1 antibody precipitated proteins from parasite lysate. (elsevierpure.com)

Our results suggest that the combined use of Roscovitine and Kenpaullone may be useful for identifying substrates and physiological roles of cyclin-dependent protein kinases, whereas the combined use of Kenpaullone and LiCl may be useful for identifying substrates and physiological roles of glycogen synthase kinase 3. (nih.gov)
The combined use of SU 6656 and either PP1 or PP2 may be useful for identifying substrates of Src family members. (nih.gov)
The new features significantly enhance the ability of Predikin to analyse protein kinases and their substrates. (biomedcentral.com)
Protein kinases and their substrates regulate essentially all cellular processes through complex regulatory networks, in which phosphorylated proteins act as switches that tune the response of the cell to environmental stimuli. (biomedcentral.com)
In general, a protein kinase acts on a discrete set of substrates to ensure that signalling fidelity is maintained. (biomedcentral.com)
The prediction of peptide specificity is therefore the basis for most of the available computational methods aimed at predicting substrates of protein kinases. (biomedcentral.com)

Crystal structure of human dual specificity protein kinase (TTK). (guidetomalariapharmacology.org)

This kinase can be recruited to vesicle tubular clusters (VTCs) by direct interaction with the small GTPase RAB2, where this kinase phosphorylates glyceraldehyde-3-phosphate dehydrogenase (GAPD/GAPDH) and plays a role in microtubule dynamics in the early secretory pathway. (nih.gov)
Also, other proteins which involved in the same pathway with MAPK4 were listed below. (creativebiomart.net)
Hence, evidenced the blocking of phosphatidylinositol 3-kinase/protein kinase B signaling pathway. (ijpsonline.com)
It induced apoptosis, suppressed cell migration and invasion, blocked cell cycle and phosphatidylinositol 3-kinase/ protein kinase B signaling pathway. (ijpsonline.com)
The mutation appears to have a direct role in activating the MAP kinase pathway, which controls processes such as cell proliferation, differentiation, survival and apoptosis (cell death). (gsk.com)
There is evidence that metformin has activity on the 5'-AMP-activated protein kinase pathway, where it can help reduce inflammation and cellular stress. (medscape.com)

Members of the RYK/Derailed family have recently been shown to regulate axon guidance in both Drosophila and mammals by acting as Wnt receptors. (biologists.com)
A family of structurally related cell-surface receptors that signal through an intrinsic PROTEIN-TYROSINE KINASE. (bvsalud.org)

Oomycetes possess a family of novel proteins called GPCR-PIPKs (GKs) that are composed of a seven-transmembrane spanning (7-TM) domain fused to a phosphatidylinositol phosphate kinase (PIPK) domain. (wur.nl)
PIK3CA (phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit a) is one of the four subunits of the 110kDa catalytic subunit of PI3K protein, which contains a regulatory region of 85kDa. (sigmaaldrich.com)

RESEARCH DESIGN AND METHODS- To examine whether hypothalamic protein kinase C (PKC) mediates the ability of central nervous system lipids to activate K ATP channels and regulate glucose production in normal rodents, we first activated hypothalamic PKC in the absence or presence of K ATP channel inhibition. (diabetesjournals.org)

Belongs to the protein kinase superfamily. (lu.se)

Essential for recruitment of Atg proteins to the pre-autophagosomal structure, the putative site for autophagosome formation, under starvation condition, resulting in the sequestration of cytoplasmic proteins and organelles for bulk degradation. (yeastgenome.org)

Sequence analysis of the protein kinase gene family in human testicular germ-cell tumors of adolescents and adults. (ox.ac.uk)
The protein kinase gene family is the most frequently mutated in human cancer. (ox.ac.uk)
Unexpected complexity of the Aquaporin gene family in the moss Physcomitrella patens. (lu.se)

The mutations that cause CASK -related intellectual disability affect the role of the CASK protein in brain development and function. (medlineplus.gov)
MICPCH is caused by mutations that eliminate CASK function, while mutations that impair the function of this protein cause XL-ID with or without nystagmus. (medlineplus.gov)
Affected individuals with nystagmus may have CASK gene mutations that disrupt the interaction between the CASK protein and the protein produced from the FRMD7 gene, leading to problems with the development of the oculomotor neural network and resulting in abnormal eye movements. (medlineplus.gov)
NEMO consists of 10 exons, and most mutations cause deletions of exons 4-10, resulting in a truncated protein. (medscape.com)
Hypomorphic mutations may impair but not abolish NEMO protein function. (medscape.com)
A number of genetic mutations have been identified in families with this disorder (heritable). (msdmanuals.com)

It phosphorylates and activates protein kinase B (PKB) protein. (sigmaaldrich.com)
These data support that PKA phosphorylates trans-sialidase super family members in vivo. (elsevierpure.com)

Bottom) The values for each domain position have been grouped according to the functional category ('catalytic', 'regulatory', 'proximal', etc.) and the distribution plotted separately at the family and subfamily level. (plos.org)

This diagram displays the protein subunits (blue) of the complex and how they interact with each other. (yeastgenome.org)
The IKB is phosphorylated by a multiprotein complex with two kinases subunits. (medscape.com)

Numb-associated kinase interacts with the phosphotyrosine binding domain of Numb and antagonizes the function of Numb in vivo. (sdbonline.org)
An inhibitory molecule of the IKB family interacts with NF-KB to sequester it in the cytoplasm. (medscape.com)

Aggregated analysis of sequence divergence across kinase families (left) and subfamilies (right). (plos.org)
Middle) Total number of switches mapped to the kinase primary sequence, with secondary structure elements represented above the bar plot. (plos.org)
We examined the coding sequence of 518 protein kinases, approximately 1.3 Mb of DNA per sample, in 25 breast cancers. (uea.ac.uk)
The deduced primary structure contains consensus sequences characteristic of protein kinase catalytic domains and, based on its amino acid sequence and domain structure, is a member of the PKC family. (bgu.ac.il)

However, Erk3 is distinguished from other MAP kinases in that it lacks the conserved TXY motif in its activation loop, poss Encodes a nuclear and cytoplasmically localized MAP kinase involved in mediating responses to pathogens. (creativebiomart.net)
Activation of the transcription factor nuclear factor KB (NF-KB) requires the NEMO protein. (medscape.com)
The NEMO protein is required for the activation of the kinase complex. (medscape.com)

This finding is inconsistent with the idea that allosteric pathways are conserved between homologues of a protein family. (figshare.com)

Phylogeny of major intrinsic proteins. (lu.se)

4: Expression of a dominant-negative mutant form of JNK1 that blocked FCS-induced JNK activity had no effect on protein production and gene expression of these cytokines. (unboundmedicine.com)
One unit of 110a/p85a kinase activity is defined as the amount of enzyme required to produce 1 pmol of Phosphoinositol-3, 4,5-Trisphosphate/min at 37°C. (sigmaaldrich.com)
The strict conservation of GH1 domain across GKAP family members and the lack of a catalytic active site required for enzyme activity imply that the GH1 domain might serve as a protein-protein interaction module for the synaptic protein clustering. (rcsb.org)
Little is known about how the kinase activity-deficient RYKs transduce Wnt signals. (biologists.com)
Derailed and SRC64B form a complex, which contains catalytically active SRC64B, the formation or stability of which requires SRC64B kinase activity. (biologists.com)

Top) Results mapped to kinase structures (mouse protein kinase A: PDB 1ATP). (plos.org)

Identification of an adaptor-associated kinase, AAK1, as a regulator of clathrin-mediated endocytosis. (sdbonline.org)
Protein kinase A (PKA) has been suggested as a regulator of stage differentiation in Trypanosoma cruzi. (elsevierpure.com)

These connexin-associated proteins are shown to regulate a number of mechanisms involved in IMPA2 antibody both channel-dependent and independent functions by connexins [8-10]. (liveconscience.com)
Immunoprecitation demonstrated that a TcPKAc monoclonal antibody was able to pull-down proteins recognized by trans-sialidase antibodies as well as a SA85-1.1 antibody and vice versa. (elsevierpure.com)

The PKC family comprises at least eight members, which are differentially expressed and are involved in a wide variety of cellular processes. (nih.gov)

Nucleotide-binding domain and leucine-rich repeat domain-containing (NLR) proteins are sentinels of plant immunity that monitor host proteins for perturbations induced by pathogenic effector proteins. (nature.com)

2011) Regulation and function of TPL-2, an IκB kinase-regulated MAP kinase kinase kinase. (guidetopharmacology.org)
Consequently, the regulation/ misregulation of kinases has linked them to a number of diseases and they provide a wealth of opportunity as targets for drug discovery. (soci.org)

Connexins a family of transmembrane proteins are components of both gap junction channels and hemichannels which mediate the exchange of ions and small molecules between adjacent cells and between the inside and outside of the cell respectively. (liveconscience.com)

A domain position is considered to be 'frequently switching' if the number of switches lies above a 90th percentile threshold for the kinase domain. (plos.org)
In this study, crystal structure of the GH1 domain of GKAP from Rattus norvegicus was determined in fusion with an N-terminal maltose-binding protein at 2.0 Å resolution. (rcsb.org)
Erk3, also known as MAPK6 or p97 MAPK, is almost 50% identical to Erk1/2 at the kinase domain located in its amino-terminal region. (creativebiomart.net)
A rabbit antiserum raised against a unique (V3 domain) bacterially expressed PKCθ fragment immunoprecipitated specifically an 82- kDa protein from Jurkat cell lysates. (bgu.ac.il)
c-Src tyrosine kinase consists of the N-terminal unique region, the Src homology 3 (SH3), SH2, linker, kinase domain, and the regulatory C-terminal tail. (intechopen.com)
TWIK-related acid-sensitive potassium channel 1 (TASK-1 encoded by KCNK3) belongs to the family of two-pore domain potassium channels. (ersjournals.com)

The main aim of our research is to understand the molecular details and physiological roles of the multitude of water channel-like proteins present in plants and animals. (lu.se)

Defects in these networks result in a variety of disease states making protein kinases important targets for drug design [ 3 ]. (biomedcentral.com)

The aim of this study was to evaluate the role of mitogen-activated protein kinase (MAPK) family in serum-induced secretion of LIF and IL-6 by bone marrow stromal cells. (unboundmedicine.com)
It is also used as a generic term for the MAPK family (ERK, JNK, p38 etc). (sciencedaily.com)

Anatomy19

Organisms9

Chemicals and Drugs167

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Phenomena and Processes41

Disciplines and Occupations1

Information Science3

Serine-threon1

Inhibitor8

Mitogen-Activat3

Inhibitors7

Signal Transduction3

Phosphorylation9

Enzymes3

Assay3

Genes6

Extracellular2

Receptor tyrosi2

Substrate10

Substrates6

Dual-specificity1

Pathway6

Receptors2

Phosphatidylinositol2

Inhibition1

Superfamily1

Cytoplasmic1

Gene family3

Mutations6

Phosphorylates2

Subfamily1

Subunits2

Interacts2

Sequence4

Activation3

Pathways1

Phylogeny1

Activity5

Structures1

Regulator2

Antibody2

Cellular processes1

Nucleotide1

Regulation2

Transmembrane1

Domain6

Physiological roles1

Targets for drug1

MAPK2