Selectively enhances protein kinase inhibitors. Medical search. Frequent questions

p38 MAPK (p38 mitogen-activated protein kinase) are a group of kinases responsive to stress stimuli. (cancer-research-network.com)
Mechanistically, we found that AMPK activation increased, whereas AMPK inhibition decreased, the levels of mitogen-activated protein kinase phosphatase-1 (MKP-1), an inducible nuclear phosphatase, by regulating proteasome-dependent degradation of MKP-1. (diabetesjournals.org)

The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. (wikipedia.org)
In primary mouse hepatocytes, GW1516 treatment stimulated AMP-activated protein kinase ( AMPK ) and acetyl-CoA carboxylase ( ACC ) phosphorylation in WT hepatocytes, but not AMPKβ1−/− hepatocytes. (edu.au)
Consistent with an increased level of cyclin D1, the phosphorylation of retinoblastoma protein (Rb) and the levels of Rb-E2F-regulated genes cyclin A, cyclin E, MCM3, and PCNA are also elevated. (elsevierpure.com)
In vitro kinase assays and immunoblotting using lysates from human MV4;11 leukemic cells showed inhibition of phosphorylation of known PIM downstream targets, such as BAD and eukaryotic translation initiation factor 4E-binding protein 1, by K00135. (ox.ac.uk)
Loss of the PPM1H phosphatase that is specific for LRRK2-phosphorylated Rab GTPases yields the same cilia loss phenotype seen in mice expressing pathogenic LRRK2 kinase, strongly supporting a connection between Rab GTPase phosphorylation and cilia loss. (elifesciences.org)
In cellular assays, Ralimetinib selectively suppresses the p-MK2 (phosphorylation of MK2 (Thr334)), but shows no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. (cancer-research-network.com)
In this study, L-selectin was found to be phosphorylated in lymphoblastoid cell lines, and phosphorylation was enhanced by phorbol ester (phorbol 12-myristate 13-acetate (PMA)) treatment. (upenn.edu)
It not only inhibits tyrosine phosphorylation but also enhances ubiquitinylation and accelerates endocytosis and subsequent intracellular destruction of ErbB-2 molecules. (lclabs.com)
Regulation of proteins through post-translational modifications, including reversible phosphorylation and ubiquitylation. (dundee.ac.uk)
From this, we have identified a handful of novel kinases that appear to either inhibit or activate TGFβ and BMP signalling, downstream of SMAD phosphorylation. (dundee.ac.uk)

The degradative pathway of ErbB receptor tyrosine kinases stimulated by tyrosine kinase inhibitors appears to be chaperone mediated, and thus is similar to the pathways activated by the heat shock protein 90 (Hsp90) antagonist geldanamycin and by stress-induced mechanisms. (lclabs.com)
Alternative inhibitory receptors have been identified that may be targeted for anti-tumor immune therapy, such as lymphocyte-activation gene-3 (LAG-3), as have several potential target oncogenes for molecularly targeted therapy, such as tyrosine kinase inhibitors. (biomedcentral.com)
Several oncogenes have been identified as potential targets for molecularly targeted melanoma therapy, such as tyrosine kinase inhibitors (TKIs). (biomedcentral.com)

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM. (abmole.com)
Erastin2 is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter. (abmole.com)
IFSP1 is an effective, selective and glutathione-independent inhibitor of ferroptosis Suppressor protein 1 (FSP1/AIFM2) with an EC50 value of 103 nM. (abmole.com)
It is also a potent, selective, and metabolically stable system XC -- inhibitor. (abmole.com)
UAMC-3203 hydrochloride is a potent and selective Ferroptosis inhibitor, with an IC50 of 12 nM. (abmole.com)
PD 146176 is a selective 15-lipoxygenase inhibitor. (abmole.com)
Here we show that pharmacological stimulation of 5-HT7R using a highly selective agonist, LP-211, enhances neurite outgrowth in neuronal primary cultures from the cortex, hippocampus and striatal complex of embryonic mouse brain, through multiple signal transduction pathways. (cirn-na.com)
Alfy, the human homologue of Drosophila blue cheese, is involved in the selective disposal of ubiquitinated protein aggregates. (adenosine-kinase.com)
Fusion incompetent COX-1 Inhibitor Source mitochondrial organelles are then removed by selective autophagy [251]. (adenosine-kinase.com)
Given the numerous degrees of mitochondrial protein turnover impairment in response to a deficit in either proteasom- associated variables or selective autophagy regulators, two theories try to pinpoint the pathways involved in mitophagy. (adenosine-kinase.com)
Oncothyreon Inc (ONTY) on April 19, 2016 announced the presentation of data highlighting the preclinical development of orally bioavailable, potent and selective checkpoint kinase 1 (Chk1) inhibitors. (broadstreetalerts.com)
Using robust endogenously driven BMP and TGFβ reporter cells (Rojas-Fernandez et al, 2015) that we have generated using CRISPR/Cas9, we have undertaken a chemical screen using highly potent and selective kinase inhibitors. (dundee.ac.uk)
Deletion of AMPKα1 or AMPKα2 resulted in activation of STAT1 and in increases in proinflammatory mediators, both of which were attenuated by administration of STAT1 small interfering RNA or fludarabine, a selective STAT1 inhibitor. (diabetesjournals.org)

Induces upregulation of the pluripotency network genes (Klf4, Klf2, Nanog, Oct4, Myc, Sox2) and epigenetic-associated proteins (Dnmt3a, Mbd3) in mouse ES cells, and inhibits retinoic acid-induced differentiation (Adamo et al. (stemcell.com)
It selectively inhibits erbB1 (epidermal growth factor receptor), erbB2, erbB3, and erbB4 without blocking tyrosine kinase activity of many other receptors such as platelet-derived growth factor receptor, fibroblast growth factor receptor, and insulin receptor. (lclabs.com)
Trouw L., Nilsson S., Goncalvez I., Landberg G. and Blom A. M. (2005) C4b-binding protein binds to necrotic cells and DNA, which limits DNA release and inhibits complement activation. (lu.se)

The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase (RTK) commonly targeted for inhibition by anti-cancer therapeutics. (biorxiv.org)
The epidermal growth factor receptor (EGFR) is a HER-family receptor tyrosine kinase (RTK) that is involved in cell signaling in healthy tissue. (biorxiv.org)

The Type II receptor phosphorylates serine residues of the Type I receptor, which activates the protein. (wikipedia.org)
Next, we observed that Acanthamoeba specifically activates phosphatidylinositol 3-kinase. (asm.org)
AICAR is an adenosine analog that selectively activates AMP-activated protein kinase (AMPK). (stemcell.com)

More specifically, substrates with certain FYVE domains (named after the first four proteins in this motif, Fab1, YotB, Vac1p, and EEA1) bind PIP, and these pathways have been implicated in vesicular trafficking or receptor-mediated endocytosis ( 5 ). (asm.org)
Transforming Growth Factor β (TGFβ), Bone Morphogenetic Protein (BMP) and Wnt signalling pathways. (dundee.ac.uk)
Nearly 60% of genetic alterations have been found in AML patients involve in signaling pathways including signaling of tyrosine kinase receptor FLT3. (lu.se)
Our results show that SLAP2 suppresses FLT3 downstream signaling pathways including AKT, ERK, p38 and STAT5 and facilitates FLT3 degradation through enhancing ubiquitination while ABL2 expression does not alter FLT3 stability or ubiquitination but partially suppresses FLT3 downstream signaling through the PI3K/AKT pathway. (lu.se)
Effector proteins are then recruited to activate various cellular signaling pathways, including RAS/RAF/MEK, PI3K/AKT/mTOR, and JAK/STAT ( 1 ). (biorxiv.org)
What pathways are this gene/protein implicaed in? (cancerindex.org)

These receptors are serine/threonine kinase receptors. (wikipedia.org)
The binding of a TGFβ family ligand causes the rotation of the receptors so that their cytoplasmic kinase domains are arranged in a catalytically favorable orientation. (wikipedia.org)
Moreover, we found that the interaction between the same glycan and different protein receptors within the same rotavirus genogroup influenced the micro-level dynamics of the glycan. (bvsalud.org)
Temporal elevations in glucocorticoid levels enhance the extracellular release of ATP in the spinal cord, which stimulates purinergic receptors on microglia in the dorsal horn. (nature.com)
Cannabinoids exert many of their effects through activation of G i -protein-coupled receptors. (jneurosci.org)
Both D1 and D2 dopamine receptors also couple to adenylate cyclase via G-proteins. (jneurosci.org)
whereas dopamine D2 receptors inhibit adenylate cyclase via G i -proteins ( Sibley and Monsma, 1992 ). (jneurosci.org)
The diversified effects of cannabinoids are now known to be mediated through the activation of G-protein-coupled receptors that are normally bound by a family of endogenous ligands, the endocannabinoids ( 1 ). (aacrjournals.org)
DDR1, also known as CAK, CD167a, RTK6, and TrkE, is a 120-140 kDa type I transmembrane glycoprotein that belongs to the discoidin-like domain containing subfamily of receptor tyrosine kinases and serve as receptors for collagen. (rndsystems.com)
These include the T cell immunoglobulin and mucin-domain containing-3 (TIM-3), lymphocyte-activation gene-3 (LAG-3), TIGIT, and B-and T-lymphocyte-associated protein (BTLA) receptors associated with T cell exhaustion and V-domain immunoglobulin suppressor of T cell activation (VISTA), a receptor found on tumor-infiltrating myeloid cells. (biomedcentral.com)

MST1R (RON) is a trans-membrane receptor tyrosine kinase (RTK), which is part of the c-MET proto-oncogene family. (frontiersin.org)

RC subunit turnover was also selectively impaired in PINK1 mutants [264]. (adenosine-kinase.com)
This kinase is a catalytic subunit of the protein kinase complex that is important for cell cycle G1 phase progression and G1/S transition. (cancerindex.org)
Kask L., Hillarp A., Ramesh B., Dahlbäck B., and Blom A. M. (2002) Structural requirements for the intra-cellular subunit polymerization of the complement inhibitor C4b-binding protein. (lu.se)

Therapeutic Candidate or Device Rebecsinib is a novel small molecule inhibitor of ADAR1 splicing that selectively eradicates therapy-resistant cancer stem cells in blood cancers. (ca.gov)
Targeting this pathway with a small molecule inhibitor, LCRF-0004, resulted in decreased proliferation with a concomitant increase in apoptosis. (frontiersin.org)

Activating LRRK2 mutations cause Parkinson's disease, and pathogenic LRRK2 kinase interferes with ciliogenesis. (elifesciences.org)
Activating mutations in the Leucine Rich Repeat Kinase 2 (LRRK2) cause Parkinson's disease and previously we showed that activated LRRK2 phosphorylates a subset of Rab GTPases (Steger et al. (stanford.edu)

Molecular 'switch' reverses chronic inflammation and aging - Science Daily, 2/6/20 - 'By studying mice and immune cells called macrophages, the team found that a protein called SIRT2 is responsible for deacetylating the NLRP3 inflammasome. (qualitycounts.com)
The molecular chaperone glucose-regulated protein 78 ( GRP78 ) or binding immunoglobulin protein (BiP), in addition to Ca 2+ binding and protein processing functions, possesses one more key role: master initiator of early UPR signaling. (molvis.org)
Subsequently, the effect of an additional small molecular inhibitor, BMS-777607 (which targets MST1R (RON), MET, Tyro3, and Axl) also resulted in a decreased proliferative capacity of MPM cells. (frontiersin.org)
The long term goal of our research is to elucidate the molecular mechanisms by which proteins are targeted to specific and distinct compartments. (stanford.edu)
We are combining the rapid genome editing capability afforded by CRISPR/Cas9 with advanced knowledge of protein chemistry to engineer robust molecular tools capable of selectively targeting individual proteins for desired functional modulation in cells. (dundee.ac.uk)
Based on our identified miRNA-regulated molecular machinery, an inhibitor of PDK1/Akt BX-912, an anthracycline antibiotic daunorubicin, and a multi-targeted protein kinase inhibitor midostaurin were discovered as potential repositioning drugs for treating lung cancer. (cdc.gov)
Mark L., Lee W. H., Villoutreix B. O., Proctor D., Blackbourn, D., Spiller B. O. and Blom A. M. (2004) KSHV complement control protein mimics human molecular mechanisms for inhibition of the complement system. (lu.se)

BKIs inhibit the apicomplexan calcium-dependent protein kinase 1 (CDPK1) selectively due to the small gatekeeper residue in the CDPK1 ATP binding site that allows the BKI access, while larger residues in mammalian kinases block BKIs from binding [5]. (iassist2012.org)
RSL3 is an inhibitor of the glutathione (GSH) peroxidase 4, and a ferroptosis activator, which can inhibit the cysteine/glutamate amino acid transporter system. (abmole.com)
Using protein stability shift assays, we identified a family of imidazo[1,2-b]pyridazines to specifically interact with and inhibit PIM kinases with low nanomolar potency. (ox.ac.uk)
Cannabinoids act at the CB1 receptor to inhibit adenylate cyclase activity via a pertussis toxin-sensitive G-protein. (jneurosci.org)

GCV, a kind of antiviral drug, can be phosphorylated by HSVtK protein finally into triphosphates, which are potent inhibitors of DNA polymerase, leading to the disruption of cellular DNA synthesis and ultimately cell death. (biomedcentral.com)
As we all know, the kinase plays a role in signaling cascade, regulates cellular responses to cytokines and stress. (cancer-research-network.com)
We aim to understand how the DUF1669 domain controls the function of the FAM83 family of proteins in their potentially diverse cellular roles. (dundee.ac.uk)

Receptor-interacting protein kinase 1 (RIPK1) is a key component of the tumor necrosis factor (TNF) receptor signaling complex that regulates both pro- and anti-apoptotic signaling. (mdpi.com)
It has been reported that RNF4 negatively regulates TNF-α-induced activation of the nuclear factor-κB (NF-κB) through downregulation of transforming growth factor β-activated kinase 1 (TAK1) activity, indicating the possibility that RNF4-mediated TAK1 suppression results in enhanced sensitivity to cell death. (mdpi.com)

Two such proteins that mediate the TGFβ pathway include SARA (the SMAD anchor for receptor activation) and HGS (Hepatocyte growth factor-regulated tyrosine kinase substrate). (wikipedia.org)
It differs from other enzyme subtypes in that it lacks a phosphorylatable activation domain that can respond to CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE KINASE. (curehunter.com)
Once p38 MAPK activation occurs in muscle stem cells, it enhances muscle regeneration. (cancer-research-network.com)
Treatment of the pertussis toxin-treated cells with cholera toxin before CB1 receptor activation amplified the stimulatory pathway, suggesting that this response was mediated through a G s -type G-protein. (jneurosci.org)
As a single agent, Chk1 inhibitors may selectively target cancer cells that have high replication stress, which can be caused by activation of oncogenic signaling and loss of tumor suppressor functions. (broadstreetalerts.com)
AIM AND STUDY: This study aims to investigate the antifibrotic mechanism of FZHY treatment by exploring its effects on the activation of NOD-like receptor protein 3 (NLRP3) inflammasome in macrophages. (bvsalud.org)
RESULTS: FZHY treatment resulted in the downregulation of NLRP3 protein expression and inhibition of its priming and activation in both human fibrotic livers and DDC-induced liver fibrosis. (bvsalud.org)
A feed-forward pathway drives LRRK2 kinase membrane recruitment and activation. (stanford.edu)
In contrast to the case of many kinases, we have found that the activation loop of FLT3 is not essential for its activation. (lu.se)
Using a panel of kinase inhibitors, we found ALK inhibitor AZD3463 selectively inhibited the activation and downstream signaling of FLT3-ITD and did not affect the wild-type FLT3 (FLT3-WT). (lu.se)
We also synthesize a library consisting of 70,290 guides targeting all human RefSeq coding isoforms to screen for genes which, upon activation, confer resistance to a BRAF inhibitor. (cdc.gov)
Cas9 nuclease can be converted into an RNA-guided DNA binding protein (dCas9) via inactivation of its two catalytic domains 12 , 13 and then fused to transcription activation domains. (cdc.gov)
Sjöberg A., Trouw L., McGrath F., Hack E. C. and Blom A. M. (2006) Regulation of complement activation by C-reactive protein: targeting of the inhibitory activity of C4b-binding protein. (lu.se)

DL-Buthionine-(S,R)-sulfoximine is a potent inhibitor of glutamylcysteine synthetase biosynthesis . (abmole.com)
SRS16-86 is a potent inhibitor of ferroptosis. (abmole.com)
Liproxstatin-1 is a potent inhibitor of ferroptosis, a non-apoptotic form of cell death characterized by iron-dependent accumulation of lethal lipid reactive oxygen species (ROS). (abmole.com)
Ritonavir is a potent inhibitor of CYP3A4- and CYP2D6- mediated drug metabolism. (who.int)

Because BRCA mutations are observed in fewer than 10% of cancer patients (cBioPortal: 6.7%) 11 , 12 , 13 the identification of additional genes that share synthetic lethal sensitivity relationships with mutated oncogenes or tumor suppressors would greatly enhance the implementation of tumor cell-specific synthetic lethal sensitivity to improve an anticancer therapeutic response. (nature.com)
Because most tumors are deficient in one or more aspects of the function of the p53 tumor suppressor, either as a consequence of mutations within p53, or impairment of upstream and downstream modulators of p53 activity 19 , targeting MK2 has the potential to selectively enhance tumor cell killing without increasing the genotoxic effects of chemotherapy on normal p53-wild type tissues. (nature.com)
Scope includes mutations and abnormal protein expression. (cancerindex.org)
Blom A. M. , Villoutreix B. O, and Dahlbäck B. (2003) Mutations in a-chain of C4BP that selectively affect its Factor I cofactor function. (lu.se)

The protein encoded by this gene is a member of the CMGC family of serine/threonine protein kinases. (cancerindex.org)

In response to DNA damage, a synthetic lethal relationship exists between the cell cycle checkpoint kinase MK2 and the tumor suppressor p53. (nature.com)
Therefore, compared to normal p53-proficient cells, p53-defective cells are more reliant on MK2 activity, which drives an alternative cell cycle checkpoint pathway that stabilizes the CKI inhibitors p27 Kip1 and Gadd45α in order to maintain G 1 /S and G 2 /M arrest after certain types of DNA damage 16 , 18 . (nature.com)
More specifically, data from our CAN-2409 clinical trial demonstrated robust evidence of local and systemic anti-tumor activity in patients with non-small cell lung cancer who had an inadequate response to immune checkpoint inhibitors. (tmcnet.com)
The data demonstrated evidence of local and systemic anti-tumor activity in patients with inadequate response to previous immune checkpoint inhibitor (ICI) treatment and showed a disease control rate of 77 percent (20/26) in patients entering the trial with disease progression despite ICI treatment. (tmcnet.com)
Combinations of these checkpoint therapies with other agents are now being explored to improve outcomes and enhance benefit-risk profiles of treatment. (biomedcentral.com)
The benefit of dual checkpoint blockade with anti CTLA-4 and anti PD-1 inhibitor over monotherapy with a CTLA-4 inhibitor has been shown, with durable disease control and improved overall survival (OS). (biomedcentral.com)

The concept has now been extended to embrace synthetic lethal drug sensitivity, such as that observed with PARP inhibitors in combination with DNA-damaging chemotherapy in a variety of BRCA defective tumors 10 . (nature.com)
The Warburg phenotype provides tumors an enhanced resistance against cytotoxic insults. (springer.com)
Throughout the year, we presented encouraging data, expanded our leadership team, and announced a partnership with the University of Pennsylvania, leveraging Candel's enLIGHTEN™ Discovery Platform to create novel viral immunotherapies to enhance CAR-T cell therapies in solid tumors. (tmcnet.com)
However, these types of inhibitors are not specific for tumors over healthy tissue and therefore cause undesirable side effects. (biorxiv.org)

The system is based on the interaction between the tetracycline-responsive element (TRE), consisting of seven copies of the prokaryotic tetracycline operator site (tetO) fused to a cytomegalovirus minimal promoter region, and the reverse tetracycline-transactivator (rtTA), consisting of the prokaryotic tetracycline repressor protein (TetR) fused to the activator domain of the herpes simplex virus VP16 protein. (biomedcentral.com)
Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
The metabolic abnormalities of type 2 diabetes, including hyperglycemia, dyslipidemia, and insulin resistance, activate the Janus kinases/signal transducer and activator of transcription (JAK/STAT) signaling pathway, a major intracellular inflammatory cascade that transmits the intracellular signaling to the nucleus ( 2 ), promoting inflammatory response, inducing insulin resistance ( 3 ), and accelerating the development of cardiovascular complications ( 4 ). (diabetesjournals.org)
Among the established custom DNA binding domains, Cas9 is most easily scaled to facilitate genome-scale perturbations 3 , 4 due to its simplicity of programming relative to zinc finger proteins and transcription activator-like effectors (TALEs). (cdc.gov)

Affinity-directed PROtein Missile (AdPROM) system (Fulcher et al, 2016) for targeted proteolysis of proteins of interest is an example of the type of technologies we want to develop and exploit. (dundee.ac.uk)

Additionally, we observed crucial TMPK dynamics brought on by ligand-binding and identified key residues such as Phe68 and Tyr101 as the critical points of the protein-ligand interaction. (bvsalud.org)
The ligand-bound TM configuration promotes asymmetric dimerization of the intracellular juxta-membrane (JM) and kinase domains, which causes autophosphorylation of intracellular tyrosine residues ( 6 , 7 ). (biorxiv.org)

The potency of these BKIs is related to hydrophobic interactions between the distal 2-cyclopropyloxy group and the N-terminal lobe of the inhibition [18], (RH strain) expressing a yellow fluorescent protein. (iassist2012.org)

By inhibiting PIKFYVE activity, it induces exosomal secretion, which robustly clears misfolded proteins including C9ORF72 dipeptide repeat proteins (DPRs), TDP-43 and tau from neurons. (ca.gov)
The bumped kinase inhibitor (BKI) class of compounds has broad activity against apicomplexan pathogens including and [4]. (iassist2012.org)
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. (ox.ac.uk)
Our lab has recently developed a new strategy to regulate RTK activity by designing a peptide that specifically binds to the transmembrane (TM) region of the RTK to allosterically modify kinase activity. (biorxiv.org)
The activity of this kinase first appears in mid-G1 phase, which is controlled by the regulatory subunits including D-type cyclins and members of INK4 family of CDK inhibitors. (cancerindex.org)
This kinase, as well as CDK4, has been shown to phosphorylate, and thus regulate the activity of, tumor suppressor protein Rb. (cancerindex.org)

Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo. (lclabs.com)

ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor that induces iron death and has shown cytotoxic effects against melanoma, lung adenocarcinoma, fibrosarcoma, and pancreatic cancer cell lines. (abmole.com)
Moreover, the PSN analysis revealed that the interaction with ligand induces changes in residual network properties, enhancing the stability of complexes. (bvsalud.org)

Unlike replication of many Escherichia coli plasmids, replication of cyanobacterial plasmids did not require added ATP, was not inhibited by omission of the ribonucleotides, and was insensitive to the RNA polymerase inhibitor rifampicin and the gyrase inhibitor novobiocin, but was inhibited by ethidium bromide. (upenn.edu)

Bone morphogenetic proteins cause the transcription of mRNAs involved in osteogenesis, neurogenesis, and ventral mesoderm specification. (wikipedia.org)
Glycogen synthase kinase 3β (GSK-3β) represses cell cycle progression by directly phosphorylating cyclin D1 and indirectly regulating cyclin D1 transcription by inhibiting Wnt signaling. (elsevierpure.com)
The encoded protein can activate transcription through pyrimidine-rich initiator (Inr) elements and E-box motifs. (cancerindex.org)
Programmable DNA binding proteins have emerged as an exciting platform for engineering synthetic transcription factors for modulating endogenous gene expression 5 - 11 . (cdc.gov)

Therapeutic Candidate or Device AS-202, an antisense oligonucleotide Indication Amyotrophic Lateral Sclerosis Therapeutic Mechanism AS-202 targets PIKFYVE, a lipid kinase. (ca.gov)

5 Conversely, p53 induction by oxidative damage may help reduce the development of atherosclerosis, perhaps by suppressing the growth or enhancing the death of cells involved in causing atherosclerotic lesions. (the-scientist.com)
Cancer cells that are defective in p53 function are deficient in their ability to transcriptionally upregulate the CDK inhibitor p21 after genotoxic stress. (nature.com)
Given that protein aggregates in liver cells are closely linked to alcoholic liver disease, these findings suggest that quercetin could be a useful treatment for patients with this condition. (qualitycounts.com)
IFSP1 can selectively induce iron death in Pfa1 cells and HT1080 cells with GPX4 knockout gene overexpressing FSP1. (abmole.com)
UAMC-3203 is an improved ferroptosis inhibitor, with an IC50 value of 10 nM in IMR-32 neuroblastoma cells. (abmole.com)
JKE-1674 reduces viability of LOX-IMVI cancer cells and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1. (abmole.com)
In the GSK-3β +/+ but not the GSK-3β -/- cells, Epm2a small interfering RNA significantly enhanced cell growth. (elsevierpure.com)
Inhibitors of GSK-3β selectively increased the cell growth of Epm2a +/+ but not of Epm2a -/- cells. (elsevierpure.com)
These results were further confirmed using brain microvascular endothelial cells expressing dominant negative forms of phosphatidylinositol 3-kinase. (asm.org)
Acanthamoeba binding to HBMEC is mediated by a mannose-binding protein expressed on the surface of Acanthamoeba cells ( 2 ). (asm.org)
As an emerging cancer immunotherapy, oncolytic virotherapies (OVTs) can not only selectively lyse cancer cells, but also induce a systemic antitumor immune response. (frontiersin.org)
Protein expression and function of organic anion transporters in short-term and long-term cultures of Huh7 human hepatoma cells. (cancerindex.org)
Chk1 is a protein kinase that plays a major role in the ability of cancer cells to respond to DNA damage and DNA replication stress. (broadstreetalerts.com)
The primary barriers for invading respiratory pathogens are the respiratory tract epithelial cells and antimicrobial proteins generated by these cells. (cdc.gov)
Pertoft H. and Fries E. (1995) Inter-a-inhibitor is required for the formation of the hyaluronan-containing coat on fibroblasts and mesothelial cells. (lu.se)

Much attention has recently been focused on PIM kinases as potential targets for the treatment of hematopoietic malignancies and some solid cancers. (ox.ac.uk)

Current therapeutics target EGFR's kinase domain or extracellular region. (biorxiv.org)

Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. (lclabs.com)

PAWS1 is a member of the poorly characterised FAM83 family of proteins that are linked through the conserved DUF1669 domain of unknown function, which possesses a pseudo-Phospholipase D catalytic motif. (dundee.ac.uk)

Here, we describe the concept of augmented synthetic lethality (ASL): depletion of a third gene product enhances a pre-existing synthetic lethal combination. (nature.com)
The more widely used suicide gene system is the herpes simplex virus thymidine kinase/ganciclovir (HSVtK/GCV). (biomedcentral.com)
We found that sorafenib may act as a histone deacetylase (HDAC) inhibitor based on similar gene expression profiles. (oncotarget.com)
Ction mutation in Drosophila blue cheese gene (bchs) outcomes in an age-dependent accumulation of ubiquitinated protein aggregates and amyloid precursor-like proteins and reduces life span. (adenosine-kinase.com)
What does this gene/protein do? (cancerindex.org)

Chk1 inhibitors may also be used in combination with chemotherapy, potentially enhancing cell death and increasing the efficacy of these agents. (broadstreetalerts.com)
Our results suggest that SLAP2 and ABL2 regulate FLT3 signaling and modulation of SLAP2 expression levels or targeting ABL2 could potentially synergize with FLT3 inhibitors to treat FLT3-ITD positive AML. (lu.se)

Here, we screened 32409 compounds against thymidylate kinase (TMPK), an emerging target for Mpox treatment. (bvsalud.org)

All round mitochondrial protein turnover in parkin null Drosophila was related to that in Atg7 deficient mutants. (adenosine-kinase.com)
Two additional kinase deficient splice forms are expressed in colon cancer. (rndsystems.com)

Accumulation of unfolded proteins in the ER lumen triggers the dissociation of GRP78 from its quiescent UPR mediators. (molvis.org)
Norepinephrine transporter, organic cation transporters, and multidrug and toxin extrusion proteins play differential roles in tumor targeting, systemic elimination, and accumulation in normal tissues. (aspetjournals.org)

Although different liposomal formulations have been administered Inhibitors,research,lifescience,medical to humans without toxicity [9], the in vivo tolerability of liposomes continues to be investigated. (inhibitorlibraries.com)
We also study the NPC1 protein that is essential for cholesterol transport in humans and can lead to Niemann Pick C disease when mutated. (stanford.edu)

SGK-1 protein levels in spinal astrocytes are increased in response to glucocorticoid stimuli and enhanced ATP release by opening the pannexin-1 hemichannels. (nature.com)

The concept of synthetic lethality (SL) holds great promise for the treatment of human cancers, best exemplified by the now widespread use of PARP inhibitors in BRCA mutant cancers. (nature.com)

A formulation of bupivacaine that provides prolonged release of the active ingredient after a single administration Inhibitors,research,lifescience,medical would simplify pain management in the postoperative period and eliminate the undesired peak plasma concentrations as a result of Inhibitors,research,lifescience,medical excessively high concentrations and reduce the risk of local and systemic reactions [7]. (inhibitorlibraries.com)

Although several FLT3 inhibitors have been developed and showed promising results in clinical trials, many patients develop drug resistance shortly after treatment starts and display poor outcome. (lu.se)

A single injection of local anesthetic around the brachial plexus nerve bundle results in block of arm selleck chemical Seliciclib tissue innervated Inhibitors,research,lifescience,medical by selleck chem inhibitor several peripheral nerves. (inhibitorlibraries.com)

Pansensitive and panresistant genes to 21 NCCN-recommended drugs with concordant mRNA and protein expression were identified. (cdc.gov)

It may also hold promise for treatment of other diseases associated with protein aggregation, such as Alzheimer's' - See quercetin at Amazon.com and iHerb . (qualitycounts.com)

We also assessed the development of obesity-induced inflammation by measuring hippocampal level of TNF-alpha, and the extent of protein oxidation by titrating nitro-tyrosine (N-Tyr). (cirn-na.com)
0.01), inflammation and protein oxidative modification, as evidenced by the increase in the concentration of TNF-alpha and nitro-tyrosine. (cirn-na.com)

In particular, human organic cation transporter 2 (hOCT2) and multidrug and toxin extrusion proteins 1 and 2-K (hMATE1/2-K) likely mediate renal secretion of mIBG, whereas hOCT1 and hOCT3 may contribute to mIBG uptake into normal tissues such as the liver, salivary glands, and heart. (aspetjournals.org)

A multifunctional calcium-calmodulin-dependent protein kinase subtype that occurs as an oligomeric protein comprised of twelve subunits. (curehunter.com)
At this time, it seems clear that delayed frontal lobe metabolic maturation occurs in autism,146 which may be related Inhibitors,research,lifescience,medical to some of the early repetitive behaviors. (inhibitorlibraries.com)

Strikingly, once phosphorylated, Rab GTPases switch their preference and bind to new sets of phospho-specific protein effectors. (elifesciences.org)

Anatomy16

Organisms7

Chemicals and Drugs172

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Phenomena and Processes42

Disciplines and Occupations1

Information Science3

Mitogen-activa2

Phosphorylation10

Tyrosine kinase inh3

Selective13

Inhibits3

Epidermal growth f2

Activates3

Pathways6

Receptors10

Receptor tyrosi1

Subunit3

Small molecule inhibitor2

Cause Parkinson's disease2

Molecular7

Inhibit4

Cellular3

Regulates2

Activation13

Potent inhibitor4

Mutations4

Serine1

Checkpoint6

Tumors4

Activator4

20161

Residues2

Inhibition1

Activity6

Vitro1

Induces2

Polymerase1

Transcription4

Lipid1

Cells15

Targets1

Extracellular1

Degradation1

Catalytic1

Gene5

Potentially2

Compounds1

Deficient2

Accumulation2

Humans2

Stimuli1

Cancers1

Systemic1

Resistance1

Peripheral1

Genes1

Treatment1

Inflammation2

Mediate1

Occurs2

Effectors1