• Neurotensin receptor type 2 is a protein that in humans is encoded by the NTSR2 gene. (wikipedia.org)
  • Endogenous RPTPkappa associated with EGF receptor and HER2, resulting in suppression of basal and ErbB ligand-induced proliferation and receptor phosphorylation. (nih.gov)
  • Two cannabinoid receptors have been characterized and cloned from mammalian tissues: the "central" CB 1 receptor and the "peripheral" CB 2 receptor. (aacrjournals.org)
  • Using T cell hybridomas express- ing either a wild-type TCR or an -CPM mutant, we show that Fyn fails to be activated by the mutant receptor follow- ing SEB binding and fails to generate tyrosine-phospho- rylated Pyk2, a member of the focal adhesion kinase family. (unisi.it)
  • Characterization of the brain penetrant neuropeptide Y Y 2 receptor antagonist SF-11. (rndsystems.com)
  • The ArfGAP paxillin kinase linker (PKL)/G protein-coupled receptor kinase-interacting protein (GIT)2 continues to be implicated in regulating cell spreading and motility through its transient recruitment of the p21-activated kinase (PAK) to focal adhesions. (healthyguide.info)
  • RESULTS Identification of a 95-kDa Tyrosine Phosphorylated Nck-binding Protein The SH3-SH3-SH3-SH2 adaptor protein Nck is a major downstream mediator of extracellular matrix and growth element receptor signaling to the cytoskeleton through its ability to associate with receptor tyrosine kinases PAK and the WASP/WAVE complex (Buday and indicated like a Box-and-Whiskers Storyline (Number 10B). (healthyguide.info)
  • The tyrosine kinase Src is a member of a family of related kinases known as the Src family kinases (SFKs) that share a common structural organization and function as key regulators of signal transduction pathways triggered by a wide variety of surface receptors, including receptor tyrosine kinases, integrins, G-protein-coupled receptors, and antigen receptors (Thomas and Brugge 1997). (mdm2-receptor.com)
  • Integrin-mediated RON growth factor receptor phosphorylation requires tyrosine kinase activity of both the receptor and c-Src. (123dok.org)
  • Integrin-in-duced epidermal growth factor (EGF) and platelet-derived growth factor (PDGF) RTK phosphorylation depends on the kinase activity of the receptor (7, 13). (123dok.org)
  • The GDNF family ligands (GFLs) function through a glycosyl-phosphatidylinositol-(GPI) anchored coreceptor, GDNF family receptor alpha (GFRα), and rearranged during transfection (RET), a well-known receptor tyrosine kinase involved in kidney development, spermatogonial stem cell maintenance, and the development and maintenance of the sympathetic, parasympathetic, and enteric nervous systems [ 1 , 2 ]. (medsci.org)
  • Since tyrphostin is known to inhibit polypeptide receptor tyrosine kinases and inhibits neuropeptide stimulated mitogenesis, the effect of tyrphostin with or without SP analogues was tested on SCLC growth in vitro. (ucl.ac.uk)
  • Focal adhesion kinase (FAK) is a key integrator of integrin-mediated signals from the extracellular matrix to the cytoskeleton and downstream signaling molecules. (techscience.com)
  • In addition, phosphorylation of other Tyr residues (Tyr-925, and Tyr-861) creates binding sites for SH2 domains of intracellular signaling molecules such as Src, PI3 kinase, and Grb2. (fishersci.com)
  • Significant reductions in the phosphorylation of signaling molecules focal adhesion kinase, extracellular signal-regulated kinases 1 and 2, and v-Akt murine thymoma viral oncogene were observed in male MIPβ1KO islets when compared to controls. (oncotarget.com)
  • FAK is activated by phosphorylation at specific tyrosine residues, which then stimulate downstream signaling including the ERK1/2 pathway, leading to a variety of cellular responses. (techscience.com)
  • NCAM based signaling complexes can initiate downstream intracellular signals by at least two mechanisms: (1) activation of FGFR and (2) formation of intracellular signaling complexes by direct interaction with cytoplasmic interaction partners such as Fyn and FAK. (uni-freiburg.de)
  • The activation of ERBB2, ERBB3 and the downstream modulators focal adhesion kinase and SHC were activated in cells with overexpression of BCAR4. (eur.nl)
  • Surprisingly, phosphorylation of the canonical downstream targets Akt and GSK3β is unaffected following ILK loss. (jneurosci.org)
  • We conclude that a Src/ FAK signaling unit inhibits differentiation to promote tumorigenesis downstream of β1 integrin and independent of βintegrin tyrosine phosphorylation. (iucc.ac.il)
  • Western blot analysis was conducted, which indicated that SKLB1002 inhibited VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal-regulated kinase, focal adhesion kinase, and Src. (medkoo.com)
  • Engagement of course I substances byHLA antibodies stimulates phosphorylation of protein kinases Src, focal adhesionkinase (FAK), and paxillin and set up of focal adhesions and activation from the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB/Akt) pathway (27-29). (cgp60474.com)
  • PKL is definitely phosphorylated on tyrosine residues 286/392/592 by Src and/or FAK and these sites are required for PKL localization to focal adhesions and for paxillin binding. (healthyguide.info)
  • Overexpression of the nonphosphorylated GFP-PKL Triple YF mutant stimulates cell distributing and protrusiveness much like overexpression of a paxillin mutant that does not bind PKL suggesting that failure to recruit PKL to focal adhesions interferes with normal cell distributing and motility. (healthyguide.info)
  • A) Normal MEF cells were transfected and plated on 5 μg/ml fibronectin for 180 min followed by acquisition of time-lapse images every … DISCUSSION We have recognized Src/FAK- and Rac-dependent phosphorylation of the ArfGAP PKL and identified that phosphorylation is required for PKL focal adhesion localization paxillin binding and normal cell adhesion dynamics. (healthyguide.info)
  • This thesis shows that the non-hydrolyzable GTP analogue, GTP?S, induced tyrosine phosphorylation of multiple proteins including the focal adhesion associated proteins p125 focal adhesion kinase and paxillin in permeabilized Swiss 3T3 cells. (ucl.ac.uk)
  • In MCF10A/HER2 cells, TGF-beta enhanced cell motility, FAK phosphorylation, F-actin assembly, and focal adhesion formation and inhibited RhoA activity. (nih.gov)
  • Surprisingly, phosphorylation of CasSD was independent of myosin contractile activity but dependent on actin polymerization. (utmb.edu)
  • Furthermore, we found that CasSD phosphorylation in the early stages of cell spreading required: (1) integrin anchorage and integrin-mediated activation of SFKs, (2) association of Cas with focal adhesion kinase (FAK), and (3) N-WASP-driven actin-assembly activity. (utmb.edu)
  • Thus, extension of the leading edge mediated by actin polymerization could stretch Cas during early cell spreading, priming it for phosphorylation. (utmb.edu)
  • ILK forms an obligate heterotrimeric complex with particularly interesting Cys-His-rich protein (PINCH) and parvin, which together lend stability to the actin cytoskeleton at focal adhesions ( Brakebusch and Fässler, 2003 ). (jneurosci.org)
  • PubMed]Murata-Hori M, Fukuta Y, Ueda K, Iwasaki T, Hosoya H. HeLa Squat kinase induces diphosphorylation of myosin II regulatory light chain and reorganization of actin filaments in nonmuscle cells. (opioid-receptors.com)
  • Epithelial cells adjacent to the area of the defect flatten, lose their hemidesmosome attachments, and migrate on transient focal contact zones that are formed between cytoplasmic actin filaments and extracellular matrix proteins. (medscape.com)
  • Mechanistic studies showed that MWCNTs induced fibrogenesis of NHLFs through promoting expression and phosphorylation of focal adhesion kinase (FAK), while attenuating intracellular tension in the cells on stiff gels could increase MWCNTs uptake and thus elevate the induced fibrogenic responses. (cdc.gov)
  • β1 integrin is the major β integrin subunit in pancreatic beta-cells and forms heterodimers with 12 α integrin subunits, which interact with components of the extracellular matrix (ECM) to control intracellular signaling via the focal adhesion kinase (FAK) and extracellular signal related kinase 1 and 2 (ERK1/2) pathways [ 4 ]. (oncotarget.com)
  • These features of HLA course II have already been shown to employ several intracellular signaling occasions, in antigen delivering cells through agonistic activities after engagement by T cell receptors, including activation of protein kinases Src, Syk, PKC, the mitogen turned on kinase (MAPK) p38, and ERK (36, 38). (cgp60474.com)
  • Having performed a kinase inhibitor library screening in macrophages, here we identify protein-tyrosine kinase 2-beta (PTK2B/PYK2) as a putative IRF5 kinase. (ox.ac.uk)
  • When T98G cells were incubated with wortmannin, a PI 3-kinase inhibitor, both PI 3-kinase activity and phosphorylation of Akt were inhibited, whereas apoptosis by oxidative stress was accelerated. (elsevierpure.com)
  • U0126 is a potent and selective non-competitive inhibitor of MAP kinase kinase. (rndsystems.com)
  • Identification of a novel inhibitor of mitogen-activated protein kinase kinase. (rndsystems.com)
  • Intravenous administraton of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. (rndsystems.com)
  • Bosutinib (SKI-606) is a 4-anilino-3-quinoline carbonitrile, which acts as a dual inhibitor of Src and ABL kinases. (mdm2-receptor.com)
  • Interestingly, distinctly lower concentrations of bosutinib are required to ablate BCR-ABL phosphorylation when compared to the first-generation tyrosine kinase inhibitor imatinib (IM). (mdm2-receptor.com)
  • Bosutinib has the potency to induce deep and fast responses in second- and third-/fourth-line treatment, and as a consequence, the drug has recently been licensed for patients previously treated with one or more tyrosine kinase inhibitor(s) and for whom imatinib, nilotinib, and dasatinib are not considered appropriate treatment options. (mdm2-receptor.com)
  • Bosutinib (SKI-606), 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3- (4-methyl-1-piperazinyl) propoxy]-3-quinolinecarbonitrile monohydrate, is a competitive inhibitor of both Src and ABL tyrosine kinases. (mdm2-receptor.com)
  • It was originally synthesized as an inhibitor of the Src kinase family. (mdm2-receptor.com)
  • Bosutinib is a potent dual inhibitor of the Src and ABL tyrosine kinases (Puttini et al. (mdm2-receptor.com)
  • Here, it is shown that addition of the protein tyrosine kinase inhibitor [(3,4,5,-trihydroxyphenyl)-methylene]-propanedinitrile (tyrphostin) to intact Swiss 3T3 cells reduces bombesin induced tyrosine phosphorylation and inhibits bombesin mediated c-fos expression and DNA synthesis. (ucl.ac.uk)
  • Our results demonstrate that FAK signaling emanating from Y397, Y925, and to a lesser extent Y576/7, but not from Y861, controls osteogenic differentiation through an ERK1/2 pathway, as measured by expression levels of key osteogenesis marker genes and subsequent matrix mineralization. (techscience.com)
  • These results suggested that in the signal transduction pathway from FAK to PI 3-kinase, Akt promotes survival. (elsevierpure.com)
  • Thus, it became apparent that FAK is the upstream signal protein of the PI 3-kinase- Akt survival pathway in hydrogen peroxide-induced apoptosis in T98G cells. (elsevierpure.com)
  • Cancer Mutations in FGFR2 Prevent a Negative Feedback Loop Mediated by the ERK1/2 Pathway. (rndsystems.com)
  • In addition, we found that BMP-2, a 4HPR target with antiangiogenic activity, decreased prostate cancer cell proliferation, migration and invasion by down-regulating the pathway described involving AKT phosphorylation, β-catenin stability and cyclin D1 expression. (biomedcentral.com)
  • These data point to 4HPR as a negative regulator of AKT phosphorylation, effectively targeting the β-catenin pathway and inducing a relatively benign phenotype in prostate cancer cells, limiting neoangiogenesis and cell invasion. (biomedcentral.com)
  • The goals of Dr. Rebecca Schweppe's lab are to understand the regulation and function of deregulated kinase pathways in thyroid cancer in order to develop more effective therapies. (cuanschutz.edu)
  • In the antiestrogen-resistant cell lines, we observed increased phosphorylation of several pathways involved in cell proliferation and survival. (eur.nl)
  • These peptides bind to seven transmembrane domain receptors which lack intrinsic tyrosine kinase activity and activate second messenger pathways via heterotrimeric G proteins. (ucl.ac.uk)
  • For example, cell adhesion to a fibronectin substratum involves concurrent activation of Src and phosphorylation of the FAK activation loop. (fishersci.com)
  • Here, we address the mechanism leading to the phosphorylation of CasSD in the context of fibronectin-induced early spreading of fibroblasts. (utmb.edu)
  • A ) Staining for phospho-Y397 focal adhesion kinase (pY397FAK) and total FAK of microglia plated on fibronectin (FN) for 1 hour. (jci.org)
  • CB 2 receptors are almost exclusively found in the immune system, with the greatest density in the spleen ( 1 ). (aacrjournals.org)
  • The mechanism by which tyrosine phosphorylation is induced by G protein coupled receptors is unknown. (ucl.ac.uk)
  • BCL2L11 Induction Mediates Sensitivity to Src and MEK1/2 Inhibition in Thyroid Cancer. (cuanschutz.edu)
  • Morphological rescue is possible following Rho kinase inhibition in an oligodendrocyte subset. (jneurosci.org)
  • Inhibition of Ced-3/ICE-related Acacetin IC50 proteases does not prevent cell death induced by oncogenes, DNA damage, or the Bcl-2 homologue Bak. (opioid-receptors.com)
  • We found that 4HPR-induced inhibition of PC cell migration and invasion correlates with decreased FAK and AKT phosphorylation, activation of the glycogen synthase kinase 3β(GSK3β) and β-catenin destabilization. (biomedcentral.com)
  • Although previous studies have identified different chemotropic and adhesion molecules that influence axonal development, the molecular mechanism by which these signals control the cytoskeleton remains poorly understood. (biologists.com)
  • Thus, FAK activity is regulated by a complex set of phosphorylation sites, and thisphospho-regulation could be important for cell motility, cell growth, cytoskeletal organization, and adhesion-dependent cell survival. (fishersci.com)
  • Persons with the most common pediatric brain malignancy, medulloblastoma, fare only slightly better than average, with a 71.9% 5-year survival, though the most common adult brain tumor, glioblastoma multiforme (GBM), incurs a mere 5.1% 5-year survival rate 2 . (nature.com)
  • The examination of surgical lung specimens and an integrated clinico-radiological evaluation allow the start of a complex differential diagnosis and prediction of survival, through the identification of different interstitial patterns [ 2 ]. (ersjournals.com)
  • Protein kinase C regulates human pluripotent stem cell self-renewal. (rndsystems.com)
  • PubMed]Kawano Y, Fukata Y, Oshiro D, Amano Meters, Nakamura Testosterone levels, Ito Meters, Matsumura Y, Inagaki Meters, Kaibuchi T. Phosphorylation of myosin-binding subunit (MBS) of myosin phosphatase by Rho-kinase in vivo. (opioid-receptors.com)
  • This impact is believed to occur via modulation of the phosphorylation of focal adhesion kinase [52] and the expression of matrix metalloproteinases 2 and 9 [52]. (irjs.info)
  • In addition, nuclear factor (NF)‑κB and matrix metalloproteinase (MMP) expression was examined by western blotting, and MMP‑2/‑9 activities were determined by gelatin zymography. (spandidos-publications.com)
  • NF-κB then translocates to the nucleus followed by p65 phosphorylation and binding to specific response elements in the DNA, which subsequently activates target gene expression ( 5 ). (spandidos-publications.com)
  • FAK's ability to bind numerous structural and signaling proteins via a variety of interactions is important for FAK activation level, and for FAK interaction with a variety of substrates localized to sites of cell adhesion. (fishersci.com)
  • We found that hydrophobic phenylalanine substitutions of both tyrosines diminished the binding of tail-interacting proteins, including talins and kindlins, resulting in reduced β1-mediated adhesion, focal adhesion kinase (FAK) signaling, and epidermal progenitor cell-derived skin tumors. (iucc.ac.il)
  • Our results suggest that the small GTP binding protein rhop21 rather than heterotrimeric GTP binding proteins mediates GTP?S induced tyrosine phosphorylation. (ucl.ac.uk)
  • Specificity and mechanism of action of some commonly used protein kinase inhibitors. (rndsystems.com)
  • Significantly, suppression of mTORC2 for 24h with rapamycin or everolimus or treatment with mTOR active-site inhibitors improved HLA II antibody-stimulated phosphorylation of ERK. (cgp60474.com)
  • The results demonstrate that inhibitors of tyrosine kinase activity prevent neuropeptide mediated mitogenesis and may be of therapeutic value for SCLC. (ucl.ac.uk)
  • ILK is composed of three domains, an N-terminal ankryin domain, a pleckstrin homology domain, and a putative kinase domain. (jneurosci.org)
  • Remarkable differences were observed for the levels of activated AMPK alpha1, cyclins, STAT5, STAT6, ERK1/2 and BCL2. (eur.nl)
  • Production of interlukin-2 and activation of the transcription factor NF-AT in response to triggering of the TCR -CPM mutant with SEB were fully restored in the presence of constitutively active Fyn. (unisi.it)
  • not really affect HLA II antibody-induced phosphorylation of ERK, mTORC1 targets were reliant on activation of ERK instead. (cgp60474.com)
  • Furthermore, knockdown of Rictor with siRNA triggered over-activation of ERK while abolishing phosphorylation of Akt Ser473 induced by course II antibody. (cgp60474.com)
  • The activation of PI3K IGF1 and Akt network marketing leads to up-regulation of anti-apoptotic Bcl-2 and Bcl-XL protein appearance in EC (27). (cgp60474.com)
  • Both cell adhesion and Rac activation stimulated PKL tyrosine phosphorylation. (healthyguide.info)
  • Tenascin C induces epithelial-mesenchymal transition-like change accompanied by SRC activation and focal adhesion kinase phosphorylation in human breast cancer cells. (ac.ir)
  • Caspase-mediated calcineurin activation contributes to IL-2 release during T cell activation. (opioid-receptors.com)
  • Tyrosine phosphorylation of the substrate domain of Cas (CasSD) correlates with increased cell migration in healthy and diseased cells. (utmb.edu)
  • Endostatin inhibits endothelial cell migration by inhibiting phosphorylation of focal adhesion kinase via binding to α5β1 integrin (Wickstrom et al. (justia.com)
  • Kindlin3 deficiency as well as Kindlin3 mutations of integrin-binding sites abolish both integrin inside-out and outside-in signaling in microglia, thereby resulting in severe deficiencies in cell adhesion, polarization, and migration in vitro, which are similar to the defects observed in macrophages. (jci.org)
  • T cell hybridomas expressing an -CPM-mutated TCR show a dramatic impairment in antigen-driven interleukin-2 pro- duction. (unisi.it)
  • In cells expressing RPTPkappa RNAi, phosphorylation of Src at Tyr527 was increased and (activating) phosphorylation of Src at Tyr416 was reduced. (nih.gov)
  • As group 2 innate lymphoid cells (ILC2s) can act as an environmental sensor and significantly contribute to protease allergen-induced lung inflammation, we aimed to elucidate the causal relationship and how inhaled acrylamide worsens allergic lung inflammation via ILC2s. (bvsalud.org)
  • Molecular Probes Eugene OR) immunoprecipitation null cells transiently transfected were lysed using radioimmunoprecipitation buffer (50 mM Tris-HCl pH 7.4 150 mM NaCl 2 mM EDTA 1% TX-100 1 sodium deoxycholate 0.1% SDS 10 glycerol 20 μg/ml aprotinin 10 μg/ml leupeptin 1 mM PMSF and 0.2 mM sodium vanadate) and then processed as explained above. (healthyguide.info)
  • The pattern of tyrosine phosphorylation closely resembled that induced by neuropeptides in intact cells. (ucl.ac.uk)
  • 2) NOVEL SCLC THERAPIES Substance P (SP) analogues [DArg1, DPhe5, DTrp7,9, Leu11] SP and [Arg6, DTrp7,9, MePhe8] SP (6-11) inhibit the action of many different calcium mobilizing neuropeptides including vasopressin and bombesin in Swiss 3T3 cells and SCLC cell lines and block the growth of SCLC xenografts in nude mice. (ucl.ac.uk)
  • PubMed]Murata-Hori M, Suizu F, Iwasaki T, Kikuchi A, Hosoya H. Squat kinase identified as a novel myosin regulatory light chain kinase in HeLa cells. (opioid-receptors.com)
  • The endomysial infiltrates in patients with s-IBM are composed primarily of CD8+ T cells and macrophages in a 2:1 ratio. (medscape.com)
  • Inhibits MEK-1 and MEK-2 (IC 50 values of 0.07 and 0.06 μ M respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. (rndsystems.com)
  • A plasma alpha 2 glycoprotein that accounts for the major antithrombin activity of normal plasma and also inhibits several other enzymes. (lookformedical.com)
  • Identification of the endogenous easy muscle myosin phosphatase-associated kinase. (opioid-receptors.com)
  • The deregulation of protein kinases plays a major role in promoting tumorigenesis in the majority of human cancers, including thyroid cancer, and targeting this deregulated activity has led to major breakthroughs in cancer therapy. (cuanschutz.edu)
  • on the kinase activity of both RON itself and c-Src. (123dok.org)
  • In 2015, 4292,000 new cancer cases and 2814,000 cancer deaths have been estimated to occur in China [ 2 ], according to the data released by the National Central Cancer Registry of China. (hindawi.com)
  • 2006). In addition, more than 45 other tyrosine and serine/threonine kinases have been identified as potential targets of bosutinib. (mdm2-receptor.com)
  • The neural cell adhesion molecule, NCAM, is a member of the immunoglobulin (Ig) superfamily and is involved in a variety of cellular processes of importance for the formation and maintenance of the nervous system. (uni-freiburg.de)