• The class 1A phosphoinositide 3-kinase (PI3K) beta (PI3Kβ) is functionally unique in the ability to integrate signals derived from receptor tyrosine kinases (RTKs), heterotrimeric guanine nucleotide-binding protein (G-protein)-coupled receptors (GPCRs), and Rho-family GTPases. (elifesciences.org)
  • c-Src can be activated by many transmembrane proteins that include: adhesion receptors, receptor tyrosine kinases, G-protein coupled receptors and cytokine receptors. (wikipedia.org)
  • 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). (wikipedia.org)
  • Although it is similar to other receptor tyrosine kinases, the Axl protein represents a unique structure of the extracellular region that juxtaposes IgL and FNIII repeats. (wikipedia.org)
  • Deregulation of receptor tyrosine kinases in human cancers can occur through positive activation of the receptor or through the loss of negative regulatory controls. (mcgill.ca)
  • Receptor tyrosine kinases including EGFR, HER-2 and c-Met and non receptor tyrosine kinase including Jaks are selectively expressed in primary tissue and metastatic tumour of advanced ovarian cancer cells. (otago.ac.nz)
  • Together with other receptor tyrosine kinases, PDGFRA, is a prominent target not only in gliomas, but also in a number of haematological malignancies for targeted therapies based on tyrosine kinase inhibitors (TKI) and anti-PDGFRA monoclonal antibodies. (biospace.com)
  • Receptor tyrosine kinases (RTKs) play an important role in a variety of cellular processes in cancer [ 3 ]. (hindawi.com)
  • The ALK gene provides instructions for making a protein called ALK receptor tyrosine kinase, which is part of a family of proteins called receptor tyrosine kinases (RTKs). (medlineplus.gov)
  • Receptor tyrosine kinases transmit signals from the cell surface into the cell through a process called signal transduction. (medlineplus.gov)
  • Genetic mutation and pharmacological inhibition of Bruton's tyrosine kinase (Btk) both have been shown to prevent the development of collagen-induced arthritis (CIA) in mice, providing a rationale for the development of Btk inhibitors for treating rheumatoid arthritis (RA). (aspetjournals.org)
  • The lysis was inhibited by two different PI 3-kinase inhibitors, wortmannin and LY294002. (elsevierpure.com)
  • Furthermore, exocytosis of cytolytic effector molecules was also inhibited by PI 3-kinase inhibitors and PKC inhibitors. (elsevierpure.com)
  • This cytotoxicity displayed by PMA-treated YT cells, however, could still be inhibited by PI 3-kinase inhibitors and PKC inhibitors. (elsevierpure.com)
  • In contrast, Btk signaling sustains growth of several B-cell neoplasms which may be treated with tyrosine kinase inhibitors (TKIs). (rcsb.org)
  • Imatinib is one of the first tyrosine kinase inhibitors and is used in several conditions based on effects on receptors like BCR-ABL, the platelet-derived growth factor receptor (PDGFR), and stem cell factor (SCF)/c-kit tyrosine kinases. (asn-online.org)
  • Managing toxicities of Bruton tyrosine kinase inhibitors. (iasp-pain.org)
  • By targeting this critical kinase in proximal B-cell receptor signaling, BTK inhibitors (BTKis) impair cell proliferation, migration, and activation of NF-κB. (iasp-pain.org)
  • My research interests are focusing on the activity of tyrosine kinases, targeted inhibitors, effects of ascitic fluid ,and anti-tumour properties of natural food compounds in the progression of advanced ovarian cancer. (otago.ac.nz)
  • [ 2 ] Options for second-line therapy in patients with relapsed/refractory disease include chemotherapy-free regimens with biologic targeted agents such as covalent Bruton tyrosine kinase (BTK) inhibitors, lenalidomide,venetoclax, and chimeric antigen receptor (CAR) T-cell therapy. (medscape.com)
  • Incubation with NADPH oxidase inhibitors inhibited both superoxide anion production and the activation of p56(Hck), p72(Syk), and p77(Btk) in response to fungal spores. (cdc.gov)
  • The treatment paradigm of AML patients harboring FLT3 mutations (30%) has been modified by the discovery of tyrosine kinase inhibitors. (dovepress.com)
  • Indeed, we observed partial restoration of dexamethasone sensitivity with a combination of dexamethasone and inhibitors targeting either these kinases or β-catenin. (lu.se)
  • Chronic myeloid leukemia (CML) is currently treated with tyrosine kinase inhibitors, but these do not effectively eliminate the CML stem cells. (lu.se)
  • Serving a critical role in cell signaling, the class I family of phosphoinositide 3-kinases (PI3Ks) catalyze the phosphorylation of phosphatidylinositol 4,5-bisphosphate [PI(4,5)P 2 ] to generate PI(3,4,5) P 3 . (elifesciences.org)
  • Binding of Sema4D to plexin-B1 stimulates the intrinsic tyrosine kinase activity of ErbB-2, resulting in the phosphorylation of both plexin-B1 and ErbB-2. (rupress.org)
  • Our data indicate that ErbB-2 is an important component of the plexin-B receptor system and that ErbB-2-mediated phosphorylation of plexin-B1 is critically involved in Sema4D-induced RhoA activation, which underlies cellular phenomena downstream of plexin-B1, including axonal growth cone collapse. (rupress.org)
  • Mast cell activation involves cross-linking of IgE receptors followed by phosphorylation of the non-receptor tyrosine kinase Syk. (ox.ac.uk)
  • Upon incubation with 20:4(n-6), the mobility of both isoforms was retarded, consistent with their activation by phosphorylation. (nih.gov)
  • In this work, we report that CD28-mediated cytotoxicity of YT involves tyrosine phosphorylation and activation of phosphatidylinositol (PI) 3-kinase, the Tec kinase Itk/Emt, and protein kinase C (PKC). (elsevierpure.com)
  • Taken together, these results are consistent with a model in which activation of CD28 and LFA-1 induces tyrosine phosphorylation of the CD28 cytoplasmic domain, recruitment and activation of PI 3-kinase, as well as the Tec kinase Itk/Emt, and the activation of PMA-nonresponsive PKC isoenzymes. (elsevierpure.com)
  • Dive into the research topics of 'CD28-mediated cytotoxicity by the human leukemic NK cell line YT involves tyrosine phosphorylation, activation of phosphatidylinositol 3-kinase, and protein kinase C'. Together they form a unique fingerprint. (elsevierpure.com)
  • 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)
  • Following B-cell receptor activation, 2 waves of tyrosine kinase phosphorylation occur. (medscape.com)
  • It is known to act through protein phosphorylation via PRKA and through the activation of guanine nucleotide exchange factors like EPAC. (plos.org)
  • Steve uses advanced microscopy (FCS and single molecule), molecular modelling (ODE and agent-based), crystallography, cell line studies and protein phosphorylation to study the mechanisms of receptor activation. (birmingham.ac.uk)
  • When we correlated protein phosphorylation levels with cellular oncogenic phenotypes, we observed a novel non-receptor tyrosine kinase, TNK2, to be hyperphosphorylated and activated in highly aggressive TNBC cells. (dtic.mil)
  • Pro-inflammatory cytokines and environmental stress cause p38 mitogen-activated protein kinase activation by dual phosphorylation on tyrosine and threonine. (nih.gov)
  • After dimerization, the kinase is tagged with a marker called a phosphate group (a cluster of oxygen and phosphorus atoms) in a process called phosphorylation. (medlineplus.gov)
  • Phosphorylation turns on (activates) the kinase. (medlineplus.gov)
  • These kinases lead to β-catenin stabilization through phosphorylation-dependent inactivation of GSK-3β either directly or indirectly. (lu.se)
  • We demonstrate that DARPP-32 inhibits MCF-7 cell migration and that this effect requires phosphorylation of Threonine-34, an event catalyzed by protein kinase A (PKA) and strongly induced by detachment of cells from the culture substrate. (lu.se)
  • Perilipin 1 binds to aquaporin 7 in human adipocytes and controls its mobility via protein kinase A mediated phosphorylation. (lu.se)
  • however, many target multiple kinase receptors in addition to AXL. (wikipedia.org)
  • Two tyrosine kinase-dependent pathways exist for activation of the respiratory burst by polymorphonuclear leukocyte (PMN) immunoglobulin G Fc receptors. (adacyte.com)
  • There is increasing evidence to support the concept that the malignant behavior of some tumors is sustained by the deregulated activation of growth factor receptors. (mcgill.ca)
  • Abl tyrosine kinases likely play important roles as downstream receptors in regulating actin cytoskeleton remodeling and intracellular trafficking. (asn-online.org)
  • The cytokine receptors lack intrinsic kinase activity and require interaction with members of the Jak family of intracellular signaling molecules. (jneurosci.org)
  • Steve's research interests focus on mechanisms of platelet activation by tyrosine kinase-linked receptors (notably CLEC-2, FcgammaRIIA, GPVI and PEAR1) and in developing novel antiplatelet agents that target these receptors in thrombi-inflammatory disease. (birmingham.ac.uk)
  • Steve's undertakes a multi- and inter-disciplinary to investigate the molecular mechanisms underlying platelet activation by tyrosine kinase linked glycoprotein receptors. (birmingham.ac.uk)
  • Both receptors and ligands are membrane-bound proteins that require direct cell-cell interaction for activation. (hindawi.com)
  • The tyrosine kinase receptors Tyro3, Axl and Mer (TAMs) and their ligands protein S and Gas6 are involved in the uptake of PS-exposing apoptotic cells in macrophages and dendritic cells. (lu.se)
  • Activation of the protein-tyrosine kinase activity of the receptors occurs by ligand-induced dimerization or heterodimerization of PDGF receptor types. (bvsalud.org)
  • the second activates Bruton tyrosine kinase and Syk. (medscape.com)
  • X-linked agammaglobulinemia (XLA), or Bruton agammaglobulinemia, is an inherited immunodeficiency disease caused by mutations in the gene coding for Bruton tyrosine kinase (BTK). (medscape.com)
  • This disorder is now formally referred to as X-linked agammaglobulinemia (XLA), and the gene defect has been mapped to the gene that codes for Bruton tyrosine kinase (Btk) at band Xq21.3. (medscape.com)
  • Reversible inhibitor of EGFR (HER1) and HER2 receptor kinases. (pharmacology2000.com)
  • Activation of Abl tyrosine kinases increases cell surface expression of EGFR. (asn-online.org)
  • Therefore, inhibition of Abl tyrosine kinases by imatinib may lead to blockade of the EGF/EGFR signaling that regulates AQP2 distribution and FR. (asn-online.org)
  • In NSCLC, activation of the EGFR/HER1 pathway results in a signalling cascade that promotes tumour growth and progression 6 . (ersjournals.com)
  • Mediated by both on-target inhibition of BTK and variable off-target inhibition of other kinases including interleukin-2-inducible T-cell kinase (ITK), tyrosine-protein kinase (TEC), and endothelial growth factor receptor (EGFR), the toxicity profile of BTKis is closely linked to their pattern of kinase binding. (iasp-pain.org)
  • and (b) direct inhibition of the slow Ca2+ channels (i.e. independent of inhibition of tyrosine kinase activity). (unboundmedicine.com)
  • This effect was mediated by an action on cholesterol metabolism in lipid rafts and was prevented by tyrosine kinase inhibition. (jneurosci.org)
  • Therefore, the SH2-kinase interface is critical for Btk activation and a targetable site for allosteric inhibition. (rcsb.org)
  • Inhibition of Bruton's tyrosine kinase (BTK) has revolutionized the treatment landscape for patients with chronic lymphocytic leukemia (CLL). (iasp-pain.org)
  • Pharmacological inhibition of cathepsin activity with CA074-Me resulted in a substantial reduction of both mature IL-1β production and caspase-1 activation in infected macrophages. (frontiersin.org)
  • Moreover, cathepsin inhibition abolished the interaction between NLRP3 and ASC, measured by immunofluorescence imaging in H37Rv-infected macrophages, demonstrating a critical role of the enzyme in NLRP3-inflammasome activation. (frontiersin.org)
  • Effects of genistein, a specific inhibitor of tyrosine kinase, on the L-type Ca2+ channels were examined in freshly isolated young (days 10-18) rat ventricular cells using the whole-cell patch-clamp technique. (unboundmedicine.com)
  • and liver fibrosis resolved on treatment with the Src kinase inhibitor dasatinib. (nature.com)
  • Two patients with truncating mutations had liver fibrosis that in one patient resolved on treatment with the Src kinase inhibitor dasatinib. (nature.com)
  • Afatinib is considered a highly selective tyrosine kinase inhibitor. (pharmacology2000.com)
  • Olsson PO, Gustafsson R, In 't Zandt R, Friman T, Maccarana M, Tykesson E, Oldberg Å, Rubin K, Kalamajski S. The Tyrosine Kinase Inhibitor Imatinib Augments Extracellular Fluid Exchange and Reduces Average Collagen Fibril Diameter in Experimental Carcinoma. (lu.se)
  • Two of the phosphotyrosine-containing proteins, migrating in SDS-polyacrylamide gels of approximately 43 and 45 kDa, corresponded in mobility to phosphorylated species of the 42- and 44-kDa mitogen-activated protein kinase (MAPK) isoforms. (nih.gov)
  • Treatment of AMs with H(2)O(2) (1 mM) caused the activation of p72(Syk) only, whereas treatment with superoxide dismutase and catalase before treatment with the spores had no effect on tyrosine kinase activation. (cdc.gov)
  • A common mechanism is that there are genetic mutations that result in the increased activity or the overexpression of the c-Src leading to the constant activation of the c-Src. (wikipedia.org)
  • Here, we uncovered the structural mechanism by which certain XLA mutations in the SH2 domain strongly perturb Btk activation. (rcsb.org)
  • Using a combination of molecular dynamics (MD) simulations and small-angle X-ray scattering (SAXS), we discovered an allosteric interface between the SH2 and kinase domain required for Btk activation and to which multiple XLA mutations map. (rcsb.org)
  • Mutations in the ALK gene change single protein building blocks (amino acids) in ALK receptor tyrosine kinase. (medlineplus.gov)
  • To understand the mechanisms of resistance to glucocorticoids, such as dexamethasone, we generated dexamethasone-resistant B-ALL cell lines in paper I. One such resistant cell line was found to possess increased FLT3 expression levels with FLT3-ITD and FLT3-R845G mutations that led to the activation of oncogenic RTK signaling. (lu.se)
  • MEN 2A and familial medullary thyroid carcinoma mutations result in activation of certain intracellular pathways. (msdmanuals.com)
  • and transmembrane receptor protein tyrosine kinase signaling pathway. (nih.gov)
  • In vitro , GnRH neuronal cell lines respond to a variety of ligands that activate the Jak (Janus-activated kinase)/STAT (signal transducers and activators of transcription) intracellular signaling pathway. (jneurosci.org)
  • The activation continues through a series of proteins in a signaling pathway. (medlineplus.gov)
  • As a result, the kinase and the downstream signaling pathway are constantly turned on (constitutively activated). (medlineplus.gov)
  • Chromatography of soluble fractions from these cells on Mono Q columns revealed early and late eluting peaks of myelin basic protein kinase activity, which contained the 42- and 44-kDa MAPK isoforms, respectively. (nih.gov)
  • Rapid and transient activation of myelin basic protein kinase in tobacco leaves treated with hairpin from Erwinia amylovora . (springer.com)
  • G, p.Y508* (transcript NM_002350), that resulted in truncation of five terminal amino acids, including a regulatory tyrosine at position p.Y508. (nature.com)
  • The BTK gene defect has been mapped to the long arm of the X chromosome at band Xq21.3 to Xq22, spanning 37.5kb with 19 exons forming 659 amino acids to complete the BTK cytosolic tyrosine kinase. (medscape.com)
  • The BTK gene is large and consists of 19 exons that encode the 659 amino acids that form the Btk cytosolic tyrosine kinase. (medscape.com)
  • pronounced "sarc", as it is short for sarcoma), is a non-receptor tyrosine kinase protein that in humans is encoded by the SRC gene. (wikipedia.org)
  • It belongs to a family of Src family kinases and is similar to the v-Src (viral Src) gene of Rous sarcoma virus. (wikipedia.org)
  • Tyrosine-protein kinase receptor UFO is an enzyme that in humans is encoded by the AXL gene. (wikipedia.org)
  • The protein encoded by this gene is a member of the receptor tyrosine kinase subfamily. (wikipedia.org)
  • 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)
  • These changes led to the constitutive activation of a prominent oncogene - receptor tyrosine kinase gene PDGFRA. (biospace.com)
  • This phenomenon, known as gene amplification, results in overexpression of ALK receptor tyrosine kinase. (medlineplus.gov)
  • We now report that incubation of WB cells with 20:4(n-6) resulted in the appearance of several tyrosine-phosphorylated cytosolic proteins. (nih.gov)
  • Previous experiments have not been able to elucidate whether interactions with membrane-tethered proteins primarily control PI3Kβ localization versus directly modulate lipid kinase activity. (elifesciences.org)
  • i) which Gab1 dependent signals are required for morphogenesis, by assessing known Gab1 associated proteins and Gab1 associated proteins identifid by tandem mass spectroscopy, ii) the molecular basis through which the tyrosine phosphatase SHP-2 is required for morphogenesis. (mcgill.ca)
  • Its activation is tightly controlled by numerous other signaling proteins including protein kinase C (PKC), Sab/SH3BP, and caveolin-1. (medscape.com)
  • c-Src phosphorylates specific tyrosine residues in other tyrosine kinases. (wikipedia.org)
  • Kinetic analysis of specific tyrosine kinases demonstrated that p56(Hck), p72(Syk), and p77(Btk) were activated faster and to a greater extent by spores from A. candidus as compared with spores from E. amstelodami. (cdc.gov)
  • Orthologous to human ABL2 (ABL proto-oncogene 2, non-receptor tyrosine kinase). (nih.gov)
  • My lab has focused on and will continue to address these questions using the Met receptor tyrosine kinase and oncogene as a model. (mcgill.ca)
  • Ca2+ entry through CRAC channels therefore provides a means whereby the Ca2+ and tyrosine kinase signaling pathways can interact with one another. (ox.ac.uk)
  • Since the activation of c-Src leads to the promotion of survival, angiogenesis, proliferation and invasion pathways, the aberrant growth of tumors in cancers is observed. (wikipedia.org)
  • To investigate the conformational change of c-Src tyrosine kinase, we applied network analysis to time series of correlation among residues. (intechopen.com)
  • With centrality measures such as betweenness centrality, degree centrality, and closeness centrality, we observed a few important residues that significantly contribute to the conformational change of c-Src tyrosine kinase for the different time steps. (intechopen.com)
  • Notably, the first two post-translational modifications, which are required for the initial activation of these complexes, occur on solvent inaccessible (i.e., buried) tyrosine residues. (lu.se)
  • If these residues are inaccessible to kinases, how do they get phosphorylated then? (lu.se)
  • We characterize the role of increased Lyn kinase activity in neutrophils, endothelial cells and lesional liver biopsies and utilized an iPSC-derived endothelial cell platform for disease modeling of neutrophilic vasculitis and to screen and evaluate drug efficacy. (nature.com)
  • As circulating PMPs-levels were not altered in Gas6-/- mice compared to Gas6+/+ mice, we hypothesize that the Gas6-mediated uptake is not a means to clear the bulk of circulating PMPs but may serve to phagocytose PMPs locally generated at sites of platelet activation and as a way to affect endothelial responses. (lu.se)
  • This induces long-range allostery via protein domain dynamics, causing the structure to be destabilized, resulting in the opening up of the SH3, SH2 and kinase domains and the autophosphorylation of the residue tyrosine 416. (wikipedia.org)
  • We observed that dexamethasone exposure caused upregulation of Aurora kinase and its various downstream effector kinases such as JAK, p38, mTOR, and S6K. (lu.se)
  • Activation of IL-4/IL-13 signaling promotes proliferation of FAPs to support myogenesis while inhibiting their differentiation into adipocytes. (scienceexhibitions.org)
  • 2008 For instance autocrine Notch signaling regulates the activation and proliferation of satellite cells (Bjornson et al. (scienceexhibitions.org)
  • The repebody prevents activation of wild-type and TKI-resistant Btk, inhibiting Btk-dependent signaling and proliferation of malignant B-cells. (rcsb.org)
  • Although the specific function of ALK receptor tyrosine kinase is unknown, it is thought to act early in development to help regulate the proliferation of nerve cells. (medlineplus.gov)
  • Constitutive activation of ALK receptor tyrosine kinase may increase the proliferation of immature nerve cells, leading to neuroblastoma. (medlineplus.gov)
  • Here, we show that primitive (CD34(+)CD38(-)) CML cells, in contrast to corresponding normal cells, express a functional interleukin-1 (IL-1) receptor complex and respond with NF-κB activation and marked proliferation in response to IL-1. (lu.se)
  • they also indicate that some species of spores are capable of activating tyrosine kinases independent of superoxide anion. (cdc.gov)
  • AXL is a cell surface receptor tyrosine kinase, part of the TAM family of kinases including TYRO3 and MERTK. (wikipedia.org)
  • Here, we show that plexin-B family members stably associate with the receptor tyrosine kinase ErbB-2. (rupress.org)
  • Regulation of MT dynamics via direct binding of an Abl family kinase. (nih.gov)
  • Given the versatility inherent in this intrinsically disordered region, its multisite phosphorylations, and its divergence within the family, the unique domain likely functions as a central signaling hub overseeing much of the enzymatic activities and unique functions of Src family kinases. (wikipedia.org)
  • Here we show that direct ligation of FcγRII leads to activation and Triton X-100 insolubility of the Src family kinase Fgr, without effect on the related myeloid Src family member Hck. (adacyte.com)
  • Next-generation sequencing identified two de novo truncating variants in the Src-family tyrosine kinase, LYN , p.Y508*, p.Q507* and a de novo missense variant, p.Y508F, that result in constitutive activation of Lyn kinase. (nature.com)
  • A role of Src family kinase members in causing sterile inflammation and human disease is only recently recognized. (nature.com)
  • The CD20 molecule is involved in B-cell activation and is associated with various Src family kinases (Lyn, Lck, Fyn). (biolegend.com)
  • Moreover, Wnt-5a is known to inhibit migration of breast epithelial cells in culture and expression of Wnt-5a potentiates activation of the receptor tyrosine kinase DDR1, a collagen receptor implicated in cell adhesion and migration. (lu.se)
  • The dimerization of c-Src is mediated by the interaction of the myristoylated N-terminal region of one partner and the kinase domain of another partner. (wikipedia.org)
  • Although pY peptides strongly localize PI3Kβ to membranes, they only modestly stimulate lipid kinase activity. (elifesciences.org)
  • Our results reveal a positive feedback step in mast cell activation where receptor-triggered Syk activation and subsequent Ca2+ release opens CRAC channels, and the ensuing local Ca2+ entry then maintains Syk activity. (ox.ac.uk)
  • 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. (wikipedia.org)
  • Despite wealth information of these tyrosine kinase expressions and activation, little is known about the biological activity of tyrosine kinases in ovarian cancer cells are present in ascitic fluid. (otago.ac.nz)
  • Finally, we found that phospho-DARPP-32 inhibited the activity of the focal adhesion kinase (FAK) in MCF-7 breast cancer cells, and that MCF-7 cells expressing phospho-DARPP-32 displayed less filopodia formation. (lu.se)
  • We hypothesize that a dynamic equilibrium between the dominant buried state and an transiently open, kinase-accessible state is present in the p27-cyclin A-CDK2 complex, and aim to test this hypothesis through the use of unbiased molecular dynamics and metadynamics simulations. (lu.se)
  • Existing medicines (imatinib) therefore target this kinase. (eurekalert.org)
  • Acalabrutinib, the initial second-generation BTKi to earn approval from the US Food and Drug Administration, demonstrates improved kinase selectivity for BTK, with commonly observed adverse reactions including infection, headache, and diarrhea. (iasp-pain.org)
  • Other emerging BTKis include second-generation agents with variable degrees of kinase selectivity and third-generation agents that exhibit reversible noncovalent binding to BTK. (iasp-pain.org)
  • When Src is inactive, the phosphorylated tyrosine group at the 527 position interacts with the SH2 domain which helps the SH3 domain interact with the flexible linker domain and thereby keeps the inactive unit tightly bound. (wikipedia.org)
  • Sustained activation of the tyrosine kinase Syk by antigen in mast cells requires local Ca2+ influx through Ca2+ release-activated Ca2+ channels. (ox.ac.uk)
  • Activation of PI 3-kinase and PMA-nonresponsive PKC isoenzymes is shown to be involved directly in cytolytic granule release by YT cells. (elsevierpure.com)
  • This kinase causes the trouble, leading to the increase in CML cells. (eurekalert.org)
  • 4 It encodes a receptor tyrosine kinase involved in the development and homeostasis of several cell lines including melanocytic (pigment), hematologic (blood), mast, and germ cells. (creation.com)
  • This project is investigating the expression and activation of tyrosine kinases in ovarian cancer cells isolated from ascitic fluid. (otago.ac.nz)
  • Activation of Btk results in a cascade of signaling events resulting in calcium mobilization and fluxes, cytoskeletal rearrangements, and transcriptional regulation involving nuclear factor-kappaB (NF-kappaB) and nuclear factor of activated T cells (NFAT). (medscape.com)
  • Plexin-B1 has recently been shown to mediate activation of RhoA through a stable interaction with the Rho guanine nucleotide exchange factors PDZ-RhoGEF and LARG. (rupress.org)
  • As allosteric interactions provide unique targeting opportunities, we developed an engineered repebody protein binding to the SH2 domain and able to disrupt the SH2-kinase interaction. (rcsb.org)
  • Our findings reveal a critical role for Lyn kinase in modulating inflammatory signals, regulating microvascular permeability and neutrophil recruitment, and in promoting hepatic fibrosis. (nature.com)
  • FMS-like tyrosine kinase 3 ( FLT3 ) is one of the most frequently mutated genes in acute myeloid leukemia (AML). (dovepress.com)
  • Approximately 30% of the adult cases harbor an internal tandem duplication ( FLT3 -ITD) and 5- 10% a tyrosine kinase domain (TKD) amino acid substitution ( FLT3-TKD ). (dovepress.com)
  • Among the most mutated driver genes in AML is FMS-like tyrosine kinase 3 ( FLT3 ). (dovepress.com)
  • This results in activation of the plasma membrane-bound enzyme phospholipase Cgamma1, which hydrolyzes the minor membrane phospholipid phosphatidylinositol 4,5-bisphosphate to generate diacylglycerol and inositol trisphosphate. (ox.ac.uk)
  • Using single molecule Total Internal Reflection Fluorescence (TIRF) Microscopy, we determined the mechanism controlling membrane localization of PI3Kβ, prioritization of signaling inputs, and lipid kinase activation. (elifesciences.org)
  • The manuscript describes the synergy among PI3Kβ activators, providing compelling results concerning the mechanism of their activation. (elifesciences.org)
  • The mechanism of this differential activation was studied. (cdc.gov)
  • Increased receptor autophosphorylation may cause receptor activation possibly without ligand binding. (pharmacology2000.com)
  • Receptor activation causes Jak2 autophosphorylation, which phosphorylates its associated receptor. (jneurosci.org)
  • 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)
  • Used (as the hydrochloride salt) for the treatment of patients with anaplastic lymphoma kinase-positive, metastatic non-small cell lung cancer. (chemspider.com)
  • Our work in the past few years has uncovered an important regulator of invasive cell growth, the Met receptor tyrosine kinase. (mcgill.ca)
  • The receptor makes a single pass through the cell membrane and contains an intracellular kinase catalytic region divided by a hydrophilic insert. (creation.com)
  • In order to explore the role of tyrosine kinase signaling in TNBCs, we have performed global phosphotyrosine profiling for a panel of 25 TNBC cell lines. (dtic.mil)
  • The process begins when the kinase is stimulated at the cell surface and then attaches to a similar kinase (dimerizes). (medlineplus.gov)
  • The activated kinase is able to transfer a phosphate group to another protein inside the cell, which is activated as a result. (medlineplus.gov)
  • Mutated or overexpressed ALK receptor tyrosine kinase no longer requires stimulation from outside the cell to be phosphorylated. (medlineplus.gov)
  • As a biologically important example we have studied the complex formed by cyclins and cyclin-dependent kinases (CDKs), which play an essential role in the control of the eukaryotic cell cycle. (lu.se)
  • Pharmacological activation of this pathway may constitute a novel way of limiting breast cancer metastasis. (lu.se)