• The phosphorylation leads to association with JAK/Tyk tyrosine kinases and STAT protein transcription factors. (wikipedia.org)
  • Here, we showed that hepatocyte growth factor (HGF), a ligand of MET oncoprotein, induces gefitinib resistance of lung adenocarcinoma cells with EGFR -activating mutations by restoring the phosphatidylinositol 3-kinase/Akt signaling pathway via phosphorylation of MET, but not EGFR or ErbB3. (aacrjournals.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)
  • Brain-derived neurotrophic factor (BDNF), neurotrophin-3 (NT-3), and neurotrophin-4 (NT-4) activated the FL receptor, as determined by tyrosine phosphorylation. (jneurosci.org)
  • 2016). Here, we expand this high-throughput platform to analyze the intrinsic specificity of any tyrosine kinase domain against thousands of peptides derived from human tyrosine phosphorylation sites. (escholarship.org)
  • Phosphorylation is mediated by additionally recruited kinases. (encyclopedia.pub)
  • Ligand binding to the four closely related members of this RTK family -epidermal growth factor receptor (EGFR, also known as ErbB-1 or HER1), ErbB-2 (HER2), ErbB-3 (HER3), and ErbB-4 (HER4)-induces the formation of receptor homo- and heterodimers and the activation of the intrinsic kinase domain, resulting in phosphorylation on specific tyrosine residues (pY) within the cytoplasmic tail. (genome.jp)
  • Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. (drugbank.com)
  • The exact relationship between these events is likely to be functionally significant, as cytoplasmic-domain serine phosphorylation and internalization have been shown to regulate the function of receptors that possess intrinsic protein-tyrosine kinase activity. (mssm.edu)
  • Pharmacologic blockade of PKC inhibits cell adhesion and spreading as well as focal adhesion formation and focal adhesion kinase (FAK) phosphorylation [13,14]. (mirnamimic.com)
  • Tyrosine kinase inhibitors (TKIs) against the human epidermal growth factor receptor (EGFR) are now standard treatment in the clinic for patients with advanced EGFR mutant non-small-cell lung cancer (NSCLC). (researchgate.net)
  • Lung cancer with epidermal growth factor receptor (EGFR)-activating mutations responds favorably to the EGFR tyrosine kinase inhibitors gefitinib and erlotinib. (aacrjournals.org)
  • Background: Most patients with lung cancer experience relapse, although epidermal growth factor receptor (EGFR) of tyrosine kinase inhibitor (TKI) has an astounding effect on tumors with EGFR-activating mutations. (iiarjournals.org)
  • BDTX-1535, a fourth-generation, brain-penetrant epidermal growth factor receptor (EGFR) MasterKey tyrosine kinase inhibitor (TKI), is under investigation for the treatment of NSCLC harboring intrinsic driver and/or acquired resistance (post-osimertinib) EGFR mutations and glioblastoma multiforme (GBM) with multiple EGFR alterations. (drug-dev.com)
  • b ) receptors that associate with other tyrosine kinases, and ( c ) tyrosine-kinase-associated receptors with the ligand-binding subunit membrane anchored by a glycolipid, such as that for ciliary neurotrophic factor. (aspetjournals.org)
  • What is the most common activity found intrinsic to transmembrane receptors? (flashcardmachine.com)
  • What are physical characteristics found in all tyrosine kinase receptors? (flashcardmachine.com)
  • The trk receptors, a family of receptor tyrosine kinases including trkA, trkB, and trkC, serve as the principal signal-transducing receptors for the neurotrophins ( Barbacid, 1994 ). (jneurosci.org)
  • Non-Catalytic Tyrosine-Phosphorylated Receptors" Encyclopedia , https://encyclopedia.pub/entry/36839 (accessed November 29, 2023). (encyclopedia.pub)
  • Non-catalytic tyrosine-phosphorylated receptors (NTRs), also called immunoreceptors or Src-family kinase-dependent receptors, are a group of cell surface receptors expressed by leukocytes that are important for cell migration and the recognition of abnormal cells or structures and the initiation of an immune response. (encyclopedia.pub)
  • For that tyrosine residues in the cytoplasmic tail of the receptors have to be phosphorylated, hence the receptors are referred to as tyrosine-phosphorylated receptors. (encyclopedia.pub)
  • They are called non-catalytic receptors, as the receptors have no intrinsic tyrosine kinase activity and cannot phosphorylate their own tyrosine residues. (encyclopedia.pub)
  • The most prominent feature is the presence of conserved signalling motifs containing tyrosine residue, such as Immunoreceptor tyrosine-based activation motifs (ITAMs), in the cytoplasmic tail of the receptors. (encyclopedia.pub)
  • The receptors themselves have no intrinsic tyrosine kinase activity. (encyclopedia.pub)
  • The Shc- and/or Grb2-activated mitogen-activated protein kinase (MAPK) pathway is a common target downstream of all ErbB receptors. (genome.jp)
  • A family of structurally-related cell-surface receptors that signal through an intrinsic PROTEIN-TYROSINE KINASE. (edu.au)
  • Eph receptors constitute the largest family of receptor tyrosine kinases (RTKs). (silverchair.com)
  • Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3 , FGFR1-4 , PDGFR , KIT , and RET , shows potent antitumor activities. (medchemexpress.com)
  • Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC 50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3 , PDGFRβ , Kit , RET and Raf-1 , respectively. (medchemexpress.com)
  • Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ ABL , v-Abl , PDGFR and c-kit kinase activity. (medchemexpress.com)
  • KBP-7018 is a tyrosine kinase-selective inhibitor. (medchemexpress.com)
  • Labuxtinib is c-kit tyrosine kinase inhibitor. (medchemexpress.com)
  • CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. (medchemexpress.com)
  • Bortezomib restores expression of FoxO3a in imatinib resistant T315I cells The T315I BCR ABL mutation frequently occurs in CML patients that are resistant to imatinib, and even remains refractory to the more potent second generation kinase inhibitors. (mi-rna.com)
  • First-generation EGFR TKIs, binding competitively and reversibly to the ATP-binding site of the EGFR tyrosine kinase domain, have resulted in a significant improvement in outcome for NSCLC patients with activating EGFR mutations (L858R and Del19). (researchgate.net)
  • However, 25% to 30% of patients with EGFR -activating mutations show intrinsic resistance, and the responders invariably acquire resistance to gefitinib. (aacrjournals.org)
  • The BDTX-1535 expansion cohort portion of the study will assess single-agent objective response rate (ORR) in a second- or third-line setting in NSCLC patients with EGFR intrinsic driver and/or acquired resistance mutations, who have received prior treatment with approved EGFR TKI. (drug-dev.com)
  • The dosing of the first patients in the expansion cohorts follows the company's initial data readout from the dose escalation portion of the BDTX-1535 Phase 1 clinical study, which demonstrated clinical proof of activity through radiographic responses in NSCLC patients harboring diverse types of EGFR mutations including intrinsic driver and post-osimertinib acquired resistance EGFR mutations. (drug-dev.com)
  • Emergence of intrinsic driver and acquired resistance EGFR mutations to osimertinib represents a significant unmet need for patients with EGFR-mutant lung cancer. (drug-dev.com)
  • Thirteen percent of patients in the US with EGFR mutation-positive NSCLC show presence of intrinsic driver mutations, which are associated with worse clinical outcomes when treated with currently approved EGFR TKIs. (drug-dev.com)
  • The company is advancing BDTX-1535 as a potential targeted therapy option for patients with this broad spectrum of EGFR mutations in second-line NSCLC, and plans to investigate safety and efficacy in a first-line setting in NSCLC patients with intrinsic driver EGFR mutations after discussion with the US FDA. (drug-dev.com)
  • EGFR dimerization stimulates its intrinsic intracellular protein-tyrosine kinase activity. (egfr-inhibitor.com)
  • Instead, it is phosphorylated on tyrosine residues after complexing with other proteins. (wikipedia.org)
  • Upon binding, the tyrosine residues in the signaling motifs are phosphorylated by membrane-associated tyrosine kinases. (encyclopedia.pub)
  • FN2 is followed by a transmembrane (TM) helix, and an intracellular part consisting of a juxtamembrane (JM) region with several conserved tyrosine (Y) residues, a tyrosine kinase domain, a sterile-α motif (SAM) protein-protein interaction domain, and a C-terminal Psd-95, Dlg and ZO1 domain (PDZ)-binding motif ( Pasquale, 2008 ). (silverchair.com)
  • Upon activation of protein kinase C by phorbol ester, CD4 is phosphorylated on cytoplasmic serine residues and internalized from the cell surface, and disruption of the CD4- p56(lck) complex occurs. (mssm.edu)
  • These events are influenced by and activate other molecular pathways, including phosphatidylinositol 3-kinase (PI3K), mammalian target of rapamycin (mTOR), and mitogen-activated protein kinase (MAPK),[2] and therapies are now available that target these pathocellular processes. (cancernetwork.com)
  • Insulin-induced phosphatidylinositol 3-kinase (PI3K)/Akt signaling and interleukin-6 (IL-6)-instigated JAK/STAT3-signaling pathways in the liver inhibit the expression of gluconeogenic genes to decrease hepatic glucose output. (diabetesjournals.org)
  • Similarly, the phosphatidylinositol-3-kinase (PI-3K) pathway is directly or indirectly activated by most ErbBs. (genome.jp)
  • Mutations in the PIK3R1 gene encoding phosphatidylinositol 3-kinase (PI3-kinase) have been found to cause severe insulin resistance [Baynes et al. (lu.se)
  • Polycythemia is categorized as primary or secondary due to intrinsic or extrinsic changes, respectively, to erythroid progenitors and RBCs. (medscape.com)
  • Pigmented entities are relatively common in the oral mucosa and arise from intrinsic and extrinsic sources. (medscape.com)
  • Similar to other family members it possesses a highly glycosylated extracellular region comprised of five immunoglobulin domains (D1-D5 498 amino acids) a transmembrane domain name (21 amino acids) and an intracellular area made up of a juxtamembrane area GSI-IX (JMD) (36 proteins) and an intracellular tyrosine GSI-IX kinase area (398 proteins) that's interrupted with a kinase put area (73 proteins) (Fig. 1A) (Coussens et al. (techblessing.com)
  • The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. (genome.jp)
  • Monoclonal antibody therapy has been developed over the past 30 years to target receptor tyrosine kinases (RTKs), which sit on the outer membrane of cancerous cells. (wisc.edu)
  • It contains an intrinsic protein-tyrosine kinase activity. (rush.edu)
  • The receptor contains an intrinsic TYROSINE KINASE domain that is located within the beta subunit. (bvsalud.org)
  • gp130 has no intrinsic tyrosine kinase activity. (wikipedia.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)
  • RON is a 180-kDa heterodimeric protein composed of a 40-kDa α-chain and a 150-kDa transmembrane β-chain with intrinsic tyrosine kinase activity. (spandidos-publications.com)
  • Maturation occurs in the cell membrane resulting in a 180-kDa heterodimeric protein composed of a 40-kDa α-chain and a 150-kDa transmembrane β-chain with intrinsic tyrosine kinase activity ( 5 , 6 ). (spandidos-publications.com)
  • When c-Kit binds to stem cell factor (SCF) it forms adimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. (medchemexpress.com)
  • 1987) of the CSF-1 receptor (CSF-1R) and the demonstration that it possessed intrinsic tyrosine kinase activity (Yeung et al. (techblessing.com)
  • RASA1 acts by enhancing the intrinsic GTPase activity of Ras, leading to hydrolysis of bound GTP to GDP and down regulation of Ras activity [Gold, et al. (lu.se)
  • Noonan syndrome (NS) is caused by mutations in PTPN11 , a gene encoding the nonreceptor protein tyrosine phosphatase SHP2. (lu.se)
  • Primary polycythemias are due to factors intrinsic to red cell precursors caused by acquired or inherited mutations. (medscape.com)
  • X-linked agammaglobulinemia (XLA) is an immunodeficiency caused by mutations in the gene coding for Bruton's tyrosine kinase (BTK) [Väliaho et al. (lu.se)
  • ZAP-70 deficiency is a rare autosomal recessive form of severe combined immunodeficiency (SCID) caused by mutations in the gene coding for T cell receptor z-chain associated protein kinase [ Chan et al. (lu.se)
  • Regional differences in the intrinsic regulation of resident myeloid cell populations may mediate susceptibility to lesion formation. (listlabs.com)
  • In experiments probing for a role of PKCa in human laminin-2-integrin-mediated cell adhesion and spreading of PC12 cells, we observed unexpected enhancements of adhesion, spreading and stress fiber formation to 1 mM Go¨6976 with concomitant increase in membrane translocation of PKCd and autophosphorylation of focal adhesion kinase (FAK). (mirnamimic.com)
  • My laboratory is focused on understanding mechanisms of resistance to molecular targeting agents directed against receptor tyrosine kinases. (wisc.edu)
  • However, despite initial response, acquired and intrinsic resistance to this promising molecular therapeutic eventually develops. (wisc.edu)
  • Background Multiple medication resistance (MDR) of cancer cells is the main reason of intrinsic or acquired insensitivity to chemotherapy in many cancers. (scienceexhibitions.org)
  • CD4 is noncovalently associated via the cytoplasmic domain with the protein-tyrosine kinase p56(lck), a member of the src protein-tyrosine kinase family. (mssm.edu)
  • Using this, we showed that the tyrosine kinase ZAP-70, which is critical for T cell signaling, discriminates substrates through an electrostatic selection mechanism encoded within its catalytic domain (Shah et al. (escholarship.org)
  • PKC family of serine-threonine kinases plays key roles in many of the signaling pathways that control cellular function, including those mediated through integrin signaling. (mirnamimic.com)
  • Here, we show that the non-receptor Src family tyrosine kinases, SRC64B and SRC42A, are involved in WNT5-mediated signaling through Derailed in the Drosophila embryonic central nervous system. (biologists.com)
  • Here, we show that plexin-B family members stably associate with the receptor tyrosine kinase ErbB-2. (rupress.org)
  • Using this approach, we find a difference in the electrostatic recognition of substrates between the closely related Src-family kinases Lck and c-Src. (escholarship.org)
  • Members of the Non-catalytic tyrosine-phosphorylated receptor family share a couple of common features. (encyclopedia.pub)
  • We have found that Axl and Mer, two members of the TAM family of tyrosine kinases, are highly expressed on microglia in the hindbrain, compared to the spinal cord, both during homeostasis and at EAE onset. (listlabs.com)
  • Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. (drugbank.com)
  • Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. (medchemexpress.com)
  • It interacts with Janus kinases to elicit an intracellular signal following receptor interaction with its ligand. (wikipedia.org)
  • These results point to the importance of direct recognition at the kinase active site in fine-tuning specificity. (escholarship.org)
  • Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. (drugbank.com)