• Several inhibitors of Src have been developed as anti-cancer drugs. (umbc.edu)
  • After activation of different receptors at the cell surface, this dimeric protein serves as a platform for assembling other adaptors such as FYB and some SRC family kinase members, although these mechanisms are still poorly understood. (oncotarget.com)
  • Tyrosine-protein kinase BLK, also known as B lymphocyte kinase, is a non-receptor tyrosine kinase that in humans is encoded by the BLK gene. (wikipedia.org)
  • The tyrosine-protein kinase BLK has been shown to interact with UBE3A. (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • Src contains at least three flexible protein domains, which, in conjunction with myristoylation, can mediate attachment to membranes and determine subcellular localization. (wikipedia.org)
  • This gene is a member of the protein-tyrosine kinase oncogene family. (cancerindex.org)
  • The protein associates with the p85 subunit of phosphatidylinositol 3-kinase and interacts with the fyn-binding protein. (cancerindex.org)
  • These compounds exhibit high selectivity for SFKs over a panel of recombinant protein kinases, excellent pharmacokinetics, and in vivo activity following oral dosing. (rcsb.org)
  • In the resultant ETV6/FRK fusion protein, the entire PNT oligomerization domain of ETV6 and the kinase domain of FRK are fused in frame. (atlasgeneticsoncology.org)
  • SH3 (Src Homolgy 3) domains are small protein modules of about 50-60 residues. (eu.org)
  • Association of p62, a multifunctional SH2- and SH3-domain-binding protein, with src family tyrosine kinases, Grb2, and phospholipase C gamma-1. (eu.org)
  • ASAP1, a phospholipid-dependent arf GTPase-activating protein that associates with and is phosphorylated by Src. (eu.org)
  • Scar/WAVE-1, a Wiskott-Aldrich syndrome protein, assembles an actin-associated multi-kinase scaffold. (eu.org)
  • The Src-homology 3 (SH3) region is a protein domain consisting of approximately 60 residues. (rcsb.org)
  • Src and other Src family protein tyrosine kinases are proto-oncogenes that play key roles in regulating cell growth and differentiation. (rndsystems.com)
  • Catalytic domain of the Protein Tyrosine Kinase, Src. (umbc.edu)
  • The PTKc family is part of a larger superfamily that includes the catalytic domains of other kinases such as protein serine/threonine kinases, RIO kinases, and phosphoinositide 3-kinase (PI3K). (umbc.edu)
  • PTKs catalyze the transfer of the gamma-phosphoryl group from ATP to tyrosine (tyr) residues in protein substrates. (umbc.edu)
  • c-Src is the vertebrate homolog of the oncogenic protein (v-Src) from Rous sarcoma virus. (umbc.edu)
  • Rapid detection of intracellular SH2D1A protein in cytotoxic lymphocytes from patients with X-linked lymphoproliferative disease and their family members. (lu.se)
  • src-family tyrosine kinase p55fgr is expressed in murine splenic B cells and is activated in response to antigen receptor cross-linking. (aai.org)
  • One of the earliest and most critical events following Ag receptor cross-linking is the activation of receptor-associated tyrosine kinases, which phosphorylate a variety of substrates involved in transducing signals generated through the receptor. (aai.org)
  • We also show that Fgr, like other B cell kinases, is activated in response to cross-linking of the Ag receptor. (aai.org)
  • Unlike these other kinases, however, Fgr does not appear to be physically associated with the receptor, and does not become activated until several minutes after stimulation. (aai.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)
  • 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)
  • SRC is the prototype for a family of genes that encode non-receptor tyrosine kinases implicated in a variety of cellular processes. (atlasgeneticsoncology.org)
  • Tau interacts with src-family non-receptor tyrosine kinases. (eu.org)
  • Exhibits selectivity for Fgr and Lyn over other Src family kinases and other nonreceptor and receptor tyrosine kinases. (tocris.com)
  • Src (or c-Src) is a cytoplasmic (or non-receptor) tyr kinase, containing an N-terminal SH4 domain with a myristoylation site, followed by SH3 and SH2 domains, a tyr kinase domain, and a regulatory C-terminal region with a conserved tyr. (umbc.edu)
  • Src kinase family is a family of non-receptor tyrosine kinases. (srcsignaling.com)
  • Identification of two SH3-binding motifs in the regulatory subunit of phosphatidylinositol 3-kinase. (eu.org)
  • Together with other Src subfamily proteins, it is involved in signaling pathways that regulate cytokine and growth factor responses, cytoskeleton dynamics, cell proliferation, survival, and differentiation. (umbc.edu)
  • Demographic and that this particular family of angiogenic clinical data were collected during routine proteins plays an important role in placental obstetric visits. (who.int)
  • Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for cancer progression. (rcsb.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)
  • Meltrin alpha cytoplasmic domain interacts with SH3 domains of Src and Grb2 and is phosphorylated by v-Src. (eu.org)
  • Analysis of conformational changes associated with activation/inhibition of SRC family members, presently limited to their effect on kinase activity, is extended to their interactive network, which paves the way for therapeutic development. (oncotarget.com)
  • Die Rolle von Src-Kinasen wurde durch pharmakologische Inhibition analysiert. (uni-wuerzburg.de)
  • Außerdem konnte demonstriert werden, dass die Inhibition von Src-Kinasen den Anstieg der Endothelpermeabilität signifikant reduziert. (uni-wuerzburg.de)
  • the second activates Bruton tyrosine kinase and Syk. (medscape.com)
  • Identification of Bruton tyrosine kinase mutations in 12 Chinese patients with X-linked agammaglobulinaemia by long PCR-direct sequencing. (lu.se)
  • We report here a novel subseries of C-5-substituted anilinoquinazolines that display high affinity and specificity for the tyrosine kinase domain of the c-Src and Abl enzymes. (rcsb.org)
  • N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. (rcsb.org)
  • Mutations in c-Src could be involved in the malignant progression of colon cancer. (wikipedia.org)
  • 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)
  • Two patients with truncating mutations had liver fibrosis that in one patient resolved on treatment with the Src kinase inhibitor dasatinib. (nature.com)
  • Members of the RYK/Derailed family have recently been shown to regulate axon guidance in both Drosophila and mammals by acting as Wnt receptors. (biologists.com)
  • The activation of the c-Src pathway has been observed in about 50% of tumors from colon, liver, lung, breast and the pancreas. (wikipedia.org)
  • 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)
  • 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)
  • In 1979, J. Michael Bishop and Harold E. Varmus discovered that normal chickens possess a gene that is structurally closely related to v-Src. (wikipedia.org)
  • The normal cellular gene was called c-src (cellular-src). (wikipedia.org)
  • It is believed that at one point an ancestral virus mistakenly incorporated the c-Src gene of its cellular host. (wikipedia.org)
  • Identification of a SRC-like tyrosine kinase gene, FRK, fused with ETV6 in a patient with acute myelogenous leukemia carrying a t(6;12)(q21;p13) translocation. (atlasgeneticsoncology.org)
  • and liver fibrosis resolved on treatment with the Src kinase inhibitor dasatinib. (nature.com)
  • c-Src is made up of 6 functional regions: Src homology 4 domain (SH4 domain), unique region, SH3 domain, SH2 domain, catalytic domain and short regulatory tail. (wikipedia.org)
  • De novo variant in tyrosine kinase SRC causes thrombocytopenia: case report of a second family. (bvsalud.org)
  • Antitumor activity of NVP-BKM120- a selective pan class 1 PI3 Kinase inhibitor showed differential forms of cell death based on P53 status of glioma cells. (mdanderson.org)
  • The crystal structures of spectrin and Fyn SH3 domains as well as the solution structure of the Src SH3 domain show that these all have the same basic fold. (rcsb.org)
  • These loops are different in tyrosine kinase and spectrin SH3 domains. (rcsb.org)
  • Although previous studies have suggested that Fgr expression in the mouse is restricted to cells of the myeloid lineage, we demonstrate that highly purified murine splenic B cells express the kinase as well. (aai.org)
  • Wnt-5a/Ca2+-induced NFAT activity is counteracted by Wnt-5a/Yes-Cdc42-casein kinase 1alpha signaling in human mammary epithelial cells. (atlasgeneticsoncology.org)
  • An elevated level of activity of c-Src is suggested to be linked to cancer progression by promoting other signals. (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • It has been shown that ETV6/FRK is an oncoprotein with dual functions: deregulated tyrosine kinase activity and a dominant-negative modulation of transcriptional repression by ETV6. (atlasgeneticsoncology.org)
  • Elevated levels of Src kinase activity have been reported in a variety of human cancers. (umbc.edu)
  • 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)
  • 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)
  • 8000 Bahía Blanca, Argentina In the present work, we examined the role of ATP in the activation of the MAP kinases (MAPKs) ERK1/2, JNK1/2 and p38 and their involvement in the modulation of transcription factors and proliferation of human colon cancer Caco-2 cells. (conicet.gov.ar)
  • Src also play a role in regulating cell adhesion, invasion, and motility in cancer cells and tumor vasculature, contributing to cancer progression and metastasis. (umbc.edu)
  • Herein, a fine-tuning between the binding of SRC kinases and their activation was identified. (oncotarget.com)
  • 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)
  • Src is also implicated in acute inflammatory responses and osteoclast function. (umbc.edu)
  • AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily. (rcsb.org)
  • These findings provide new molecular basis for further understanding the mechanisms involved in ATP functions, as a signal transducer and activator of MAP kinase cascades, in Caco-2 cells derived from human colon adenocarcinoma. (conicet.gov.ar)
  • The mammalian orthologs of Derailed and SRC64B also form complexes, suggesting that Src roles in RYK signaling are conserved. (biologists.com)
  • The SRC Kinase Adaptor Phosphoprotein 2 (SKAP2) is a broadly expressed adaptor associated with the control of actin-polymerization, cell migration, and oncogenesis. (oncotarget.com)
  • Differential trafficking of Src, Lyn, Yes and Fyn is specified by the state of palmitoylation in the SH4 domain. (atlasgeneticsoncology.org)
  • Taxol-induced TRPV4-mediated hyperalgesia and the enhanced osmotransduction in cultured nociceptors were dependent on integrin/Src tyrosine kinase signaling. (jneurosci.org)
  • We also demonstrate that Taxol-induced TRPV4-mediated hyperalgesia is essentially dependent on integrin/Src tyrosine kinase signaling. (jneurosci.org)
  • TWIK-related acid-sensitive potassium channel 1 (TASK-1 encoded by KCNK3) belongs to the family of two-pore domain potassium channels. (ersjournals.com)
  • FRK belongs to a family of SRC kinases. (atlasgeneticsoncology.org)