• Examination of the different signaling cascades induced by RTKs established Ras/mitogen-activated protein kinase (MAPK), PI-3 kinase, and phospholipase-γ (PLCγ) pathways as key downstream mediators of PDGFR signaling. (wikipedia.org)
  • Nuclear localized HER family receptor tyrosine kinases (RTKs) have been observed in primary tumor specimens and cancer cell lines for nearly two decades. (plos.org)
  • The ErbB/HER family of receptor tyrosine kinases (RTKs) consists of four family members: the epidermal growth factor receptor (EGFR/ErbB1), HER2 (ErbB2/Neu), HER3 (ErbB3), and HER4 (ErbB4). (plos.org)
  • This family of RTKs has been highly implicated in the formation and progression of various cancers via aberrant overexpression, kinase activation, and mutation [1] , [2] . (plos.org)
  • While the classical membrane-bound functions of HER family RTKs have been extensively studied, accumulating data suggest that these receptors can be found in the cell's nucleus where they can function as co-transcriptional activators [4] , [5] . (plos.org)
  • Ras signaling is activated by cellular receptors including receptor tyrosine kinases (RTKs), G-protein coupled receptors (GPCRs), cytokines receptors, and extracellular matrix receptors [ 12 ] . (encyclopedia.pub)
  • However, over recent years, it became clear that RTKs cannot be sufficiently activated by growth factors or receptor agonists in the adult and aging brain to exert significant neuroprotective or neurorestorative effects. (springer.com)
  • 2003 Stokowski and Cox 2000 Although the exact mechanisms by which Merlin confers contact dependent inhibition of cell growth remain unclear it appears to involve rules of receptor tyrosine kinases (RTKs) and downstream mitogen-activated protein kinase (MAPK) pathways. (hiv-proteases.com)
  • Several recent studies possess illustrated that loss of Merlin prospects to build up of RTKs in the cell surface possibly due to problems in receptor trafficking (Ammoun et al. (hiv-proteases.com)
  • Recent data suggest that integrin association with RTKs might also protect the latter against the activity of phosphatases (17, 19) and/or ensure the correct subcellular juxtaposition of cytoplasmic tails of dimer-ized growth factor receptors (17). (123dok.org)
  • EphRs comprise the largest subfamily of receptor tyr kinases (RTKs). (umbc.edu)
  • Eph receptors constitute the largest family of receptor tyrosine kinases (RTKs). (silverchair.com)
  • Canonical Notch signaling activates the transcription of BMI1 proto‑oncogene polycomb ring finger, cyclin D1, CD44, cyclin dependent kinase inhibitor 1A, hes family bHLH transcription factor 1, hes related family bHLH transcription factor with YRPW motif 1, MYC, NOTCH3, RE1 silencing transcription factor and transcription factor 7 in a cellular context‑dependent manner, while non‑canonical Notch signaling activates NF‑κB and Rac family small GTPase 1. (spandidos-publications.com)
  • p27(Kip1) is a cyclin-dependent kinase inhibitor. (biomedcentral.com)
  • The cyclin-dependent kinase (CDK) inhibitor p27(Kip1) is a key cell-cycle regulator of G1-to-S phase transition [ 1 ]. (biomedcentral.com)
  • Sunitinib (marketed as Sutent by Pfizer, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor. (ncats.io)
  • Sunitinib was evaluated for its inhibitory activity against a variety of kinases and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony-stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET). (ncats.io)
  • SUTENT is a kinase inhibitor indicated for the treatment of: Gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate. (ncats.io)
  • Patients with EGFR-mutant NSCLC can derive significant benefit from EGFR tyrosine kinase inhibitor (TKI) therapy, including the third-generation EGFR TKI osimertinib. (bvsalud.org)
  • Turalio (pexidartinib) is a kinase inhibitor indicated for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT) associated with severe morbidity or functional limitations and not amenable to improvement with surgery. (rxlist.com)
  • Pexidartinib is a kinase inhibitor. (rxlist.com)
  • Our data reveal that Pyk2 couples the activation mGluRs to the mitogen-activated protein kinase pathway even though it attenuates mGluR1-dependent G protein signaling. (uwo.ca)
  • Small‑molecule γ‑secretase inhibitors (AL101, MRK‑560, nirogacestat and others) and antibody‑based biologics targeting Notch ligands or receptors [ABT‑165, AMG 119, rovalpituzumab tesirine (Rova‑T) and others] have been developed as investigational drugs. (spandidos-publications.com)
  • Small-molecule inhibitors, antagonistic monoclonal antibodies (mAbs), antibody-drug conjugates (ADCs), bispecific antibodies or biologics (bsAbs) and chimeric antigen receptor-modified T cells (CAR-Ts) targeting Notch signaling components have been developed as investigational anti-cancer drugs ( 10 - 12 ). (spandidos-publications.com)
  • Among them are the Sprouty proteins which mainly act as inhibitors of growth factor-dependent neuronal and glial signaling pathways. (springer.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)
  • The treatment paradigm of AML patients harboring FLT3 mutations (30%) has been modified by the discovery of tyrosine kinase inhibitors. (dovepress.com)
  • Activity of these inhibitors depends on their mechanism of receptor binding (active vs inactive conformation) and efficacy against the FLT3-ITD and -TKD mutations (type 1 inhibitors are active both on FLT3 -ITD and TKD, whereas type 2 inhibitors are active only on FLT3 -ITD). (dovepress.com)
  • 0.05) of control values by the phosphatidylinositol 3-kinase (PI3-K) inhibitors LY294002 (25 μmol/l) and wortmannin (100 nmol/l), respectively. (diabetesjournals.org)
  • It belongs to a class of drugs known as kinase inhibitors. (ndclist.com)
  • Targeting the MET tyrosine kinase domain in the setting of MET exon 14 mutations using effective MET tyrosine kinase inhibitors is a current targeted therapy option for patients with metastatic lung cancer. (bvsalud.org)
  • In this Review, we focus on the management of patients with MET exon 14 skipping alterations by addressing the biology of the MET receptor and exon 14 skipping mutations, current treatment strategies, and sequential treatment options based on resistance mechanisms to MET inhibitors in patients with non-small-cell lung cancer. (bvsalud.org)
  • Inhibitors for c-Met and RON including small molecular weigh kinase inhibitors and neutralizing antibodies are in pre-clinical investigation and clinical trials. (oncotarget.com)
  • Several of the tyrosine kinase inhibitors have activity against both c-Met and RON kinases whereas the antibodies generally are target specific. (oncotarget.com)
  • The extracellular region of the receptor consists of five immunoglobulin-like domains while the intracellular part is a tyrosine kinase domain. (wikipedia.org)
  • Phosphorylated tyrosine residues recruit various intracellular adaptor and effector molecules that result in the propagation of growth promoting signal transduction cascades [1] , [2] . (plos.org)
  • Insulin receptor, with the extracellular portion at the top, intracellular portion at the bottom, and the cell membrane shown schematically in gray. (rcsb.org)
  • Ras proteins are membrane-bound small GTPases that act as molecular transducers, coupling cell surface receptors to intracellular effector pathways to regulate cellular processes such as cell proliferation, differentiation, migration, and apoptosis [ 3 ] [ 4 ] . (encyclopedia.pub)
  • In recent years, the search for intracellular signaling integrator downstream of receptor tyrosine kinases provided valuable novel substrates. (springer.com)
  • This results in the release of Ca2+ from intracellular stores and the activation of protein kinase C. The activation of Group I mGluRs also results in ERK1/2 phosphorylation. (uwo.ca)
  • Pyk2 also interacts with GST-fusion proteins corresponding to the second intracellular loop and the distal carboxyl-terminal tail domains of mGluR1a. (uwo.ca)
  • CCK4, also called protein tyrosine kinase 7 (PTK7), is an orphan receptor tyr kinase (RTK) containing an extracellular region with seven immunoglobulin domains, a transmembrane segment, and an intracellular inactive pseudokinase domain. (umbc.edu)
  • Its activity is directed by intracellular signals mediated by various types of receptors such as G protein-coupled receptors. (embl-heidelberg.de)
  • In turn, high levels of cyctoplasmic calcium may trigger mbrane trafficking and transport of viral ER-associated proteins to viroplasms, sites of viral genome replication .Protein 2C: Induces and associates with structural rearrangents of intracellular mbranes. (enquirebio.com)
  • Moreover, Eph/ephrin signalling can be bi-directional, with intracellular pathways operating downstream of both the Eph receptor (forward signalling) and the ephrin ligand (reverse signalling) ( Kullander and Klein, 2002 ). (silverchair.com)
  • 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)
  • Tyrosine phosphorylation sites in growth factor receptors serve two major purposes-to control the state of activity of the kinase and to create binding sites for downstream signal transduction molecules, which in many cases also are substrates for the kinase. (wikipedia.org)
  • As an indicator of downstream apoptotic events in response to bortezomib treatment, the protein expression of BIM splice variant was increased upon bortezomib treatment. (mi-rna.com)
  • 2007 The entire activation of ERK needs the phosphorylation of c-Raf (serine 338) and MEK1 (serine 298) with the p21-turned on kinases (Paks) the instant downstream effectors of Rac1 (Beeser et al. (hiv-proteases.com)
  • L-783,281-induced activation of IRTK stimulates downstream signaling proteins, including insulin receptor substrate 1 (IRS-1), Akt, and phosphatidylinositol 3-kinase (PI3-K). L-783,281 also induces glucose uptake in a dose-dependent manner from rat primary adipocytes and soleus muscle tissue from lean mice. (diabetesjournals.org)
  • Following this, ATP can bind to the tyrosine kinase domain on the cytoplasmic side of EGFR, leading to the phosphorylation of the receptor, and activation of downstream signalling through pathways such as the PI3K/AKT/mTOR and RAS/RAF/ MAPK pathways (fig. 2). (janssenmedicalcloud.com)
  • Here, potential mechanisms involving alterations in T-cell receptor expressions, postreceptor downstream signalling, epigenetics, and oxidative stress which favour activation of lupus T cells will be discussed. (hindawi.com)
  • Phenotypic and functional alterations in lupus T cells including expansion of the Th17 population, perturbations of the physiology of T-cell receptors (TCRs) and postreceptor downstream signalling, oxidative stress, and epigenetic changes result in exaggeration of TCR response to stimuli and the propensity of lupus T cells to get activated [ 6 ]. (hindawi.com)
  • This protein regulates signal transducing molecules, which include members of the Srckinase family of non-receptor tyrosine kinases, serine/threonine kinases and transcription factors. (eurekaselect.com)
  • HGF is secreted as a single inactive polypeptide and is cleaved by serine proteases into a 62-kDa heavy-chain and 32-36-kDa light-chain. (qkine.com)
  • Under growth-permissive (sparse) conditions Merlin is definitely phosphorylated by p21-triggered kinase 1 (Pak1) or cAMP-dependent kinase A (PKA) on serine 518 within its C-terminal tail (Alfthan et al. (hiv-proteases.com)
  • The PTKc (catalytic domain) family, to which this subfamily belongs, includes the catalytic domains of other kinases such as protein serine/threonine kinases, RIO kinases, and phosphoinositide 3-kinase (PI3K). (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)
  • Platelet-derived growth factor receptors (PDGF-R) are cell surface tyrosine kinase receptors for members of the platelet-derived growth factor (PDGF) family. (wikipedia.org)
  • As an alternative approach, growth factor receptors or components of their signal transduction machinery may be targeted directly. (springer.com)
  • As to the basis for their collaboration, integrins and growth factor receptors may form macromolecular complexes on the cell membrane (7, 8, 13, 16 -18). (123dok.org)
  • Typical products of proto-oncogenes are signaling molecules, growth factors or growth factor receptors. (wikilectures.eu)
  • Membrane-bound HER receptors activate numerous tumor promoting signaling cascades via this mechanism, including the PI3K/AKT, Ras/Raf/Mek/Erk, PLCγ/PKC, and signal transducer and activator of transcription (STAT) pathways [1] , [2] . (plos.org)
  • Tyrosine-kinase receptor is effective when the cell needs to regulate and coordinate a variety of activities and trigger several signal pathways at once. (vdocuments.net)
  • ADP ribosylation factors (ARFs), which are members of the Ras superfamily of GTP-binding proteins, are critical components of vesicular trafficking pathways in eukaryotes. (embl.de)
  • Dysregulation of the MET receptor leads to cell proliferation and survival by activation of the PI3K-AKT-TOR and RAS-RAF-MET-ERK canonical pathways. (bvsalud.org)
  • EGFR is a tyrosine kinase receptor member of the ERBB family that regulates signalling pathways that control cell growth, motility, and survival (fig. 1). (janssenmedicalcloud.com)
  • Additionally, Ras proteins are recognized as major oncogenes, as mutations in all three Ras genes occur in approximately 30% of human cancers [ 10 ] . (encyclopedia.pub)
  • Several skeletal dysplasias in specific dog breeds have been associated with mutations in members of the collagen gene family or its binding proteins ( 8 - 10 ), fibrilin related protein ( 11 ), as well as an altered sulfate transporter protein ( 12 ). (frontiersin.org)
  • The recruitment of Merlin to cell junctions is vital for its tumor suppressive function as patient-derived mutations that impair Merlin junctional localization render the protein inactive (Deguen et al. (hiv-proteases.com)
  • Proto-oncogene changes to oncogene mainly by somatic point mutations, gene amplifications, or chromosomal translocations that bring proto-oncogene under control of differentially expressed protein. (wikilectures.eu)
  • Several oncogenic mechanisms have been identified for MET, including MET amplification, fusions, mutations in the tyrosine kinase domain and exon 14 skipping alterations. (bvsalud.org)
  • Aberrant expression and activities of c-Met and RON in cancer are attributed to various mechanisms including increased expression of their ligands or receptors and by activating mutations [ 4 , 15 ]. (oncotarget.com)
  • Mutations in the RON and c-Met promoters are known to enhance transcription and point mutations have been identified that enhance tyrosine kinase activity [ 19 - 21 ]. (oncotarget.com)
  • Many EGFR mutations result in the constitutive activation of EGFR (where the receptor is always switched "on"), even in the absence of a binding ligand, which drives tumour growth and survival. (janssenmedicalcloud.com)
  • In conjunction with dimerization and kinase activation, the receptor molecules undergo conformational changes, which allow a basal kinase activity to phosphorylate a critical tyrosine residue, thereby "unlocking" the kinase, leading to full enzymatic activity directed toward other tyrosine residues in the receptor molecules as well as other substrates for the kinase. (wikipedia.org)
  • The phosphorylated tyrosine residue and in general three adjacent C-terminal amino acid residues form specific binding sites for signal transduction molecules. (wikipedia.org)
  • The specificity of these interactions appears to be very high, since mutant receptors carrying phenylalanine residues in one or several of the different phosphorylation sites generally lack the capacity to bind the targeted signal transduction molecule. (wikipedia.org)
  • This process leads to the activation of each receptors' tyrosine kinase and the subsequent phosphorylation of tyrosine residues located on their C-terminal tails. (plos.org)
  • Porcine Recombinant Protein HGF differs from human HGF at several key amino acid residues that are predicted to affect bioactivity and receptor binding. (qkine.com)
  • PTKs catalyze the transfer of the gamma-phosphoryl group from ATP to tyrosine (tyr) residues in protein substrates. (umbc.edu)
  • The proteins encoded by members of the Dbl family share a common domain, presented in this entry, of about 200 residues (designated the Dbl homology or DH domain) that has been shown to encode a GEF activity specific for a number of Rho family members. (embl-heidelberg.de)
  • Ras proteins are the founding members of the Ras superfamily of GTPases, which in humans is composed of more than 150 members [ 1 ] [ 2 ] . (encyclopedia.pub)
  • Like all members of the Ras superfamily, the Rho proteins cycle between active GTP-bound and inactive GDP-bound conformational states. (embl-heidelberg.de)
  • The details are complex and involve phosphorylation of the receptor and its substrates, modifying their action in insulin signaling. (rcsb.org)
  • Mainly cytosolic, this protein is expressed at extraordinary levels and participates in the folding of specific protein substrates. (eurekaselect.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)
  • Ligand binding activates the receptor kinase through a process of oligomerization and transphosphorylation. (utsouthwestern.edu)
  • This activates the tyrosine-kinase section of both. (vdocuments.net)
  • b) 4-Hydroxytamoxifen (but not tamoxifen), genistein (but not genistin), daidzein, and probably other nutritional and chemopreventive anti-cancer agents could up-regulate expression of p27 via receptor protein tyrosine kinases (RPTKs), phosphoinositide 3-kinase (PI3K), phosphoinosite-dependent kinase (PDK), Akt/PKB and mTOR. (biomedcentral.com)
  • They first phosphorylate and activate each other, and then phosphorylate other proteins in the signaling network inside the cell. (rcsb.org)
  • Dimerization is a prerequisite for the activation of the kinase. (wikipedia.org)
  • Classically, HER family members function from the cell surface, where binding to cognate ligands can induce receptor homo- or hetero-dimerization with other HER family receptors [3] . (plos.org)
  • The HER2 receptor does not bind to any known ligands, however, its dimerization arm is innately positioned in an open conformation. (plos.org)
  • Receptor dimerization and autophosphorylation attracts proteins containing Src homology 2 (SH2) or phosphotyrosine binding (PTB) domains including adaptor proteins like FRS2 and GRB2. (springer.com)
  • The PDGFs bind to the protein tyrosine kinase receptors PDGF receptor-α and -β. (wikipedia.org)
  • PDGF-AA binds only to PDGFR-αα, while PDGF-BB is the only PDGF that can bind all three receptor combinations with high affinity. (wikipedia.org)
  • Other signaling proteins (a small peptide from one is shown in pink) then bind and are phosphorylated on their tyrosine amino acids. (rcsb.org)
  • In general, class EphA receptors bind GPI-anchored ephrin-A ligands. (umbc.edu)
  • When ligands (small molecules that bind specifically to a larger molecule) attach to the receptor protein, the receptor typically undergoes a change in shape. (vdocuments.net)
  • When ligands bind to two receptors polypeptides, the polypeptides bind, forming a dimer. (vdocuments.net)
  • In the trans-Golgi network (TGN), phosphorylated lysosomal enzymes bind to M-6-P receptors, which direct the enzymes into clathrin-coated vesicles. (biomedcentral.com)
  • What proteins does IRS-1 bind to in order to activate Raf-1? (flashcardmachine.com)
  • They exclusively bind membrane-tethered ligands known as ephrin proteins. (silverchair.com)
  • Typically, EphA receptors bind to glycosylphosphatidylinositol anchor (GPI)-linked ephrin A proteins and EphB receptors bind to transmembrane ephrin B proteins. (silverchair.com)
  • About 25% of breast cancer patients show overexpression of HER2 receptor caused mainly by HER2 gene amplification. (wikilectures.eu)
  • The receptor for insulin is a large protein that binds to insulin and passes its message into the cell. (rcsb.org)
  • Two copies of the protein chains come together on the outside of the cell to form the receptor site that binds to insulin. (rcsb.org)
  • When insulin binds to the receptor, it is thought to cause a change in shape that is propagated inside the cell, activating the tyrosine kinases. (rcsb.org)
  • Surprisingly, insulin binds to the outer edge of the receptor, and typically only binds to one side of the symmetrical receptor. (rcsb.org)
  • In the inactive state (shown on the left, PDB entry 1irk ), a mobile loop (in bright turquoise) binds in the active site, blocking its action. (rcsb.org)
  • KRAS binds to GTP in its active form and once it cleaves the terminal phosphate of the nucleotide it releases GDP and becomes inactive. (wikilectures.eu)
  • activated by binding with an extracellular signal molecule, the receptor binds to an inactive G protein in membrane. (vdocuments.net)
  • The G protein then binds with another membrane protein, often an enzyme, altering its activity and leading to a cellular response. (vdocuments.net)
  • PAPbeta, a protein that binds to and is phosphorylated by the non-receptor tyrosine kinase PYK2, contains several modular signaling domains including a pleckstrin homology domain, an SH3 domain, ankyrin repeats and an ARF-GAP domain. (embl.de)
  • Together with protein 3CD binds the Cis-Active RNA Elent (CRE) which is involved in RNA synthesis initiation. (enquirebio.com)
  • 2002 which presumably prevents binding of the FERM Mouse monoclonal to LPP website to the C-terminal tail leaving Merlin in an "open" and inactive conformation. (hiv-proteases.com)
  • The C-helix pivots from an "outward" inactive conformation to an "inward", active conformation, exposing the ATP binding pocket. (janssenmedicalcloud.com)
  • Son of sevenless (SOS) is then recruited to the plasma membrane and catalyzes the conversion of inactive Ras-GDP to active Ras-GTP that in turn recruits Raf to the plasma membrane. (springer.com)
  • They influence cell activities by binding to receptor proteins on the plasma membrane. (vdocuments.net)
  • Are receptors always on the plasma membrane? (flashcardmachine.com)
  • After binding to its receptor, the capsid undergoes conformational changes. (enquirebio.com)
  • These two receptor isoforms dimerize upon binding the PDGF dimer, leading to three possible receptor combinations, namely -αα, -ββ and -αβ. (wikipedia.org)
  • Expression of both receptors and each of the four PDGFs is under independent control, giving the PDGF/PDGFR system a high flexibility. (wikipedia.org)
  • The second part of the tyrosine kinase domain in the PDGFβ receptor is phosphorylated at Tyr-857, and mutant receptors carrying phenylalanine at this position have reduced kinase activity. (wikipedia.org)
  • Sites of tyrosine phosphorylation involved in binding signal transduction molecules have been identified in the juxtamembrane domain, the kinase insert, and in the C-terminal tail in the PDGFβ receptor. (wikipedia.org)
  • The encoded protein is a tyrosine kinase transmembrane receptor and member of the CSF1/PDGF receptor family of tyrosine-protein kinases. (utsouthwestern.edu)
  • EphRs contain an ephrin binding domain and two fibronectin repeats extracellularly, a transmembrane segment, and a cytoplasmic tyr kinase domain. (umbc.edu)
  • In humans, the CRYAA gene encodes a 173 amino acid residue protein by single copy genes located on chromosome 21. (molvis.org)
  • In humans, three Ras genes ( H-ras , N-ras, and K-ras ) encode four distinct Ras proteins: H-Ras, N-Ras, K-Ras4A, and K-RasS4B, the latter 2 resulting from alternative RNA splicing of the K-ras gen. (encyclopedia.pub)
  • This domain occurred 250 times on human genes ( 586 proteins). (umbc.edu)
  • The semaphorin superfamily are composed of three protein families, the semaphorins, plexins and the c-Met family [ 2 ]. (oncotarget.com)
  • Pyk2 overexpression in HEK293 results in attenuated basal and agonist-stimulated inositol phosphate formation in mGluR1 expressing cells and involves a mechanism whereby Pyk2 displaces Galphaq/11 from the receptor. (uwo.ca)
  • Treatments that prevent Pyk2 phosphorylation in cortical neurons, and the overexpression of Pyk2 dominant-negative and catalytically inactive Pyk2 mutants in HEK293 cells, prevent ERK1/2 phosphorylation. (uwo.ca)
  • Although, ErbB-2 does not have any known high-affinity ligands, its kinase activity can be activated without ligand by either overexpression or heteroassociation with other members of the ErbB family. (activemotif.com)
  • Extracellular portion of the insulin receptor (blue) bound to insulin (red). (rcsb.org)
  • You can use the Protein Feature View for insulin receptor at the RCSB PDB to determine which portion of the receptor is included in each PDB entry. (rcsb.org)
  • This compound stimulates insulin receptor tyrosine kinase (IRTK) activity in CHO cells that overexpress human insulin receptors by binding to the β-subunit of the insulin receptor ( 1 ). (diabetesjournals.org)
  • A G-protein-linked receptor consists of a receptor protein associated with a G-protein on the cytoplasmic side. (vdocuments.net)
  • The active full-length CRYAA protein corresponding to amino acids 1-173 of CRYAA was recombined. (molvis.org)
  • Results from these analyses demonstrated that the C-terminal domain of HER3 (CTD, amino acids distal to the tyrosine kinase domain) contained potent transactivation potential. (plos.org)
  • BRAF kinase, a critical effector of the ERK signaling pathway, is hyperactivated in many cancers. (nature.com)
  • in the receptor that triggers a series of changes along a signal-transduction pathway. (vdocuments.net)
  • Kinase activation is visualized as tyrosine phosphorylation of the receptor molecules, which occurs between the dimerized receptor molecules (transphosphorylation). (wikipedia.org)
  • Pyk2 uncouples metabotropic glutamate receptor G protein signaling but facilitates ERK1/2 activation. (uwo.ca)
  • Group I metabotropic glutamate receptors (mGluRs) are coupled via Galphaq/11 to the activation of phospholipase Cbeta, which hydrolyzes membrane phospholipids to form inositol 1,4,5 trisphosphate and diacylglycerol. (uwo.ca)
  • The Pyk2 mediated activation of ERK1/2 phosphorylation is also Src-, calmodulin- and protein kinase C-dependent. (uwo.ca)
  • Despite the cited progress in this area of research, the molecular mechanisms underlying growth factor receptor activation by integrins remain to be defined. (123dok.org)
  • Following stimulation, the cells are fixed rapidly, which preserves activation-specific protein modifications. (activemotif.com)
  • Activation of Rho proteins through release of bound GDP and subsequent binding of GTP, is catalysed by guanine nucleotide exchange factors (GEFs) in the Dbl family. (embl-heidelberg.de)
  • Ligand binding to the extracellular portion of the receptor leads to receptor activation (fig. 2). (janssenmedicalcloud.com)
  • Brand TM, Iida M, Luthar N, Wleklinski MJ, Starr MM, Wheeler DL (2013) Mapping C-Terminal Transactivation Domains of the Nuclear HER Family Receptor Tyrosine Kinase HER3. (plos.org)
  • The ErbB-2 proto-oncogene, also called Neu, EGFR-2 or HER-2, is a member of the transmembrane receptor tyrosine kinase family, which also includes EGF receptor and EGFR-3 (HER-3 or ErbB-3). (activemotif.com)
  • It does not share significant sequence homology with other subtypes of small G-protein GEF motifs such as the Cdc25 domain and the Sec7 domain, which specifically interact with Ras and ARF family small GTPases, respectively, nor with other Rho protein interactive motifs, indicating that the Dbl family proteins are evolutionarily unique. (embl-heidelberg.de)
  • The Rho family of GTP-binding proteins has been implicated in the regulation of various cellular functions including actin cytoskeleton-dependent morphological change. (embl-heidelberg.de)
  • However, the mechanisms underlying receptor-dependent regulation of Rho family members remain incompletely understood. (embl-heidelberg.de)
  • The guanine nucleotide exchange factor (GEF) Dbl targets Rho family proteins thereby stimulating their GDP/GTP exchange, and thus is believed to be involved in receptor-mediated regulation of the proteins. (embl-heidelberg.de)
  • An amino-terminal portion conserved among a subset of Dbl family proteins is sufficient for the binding of Gbetagamma. (embl-heidelberg.de)
  • Ras proteins act as molecular switches that cycle between two conformational states: an active GTP-bound state and an inactive GDP-bound state. (encyclopedia.pub)
  • Pyk2 uncouples metabotropic glutamate receptor G protein signaling but" by Alexander A. Nicodemo, Macarena Pampillo et al. (uwo.ca)
  • We show here, that the proline-rich tyrosine kinase 2 (Pyk2) interacts with both mGluR1 and mGluR5 and is precipitated with both receptors from rat brain. (uwo.ca)
  • Crystal structure of the ARF-GAP domain and ankyrin repeats of PYK2-associated protein beta. (embl.de)
  • Myasthenia gravis is an autoimmune neurological disorder caused by autoantibodies against the acetylcholine receptor or against a receptor-associated protein, muscle-specific tyrosine kinase (MuSK-Ab). (mims.com)
  • The protein encoded by this gene is the receptor for colony stimulating factor 1, a cytokine which controls the production, differentiation, and function of macrophages. (utsouthwestern.edu)
  • The first intron of this gene contains a transcriptionally inactive ribosomal protein L7 processed pseudogene oriented in the opposite direction. (utsouthwestern.edu)
  • The gene encodes a 69-kDa protein called Merlin (Moesin ezrin and radixin like protein) that contains an N-terminal FERM website followed by an α-helical website and a charged Lactacystin C-terminal tail. (hiv-proteases.com)
  • The adaptor protein Grb2 forms a complex with Sos by the Grb2 SH3 domain. (wikipedia.org)
  • 3.0: hematopoietic cell-specific Lyn substrate 1 (HCLS1), Kelch domain-containing 6 (KLHDC6), sarcoglycan delta (SGCD), KIAA1706 protein (KIAA1706), RNA guanylyltransferase and 5′-phosphatase (RNGTT), chromosome 10 open reading frame 57 (C10orf57), chromosome 9 open reading frame 52 (C9orf52), and plasminogen activator, urokinase receptor (PLAUR). (molvis.org)
  • Pseudokinase domain of the Protein Tyrosine Kinase, Colon Carcinoma Kinase 4. (umbc.edu)
  • EphA10, which contains an inactive tyr kinase domain, may function to attenuate signals of co-clustered active receptors. (umbc.edu)
  • Taxonomic distribution of proteins containing ANK domain. (embl.de)
  • The complete taxonomic breakdown of all proteins with ANK domain is also avaliable . (embl.de)
  • Click on the protein counts, or double click on taxonomic names to display all proteins containing ANK domain in the selected taxonomic class. (embl.de)
  • The domain organisation of Eph receptors is conserved across different animal phyla. (silverchair.com)
  • Recombinant porcine HGF protein is a potent, high-purity NK1 isoform of porcine hepatocyte growth factor (HGF). (qkine.com)
  • Tyr-857 has therefore been assigned a role in positive regulation of kinase activity. (wikipedia.org)
  • This study provided evidence that the up-regulation of p27 protein expression is at least in part due to increased synthesis and that this increase fairly faithfully recapitulates the cancer preventive activity of nutritional and chemopreventive anti-cancer agents. (biomedcentral.com)
  • Please note: protein activity has been determined in a standardized assay using human cells. (qkine.com)
  • Integrin-mediated RON growth factor receptor phosphorylation requires tyrosine kinase activity of both the receptor and c-Src. (123dok.org)
  • on the kinase activity of both RON itself and c-Src. (123dok.org)
  • Like Ras, ARFs are active in their GTP-bound form, and their duration of activity is controlled by GTPase-activating proteins (GAPs), which assist ARFs in hydrolyzing GTP to GDP. (embl.de)
  • Acts as a cofactor to stimulate the activity of 3D polymerase, maybe through a nucleid acid chaperone activity .Protein 3A: Localizes the viral replication complex to the surface of mbranous vesicles. (enquirebio.com)
  • ligand binding to the extracellular portion of the receptor leads to a conformational change. (janssenmedicalcloud.com)
  • A recent structure of insulin bound to a portion of the receptor (insulin shown here in red from PDB entry 3w14 ) places another piece in the puzzle. (rcsb.org)
  • The tyrosine kinase portion of the receptor is itself a dynamic protein with many moving parts. (rcsb.org)
  • NOTCH1, NOTCH2, NOTCH3 and NOTCH4 are cell surface receptors that transduce juxtacrine signals of delta-like canonical Notch ligand (DLL)1, DLL3, DLL4, jagged canonical Notch ligand (JAG)1 and JAG2 from adjacent cells ( 1 - 3 ). (spandidos-publications.com)
  • Both hormones are small proteins that are recognized by receptors on the surface of cells. (rcsb.org)
  • Type I diabetes is caused by problems with insulin: in some cases, the pancreatic cells that produce insulin are destroyed by autoimmunity, and in other cases insulin is mutated and inactive. (rcsb.org)
  • Hsp90 associates with eNOS under inactive conditions, and upon the stimulation of endothelial cells with VEGF, estrogen, histamine, shear stress, and statins. (eurekaselect.com)
  • Similar to imatinib sensitive BCR ABL cells, FoxO3a protein expression was also restored in T315I cells upon treatment with bortezomib. (mi-rna.com)
  • Recent investigations have shown that the RON receptor is expressed in various cell types including epithelial cells (23) and that MSP-mediated effects on epithelial cells are integrin-dependent (23, 24). (123dok.org)
  • FACE is a highly sensitive high-throughput assay designed for detecting activated proteins within mammalian cells. (activemotif.com)
  • Capsid protein VP1 interacts with host cell receptor to provide virion attachment to target host cells. (enquirebio.com)
  • Eph and ephrin proteins interact with a number of other ligand/receptor systems to influence how cells translate environmental signals to orchestrate morphogenetic events. (silverchair.com)
  • The foamy stromal cells between the capillaries stain positive for glial fibrillary acid protein and neuron-specific enolase. (medscape.com)
  • This receptor mediates most if not all of the biological effects of this cytokine. (utsouthwestern.edu)
  • Is cytokine receptor association with PTK reversible or irreversible? (flashcardmachine.com)
  • Functional annotation clustering showed that they belong to cell cycle, organelle or nuclear lumen, protein transport, and DNA binding and repair clusters. (molvis.org)
  • Preliminary studies using either N -methyl- N -nitrosourea (MNU)-induced rat breast cancer model or human breast cancer cell lines in vitro had suggested, but not proved, that nutritional and chemopreventive anti-cancer agents increase p27 protein expression. (biomedcentral.com)
  • Outcomes Merlin associates using the Angiomotin/Patj/Pals1 complicated To identify protein that form steady complexes with Merlin we produced individual embryonic kidney (HEK293) cell lines stably expressing. (hiv-proteases.com)
  • Disturbing the function or the level of such specific protein in the cell environment is sufficient to cause overstimulation of the cell division, stopping of the cell differentiation and immortality. (wikilectures.eu)
  • L-767,827, an inactive structural analog of the insulin mimetic, had no effect on β-cell [Ca 2+ ] i . (diabetesjournals.org)
  • A cell targeted by a particular chemical signal has a receptor protein that recognizes the signal molecule. (vdocuments.net)
  • Fast Activated Cell-based ELISA (FACE™) Kits provide a simple, sensitive method for detecting protein phosphorylation directly in the cell, without making extracts or performing electrophoresis and membrane blotting. (activemotif.com)
  • Flow chart of the FACE in cell Western method that uses a cell based ELISA to measure the levels of the native and phospho forms of signaling proteins and kinases that are activated by phosphorylation. (activemotif.com)
  • Here, we show the association of Dbl with G protein betagamma subunits (Gbetagamma) in transient co-expression and cell-free systems. (embl-heidelberg.de)
  • Capsid protein VP4 is released, Capsid protein VP1 N-terminus is externalized, and together, they shape a pore in the host mbrane through which the viral genome is translocated into the host cell cytoplasm. (enquirebio.com)
  • This would result in depletion of MHC, trail receptors and IFN receptors at the host cell surface .Viral protein genome-linked: acts as a primer for viral RNA replication and rains covalently bound to viral genomic RNA. (enquirebio.com)
  • Trans interactions of Eph receptors with ephrins at cell-cell interfaces promote a variety of cellular responses, including repulsion, attraction and migration. (silverchair.com)