• It is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. (antibodyguide.com)
  • The EGFR gene provides instructions for making a receptor protein called the epidermal growth factor receptor, which spans the cell membrane so that one end of the protein remains inside the cell and the other end projects from the outer surface of the cell. (medlineplus.gov)
  • Lung cancers with EGFR gene mutations tend to respond to treatments that specifically target the overactive epidermal growth factor receptor protein that allows cancer cells to constantly grow and divide. (medlineplus.gov)
  • The EGFR family: not so prototypical receptor tyrosine kinases. (medlineplus.gov)
  • 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)
  • EGFR (Epidermal growth factor receptor, HER1, ErbB1) is encoded by the EGFR gene located on chromosome 7 in humans. (thermofisher.com)
  • EGFR belongs to the HER/ERbB family of proteins that includes three other receptor tyrosine kinases, ERbB2, ERbB3, ERbB4. (thermofisher.com)
  • EGFR is a transmembrane receptor and binding of its cognate ligands such as EGF (Epidermal Growth Factor) and TGF alpha (Transforming Growth Factor alpha) to the extracellular domain leads to EGFR dimerization followed by autophosphorylation of the tyrosine residues in the cytoplasmic domain. (thermofisher.com)
  • Upon receptor activation and signaling, EGFR is endocytosed and targeted for degradation or recycling. (thermofisher.com)
  • Mutations in the EGFR gene are associated with lung cancer and multiple alternatively spliced transcript variants encode different protein isoforms of EGFR have been found. (thermofisher.com)
  • Epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and member of the protein kinase superfamily that regulates cell growth and differentiation. (biolegend.com)
  • Gefitinib administration prevents tyrosine residue of autophosphorylation of the EGFR receptor. (pharmacology2000.com)
  • Chemical inhibition and siRNA knockdown experiments demonstrated that STAT-3 activation is dependent on the activation of nonreceptor tyrosine-protein kinase 2 (TYK2) and epidermal growth factor receptor (EGFR) tyrosine kinases. (cdc.gov)
  • Our studies show that poultry dust extract controls the induction of immune and inflammatory mediator expression via a cellular pathway involving oxidative stress-mediated STAT-3 activation by TYK2 and EGFR tyrosine kinases. (cdc.gov)
  • Here we show that 70% of AChR-Ab-seronegative MG patients, but not AChR-Ab-seropositive MG patients, have serum auto-antibodies against the muscle-specific receptor tyrosine kinase, MuSK. (nih.gov)
  • Other antigenic targets of the NMJ, muscle-specific receptor tyrosine kinase (MuSK) antibody and low-density lipoprotein receptor-related protein 4 antibody, have also been implicated in 5%-8% of all patients with MG. The detection of AChR, via antibody test, in patients with typical clinical symptoms is a key diagnostic marker of MG and helps define the disease subtypes. (medscape.com)
  • As an alternative approach, growth factor receptors or components of their signal transduction machinery may be targeted directly. (springer.com)
  • This third edition continues to combine current understanding of classical quantitative pharmacology and drug-receptor interactions with the basics of receptor structure and signal transduction mechanisms, providing an integrated analysis of the mechanisms of drug action at membrane receptors. (routledge.com)
  • Maintaining the second edition's focus on cell membrane receptors and the immediate signal transduction events at the membrane, this edition includes updated chapters on receptor structure and signal transduction by G-proteins and tyrosine kinases as well as enhancements to the quantitative treatment of drug-receptor interactions. (routledge.com)
  • 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)
  • A common heterophilic ligand for these RTK family members is definitely Gas6 a vitamin K-dependent protein that is widely secreted by most cells including the lungs intestine Serping1 and vascular endothelium (43). (exposed-skin-care.net)
  • Unlike receptor tyrosine kinases, nRTKs lack receptor-like features such as an extracellular ligand-binding domain and a transmembrane-spanning region. (wikipedia.org)
  • The binding of a ligand to epidermal growth factor receptor allows the receptor to attach to another nearby epidermal growth factor receptor protein (dimerize), turning on (activating) the receptor complex. (medlineplus.gov)
  • These gene changes result in a receptor protein that is constantly turned on (constitutively activated), even when it is not bound to a ligand. (medlineplus.gov)
  • Upon ligand binding, type I receptors phosphorylate cytoplasmic SMAD transcription factors, which then translocate to the nucleus and interact directly with DNA or in complex with other transcription factors (Bondestam et al. (nih.gov)
  • GP30 is a potential ligand for this receptor. (hatinhibitor.com)
  • Activation of kinase activity occurs after ligand recognition and binding. (rndsystems.com)
  • Because of these profound effects on ligand specificity, reverse transcription-PCR was used to understand the expression of the FL and ED receptor isoforms at the level of single neurons. (jneurosci.org)
  • In this study, comparison of the ligand specificity of the full-length (FL) and ED receptor isoforms revealed that ED trkB exhibits a more restricted neurotrophin specificity than does FL trkB. (jneurosci.org)
  • The only ligand recognized to bind MST1R (RON) is Macrophage Stimulating 1 (MST1), also known as Macrophage Stimulating Protein (MSP) or Hepatocyte Growth Factor-Like Protein (HGFL). (frontiersin.org)
  • Sections of formalin-fixed, paraffin-embedded tumour tissue from 22 patients with mammary and extramammary Paget's disease have been stained immunohistochemically using a monoclonal antibody (NCL-CB11) raised against a synthetic peptide from the C-terminal end of the predicted sequence of the c-erbB-2 protein product. (nih.gov)
  • As ErbB-family ligands and receptors are highly expressed within the stem-cell niche 7 , we hypothesize that strong endogenous regulators must control the pathway in the stem-cell compartment. (nature.com)
  • The leucine-rich repeat protein LRIG1 is a negative regulator of ErbB family receptor tyrosine kinases. (nature.com)
  • Its effect on the function of other proteins in the ErbB family of proteins that may also fuel cancer cell growth is being studied. (cancer.gov)
  • Cediranib is an oral VEGFR1, VEGFR2 and VEGFR3 tyrosine kinase inhibitor (TKI), with additional activity against platelet-derived growth factor (PDGF) receptors and c-KIT. (nature.com)
  • Aside from binding to membranes, the activated FERM domain of ERM proteins can also bind the guanine nucleotide dissociation inhibitor of Rho GTPase (RhoDGI), which suggests that in addition to functioning as a cross-linker, ERM proteins may influence Rho signalling pathways. (embl.de)
  • Is classified as a tyrosine kinase inhibitor. (pharmacology2000.com)
  • It is a tyrosine kinase inhibitor that enters a cancer cell and binds to the part of the HER2 protein that sits just beneath the cell's outer membrane. (cancer.gov)
  • it also plays a critical role as an inhibitor of TOLL-LIKE RECEPTORS signaling. (bvsalud.org)
  • More specifically, compounds of this invention are novel as selective inhibitors of the PDGF-R protein tyrosine kinase and can be applied as potential therapeutic agents for various disease states which are characterized by uncontrolled cellular proliferation. (epo.org)
  • Among them are the Sprouty proteins which mainly act as inhibitors of growth factor-dependent neuronal and glial signaling pathways. (springer.com)
  • Receptor tyrosine kinases (RTKs) play fundamental tasks in varied cell functions including proliferation differentiation survival migration and rate of metabolism (16). (exposed-skin-care.net)
  • Unlike the receptor tyrosine kinases (RTKs), the second subgroup of tyrosine kinases, the non-receptor tyrosine kinases are cytosolic enzymes. (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • SCF R is also known as the c-kit proto-oncogene protein and as CD117. (rndsystems.com)
  • MST1R (RON) is a trans-membrane receptor tyrosine kinase (RTK), which is part of the c-MET proto-oncogene family. (frontiersin.org)
  • From NCBI Gene: The proto-oncogene MET product is the hepatocyte growth factor receptor and encodes tyrosine-kinase activity. (nih.gov)
  • A non-receptor tyrosine kinase (nRTK) is a cytosolic enzyme that is responsible for catalysing the transfer of a phosphate group from a nucleoside triphosphate donor, such as ATP, to tyrosine residues in proteins. (wikipedia.org)
  • One of the important domain of nRTKs is the tyrosine kinase catalytic domain, which is about 275 residues in length. (wikipedia.org)
  • Ectopic up-regulation of PTPRD in neuroblastoma dephosphorylates tyrosine residues in AURKA resulting in a destabilization of this protein culminating in interfering with one of AURKA's primary functions in neuroblastoma, the stabilization of MYCN protein, the gene of which is amplified in approximately 25 to 30% of high risk neuroblastoma. (biomedcentral.com)
  • The cytoplasmic region contains a juxtamembrane motif with two tyrosine residues which are the major autophosphorylation sites, a kinase domain, and a conserved sterile alpha motif (SAM) in the carboxy tail which contains one conserved tyrosine residue. (rndsystems.com)
  • For cytoskeleton-membrane cross-linking, the dormant molecules becomes activated and the FERM domain attaches to the membrane by binding specific membrane proteins, while the last 34 residues of the tail bind actin filaments. (embl.de)
  • 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)
  • Soluble monomeric ligands bind the receptor but do not induce receptor autophosphorylation and activation (2). (rndsystems.com)
  • Protein-tyrosine phosphatases PTPN3 and PTPN4, enzyme that appear to act at junctions between the membrane and the cytoskeleton. (embl.de)
  • Protein-tyrosine phosphatases PTPN14 and PTP-D1, PTP-RL10 and PTP2E. (embl.de)
  • When antigen binds to T-cell receptor, Lck becomes autophosphorylated and phosphorylates the zeta chain of the T-cell receptor, subsequently another nRTK, Zap70, binds to this T-cell receptor and then participates in downstream signaling events that mediate transcriptional activation of cytokine genes. (wikipedia.org)
  • This gene encodes a protein containing a C3HC4-type RING finger domain, which is a specialized type of Zn-finger that binds two atoms of zinc and is thought to be involved in mediating protein-protein interactions. (cancerindex.org)
  • Genetic variants at the PTPN2 locus, which encodes the tyrosine phosphatase PTPN2, cause reduced gene expression and are linked to rheumatoid arthritis (RA) and other autoimmune diseases. (researchgate.net)
  • This gene encodes a member of the neurotrophic tyrosine receptor kinase (NTRK) family. (origene.com)
  • The structure of the catalytic domain can be divided into a small and a large lobe, where ATP binds to the small lobe and the protein substrate binds to the large lobe. (wikipedia.org)
  • Filopodin, a slime mold protein that binds actin and which is involved in the control of cell motility and chemotaxis. (embl.de)
  • ERM proteins are made of three domains, the FERM domain, a central helical domain and a C-terminal tail domain, which binds F-actin. (embl.de)
  • Trastuzumab (Herceptin), a drug developed in 1990s to target HER2+ breast cancers, is a large monoclonal antibody that, once injected into patients, binds to the portion of the HER2 protein that sits on the outer surface of the cancer cell. (cancer.gov)
  • For example, specific domains that target enzymes to the cytoplasmic part of cytokine receptors (Jak family) or two domains: an integrin-binding domain and a focal adhesion-binding domain (Fak family). (wikipedia.org)
  • Focal-adhesion kinases (FAKs), cytoplasmic protein tyrosine kinases involved in signalling through integrins. (embl.de)
  • Janus tyrosine kinases (JAKs), cytoplasmic tyrosine kinases that are non-covalently associated with the cytoplasmic tails of receptors for cytokines or polypeptidic hormones. (embl.de)
  • The amino-acid sequence of the FERM domain is highly conserved among ERM proteins and is responsible for membrane association by direct binding to the cytoplasmic domain or tail of integral membrane proteins. (embl.de)
  • PTPRD has a tumor suppressor function in neuroblastoma through AURKA dephosphorylation and destabilization and a downstream destabilization of MYCN protein, representing a novel mechanism for the function of PTPRD in neuroblastoma. (biomedcentral.com)
  • We further demonstrate that PTPRD has a tumor suppressor function in neuroblastoma through dephosphorylating and destabilizing AURKA, leading to a downstream decrease of MYCN protein. (biomedcentral.com)
  • In recent years, the search for intracellular signaling integrator downstream of receptor tyrosine kinases provided valuable novel substrates. (springer.com)
  • A novel pathogenic mutation on the interleukin-7 receptor has been described in a newborn. (medscape.com)
  • The HER2 receptor does not bind to any known ligands, however, its dimerization arm is innately positioned in an open conformation. (plos.org)
  • HER2-positive (HER2+) breast cancers are defined as those that have an excess number of HER2 genes or over-produce the protein product of the HER2 gene, the HER2 cell surface receptor. (cancer.gov)
  • The ALTTO clinical trial was unique in that, for all of patients, there was central pathology review of the primary tumor, including re-evaluation of the cancer's estrogen receptor (ER), progesterone receptor (PR), and HER2 status, before patients were randomly assigned to one of the trial's four treatment groups. (cancer.gov)
  • Lapatinib acts by entering a cancer cell and binding to the part of the HER2 protein that lies just beneath the cell's outer membrane. (cancer.gov)
  • 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)
  • 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)
  • This gene is also a translocation partner in anaplastic large cell lymphoma and inflammatory myofibroblastic tumor cases, where a t(2;17)(p23;q25) translocation has been identified with the anaplastic lymphoma kinase (ALK) gene on chromosome 2, and a t(8;17)(q24;q25) translocation has been identified with the MYC gene on chromosome 8. (cancerindex.org)
  • Regulation of metabolic homeostasis by the TGF-beta superfamily receptor ALK7. (nih.gov)
  • Belongs to the protein kinase superfamily. (lu.se)
  • We first identified the bioactive phytoconstituents from Amaranthus tricolor and predicted their potential protein targets involved in the pathogenesis of cognitive dysfunction using BindingDB (p≥0.7). (ijpsonline.com)
  • Thirty nine phytoconstituents were identified in Amaranthus tricolor , five of which were predicted to modulate eight potential protein targets involved in cognitive impairment. (ijpsonline.com)
  • Protein tyrosine phosphatase receptor delta ( PTPRD ) is an important regulator of axon growth and guidance and is highly expressed in the central nervous system where it functions as a transmembrane homophilic neuronal cell adhesion molecule [ 1 ]. (biomedcentral.com)
  • Caenorhabditis elegans protein phosphatase ptp-1. (embl.de)
  • Tumor-specific apoptosis caused by deletion of the ERBB3 pseudo-kinase in mouse intestinal epithelium. (nature.com)
  • Gas6 is the product of growth arrest-specific gene 6 which was in the beginning cloned from serum-starved fibroblasts and shares about CUDC-305 (DEBIO-0932 ) 44% sequence identity and related website organization with protein S a negative regulator of blood coagulation (48). (exposed-skin-care.net)
  • Several studies shown that Axl could mediate cell adhesion and aggregation through homotypic ectodomain associations (9 23 Both CUDC-305 (DEBIO-0932 ) murine and human being Axl proteins undergo proteolytic processing to yield a soluble form of this molecule. (exposed-skin-care.net)
  • PTPN2 inhibits signaling through the T cell and cytokine receptors and loss of PTPN2 promotes T cell expansion and CD4 and CD8-driven autoimmunity. (researchgate.net)
  • One of the protein-protein interaction domains in nRTKs are the Src homology 2 (SH2) and 3 (SH3) domains. (wikipedia.org)
  • This kinase is a membrane-bound receptor that, upon neurotrophin binding, phosphorylates itself and members of the MAPK pathway. (origene.com)
  • Non-receptor tyrosine kinases regulate cell growth, proliferation, differentiation, adhesion, migration and apoptosis, and they are critical components in the regulation of the immune system. (wikipedia.org)
  • Activin receptor-like kinase 7 silencing alleviates cardiomyocyte apoptosis, cardiac fibrosis, and dysfunction in diabetic rats. (nih.gov)
  • Alternative splicing of the avian trkB receptor generates an extracellular deletion (ED) isoform missing 11 amino acids from the neurotrophin-binding domain of the full-length (FL) receptor. (jneurosci.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)
  • Calpain, a proteolytic enzyme plays critical role in the skeletal muscle physiology by maintaining the protein metabolism. (researchgate.net)
  • Up-regulation in the activity of such enzyme under diverse clinical settings (i.e. diabetes, cancer, AIDS, chronic heart failure, immobilization, aging etc) leads to loss in muscle proteins and causes atrophy/cachexia/sarcopeni. (researchgate.net)
  • Ectodomain dropping has emerged as an important posttranslational mechanism to regulate the functions of various integral membrane-bound proteins including adhesion molecules cytokines growth factors and their receptors (57 60 Both. (exposed-skin-care.net)
  • HYPOTHESIS: Do LRIG Proteins Regulate Stem Cell Quiescence by Promoting BMP Signaling? (nature.com)
  • E-selectin, which is highly expressed in vascular endothelial cells near tumor and get involved in the all tumor growth steps: occurrence, proliferation and metastasis, is considered as a promise targeted protein for antitumor drug discovery. (bvsalud.org)
  • Linkage and comparative mapping studies indicate that the transferred chromosome segment contains a number of candidate genes for hypertension, including genes encoding a brain dopamine receptor and a renal epithelial potassium channel. (jci.org)
  • Gene ontology functional enrichment analysis was performed using search tool for the retrieval of interacting genes/proteins. (ijpsonline.com)
  • Further, the present invention provides pharmaceutical compositions and a method for treating such disorders comprising the administration to a patient of a PDGF receptor inhibiting effective amount of a pyrazolo[3,4-g]quinoxaline compound exhibiting protein tyrosine kinase inhibition activity. (epo.org)
  • In approximately 80% of patients, auto-antibodies to the muscle nicotinic acetylcholine receptor (AChR) are present. (nih.gov)
  • TotalSeq™-D antibodies are compatible with Mission Bio's Tapestri Single-Cell Sequencing Platform for simultaneous detection of DNA and Protein. (biolegend.com)
  • Myasthenia gravis (MG) is a rare autoimmune neuromuscular disorder in which antibodies form against postsynaptic nicotinic acetylcholine receptors (AChRs) located at the motor endplate of the neuromuscular junction (NMJ). (medscape.com)
  • There are two classes of receptors, designated A and B. Both the A and B class receptors have an extracellular region consisting of a globular domain, a cysteine-rich domain, and two fibronectin type III domains. (rndsystems.com)
  • A receptor tyrosine kinase that transduces signals from EXTRACELLULAR MATRIX to the CYTOPLASM by binding ligands such as GALECTIN 3. (bvsalud.org)
  • Only membrane-bound or Fc‑clustered ligands are capable of activating the receptor in vitro . (rndsystems.com)
  • His current major research interests are N-methyl-D-aspartate (NMDA) receptors in the stubstantia nigra in relation to cell death in Parkinson's disease and also ion transport and signaling in mast cells in relation to intracellular pH and volume regulation. (routledge.com)
  • Neurons are capable of expressing a surprising diversity of trk receptor structural isoforms that arise via alternative splicing ( Barbacid, 1994 ). (jneurosci.org)
  • As a molecular mechanism, we demonstrate that PTPRD interacts with aurora kinase A (AURKA), an oncogenic protein that is over-expressed in multiple forms of cancer, including neuroblastoma. (biomedcentral.com)
  • Disclaimer note: The observed molecular weight of the protein may vary from the listed predicted molecular weight due to post translational modifications, post translation cleavages, relative charges, and other experimental factors. (novusbio.com)
  • Thirty-two non-receptor tyrosine kinases have been identified in human cells (EC 2.7.10.2). (wikipedia.org)
  • His research interests have included the role of bradykinin receptors in the human nasal airway, the control of microvascular circulation in human skin, and the mechanism of activation of dendritic cells. (routledge.com)
  • Real-time PCR on EDTA blood targeting the gene for the major outer membrane protein lip L32 of human pathogenic Leptospira spp. (cdc.gov)
  • The uptake of labeled MPs in the presence of protein S and Gas6 in human aortic endothelial cells (HAEC) and human umbilical vein endothelial cells (HUVEC) was monitored by flow cytometry, western blotting and confocal/electron microscopy. (lu.se)
  • This positioning allows the receptor to attach (bind) to other proteins, called ligands, outside the cell and to receive signals that help the cell respond to its environment. (medlineplus.gov)
  • as a cell surface-associated protein, it is easily accessible to drugs and as a kinase it is amenable to targeted inhibition by small molecules. (antibodyguide.com)
  • Transmembrane tyrosine-protein kinase that may modulate TEK/TIE2 activity and contribute to the regulation of angiogenesis. (cusabio.com)
  • Since the protein lacks enzymatic activities, it will be difficult to develop chemical compounds capable to directly and specifically modulate Sprouty functions. (springer.com)