• 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)
  • About one third of the time, patients can become unresponsive to Gleevec and have to switch to another tyrosine inhibitor, such as Sprycel ( dasatinib ) or Tasigna ( nilotinib ). (rxwiki.com)
  • Like sorafenib, lapatinib is a protein kinase inhibitor shown to decrease tumor-causing breast cancer stem cells. (hmdb.ca)
  • The introduction of imatinib, a selective inhibitor of the ABL tyrosine kinase, has revolutionized the treatment and the outcome of this subset of patients [ 1 ]. (hindawi.com)
  • Imatinib mesylate (IM), a potent inhibitor of the BCR/ABL tyrosine kinase, has become standard first-line therapy for patients with chronic myeloid leukemia (CML), but the frequency of resistance increases in advancing stages of disease. (lu.se)
  • Critically, the combination of a tyrosine kinase inhibitor (TKI), i.e. (lu.se)
  • Moreover, mH2A1.1-OE proteomic profile identified several upregulated proteins associated to DNA and histones hypermethylation, including S-adenosylhomocysteine hydrolase, a strong inhibitor of DNA methyltransferase and of the methyl donor S-adenosyl-methionine (SAM). (bvsalud.org)
  • Olsson PO, Gustafsson R, In 't Zandt R, Friman T, Maccarana M, Tykesson E, Oldberg Å, Rubin K, Kalamajski S. The Tyrosine Kinase Inhibitor Imatinib Augments Extracellular Fluid Exchange and Reduces Average Collagen Fibril Diameter in Experimental Carcinoma. (lu.se)
  • S364A - Strong decrease of phosphorylation by PRKACA (the catalytic subunit of protein kinase A). Csk's interaction with a phosphatase ("Lyp", gene product of PTPN22) is possibly associated with the increased autoimmune diseases associated with PTPN22 mutations. (wikipedia.org)
  • Epidermal growth factor receptor (EGFR) gene mutations are frequent in lung cancer arising in patients of Asian ethnicity, female sex, nonsmokers, and adenocarcinoma histology. (nih.gov)
  • About 70% of the patients with EGFR mutations respond to EGFR tyrosine kinase inhibitors (TKIs) including gefitinib and erlotinib, whereas only 10% of those without the mutations do so. (nih.gov)
  • Some gene mutations are acquired during a person's lifetime and are present only in certain cells. (medlineplus.gov)
  • Somatic mutations in the JAK2 gene are associated with essential thrombocythemia, a disorder characterized by an increased number of platelets, the blood cells involved in normal blood clotting. (medlineplus.gov)
  • Somatic mutations in the JAK2 gene are associated with polycythemia vera, a disorder characterized by uncontrolled blood cell production. (medlineplus.gov)
  • JAK2 gene mutations result in the production of a constitutively activated JAK2 protein, which seems to improve the survival of the cell and increase production of blood cells. (medlineplus.gov)
  • Somatic JAK2 gene mutations are also associated with primary myelofibrosis, a condition in which bone marrow is replaced by scar tissue (fibrosis). (medlineplus.gov)
  • A small number of people with this condition have mutations in the exon 12 region of the gene. (medlineplus.gov)
  • These JAK2 gene mutations result in a constitutively active JAK2 protein, which leads to the overproduction of abnormal megakaryocytes. (medlineplus.gov)
  • Somatic JAK2 gene mutations are also associated with several related conditions. (medlineplus.gov)
  • Scope includes mutations and abnormal protein expression. (cancerindex.org)
  • ALL cancers have lots of additional changes, the so-called 'passenger' mutations, that may contribute to the cancer, but are not the main genes. (cancerquest.org)
  • 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)
  • She later continued to study MRes in Cell Biology at UCL, during which she investigated how attenuated mutations in the envelope protein of pathogenic simian immunodeficiency virus affect virological synapse formation and envelope sorting during infection, under the supervision of Prof. Mark Marsh and Dr. Scott Lawrence. (portlandpress.com)
  • Mutations in the CD117 gene have been linked to malignant behavior in GISTs. (medscape.com)
  • Objective: Deregulation of the Wnt signalling pathway by mutations in the Apc or β-catenin genes underlies colorectal carcinogenesis. (eur.nl)
  • Gene mutations that cause loss of receptor function are associated with CONGENITAL INSENSITIVITY TO PAIN WITH ANHIDROSIS, while gene rearrangements that activate the protein-tyrosine kinase function are associated with tumorigenesis. (bvsalud.org)
  • Human epithelial malignancies frequently display deregulated tyrosine kinase activity. (cancer.gov)
  • 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)
  • Phosphorylation of EGFR at certain residues is also mediated by Src-non-receptor kinase. (thermofisher.com)
  • Phosphorylation of EGFR at Y1086 specifically allows binding of the adaptor protein GRB2, leading to activation of the MAPK pathway. (thermofisher.com)
  • We have shown that all mammalian Cbl proteins mediate ubiquitination and degradation of the activated EGFR as well as other components of the signaling complex. (cancer.gov)
  • 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)
  • HER2/neu (also called ERB B2 ) is the gene that encodes the human epidermal growth factor receptor type 2. (cancerquest.org)
  • FLT3 (FMS-related tyrosine kinase 3) located on chromosome 13q12.2 encodes a receptor tyrosine kinase (RTK) that activates the Ras and PI3 kinase pathway leading to the increased proliferation and inhibition of apoptosis in hemopoietic progenitor cells [ 7 ]. (hindawi.com)
  • q11) resulting in a chimeric bcr-abl (e1a2 breakpoint) fusion gene that encodes a 190 KD protein (p190) with constitutively active tyrosine kinase activity that can alter multiple signaling pathways, contributing to tumor growth and proliferation. (hindawi.com)
  • 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)
  • This gene encodes a cytoplasmic protein tyrosine kinase which is found concentrated in the focal adhesions that form between cells growing in the presence of extracellular matrix constituents. (genetex.com)
  • The most common mutation (written as Val617Phe or V617F) replaces the protein building block (amino acid) valine with the amino acid phenylalanine at position 617 in the protein. (medlineplus.gov)
  • A small number of affected individuals have a somatic mutation in another part of the JAK2 gene known as exon 12. (medlineplus.gov)
  • The V617F JAK2 gene mutation results in the production of a JAK2 protein that is constantly turned on (constitutively activated), which, in essential thrombocythemia, leads to the overproduction of abnormal blood cells called megakaryocytes. (medlineplus.gov)
  • About 3 percent of affected individuals have a somatic mutation in the exon 12 region of the JAK2 gene. (medlineplus.gov)
  • C677T mutation in methylenetetrahydrofolate reductase gene and neural tube defects: should Japanese women undergo gene screening before pregnancy? (cdc.gov)
  • It results from a mutation in the IL-2 receptor gamma gene ( IL-2RG ). (msdmanuals.com)
  • To inhibit SFKs, CSK is then recruited to the plasma membrane via binding to transmembrane proteins or adapter proteins located near the plasma membrane and ultimately suppresses signaling through various surface receptors, including T-cell receptor (TCR) and B-cell receptor (BCR) by phosphorylating and maintaining inactive several effector molecules. (wikipedia.org)
  • Both receptors belong to the TAM (TYRO3, AXL and MER - MER proto-oncogene, tyrosine kinase) receptor tyrosine kinase family, which emerged as new potential targets in many oncological diseases, from leukaemia to solid tumours ( Graham et al, 2014 ). (nature.com)
  • 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)
  • This protein is part of a signaling pathway called the JAK/STAT pathway, which transmits chemical signals from outside the cell to the cell's nucleus. (medlineplus.gov)
  • and transmembrane receptor protein tyrosine kinase signaling pathway. (nih.gov)
  • Phosphatidylinositol 3-kinase-independent signal transduction pathway for PDGF-induced chemotaxis. (researchmap.jp)
  • The peroxisome proliferator- activated receptor gamma coactivator 1-alpha ( Ppargc1a ) gene was found to be involved in the networks generated using Ingenuity Pathway Studio (IPA) from the differentially expressed transcript cluster lists of week 2 versus 1, week 3 versus 2, week 6 versus 3, and week 8 versus 6. (molvis.org)
  • In 7 MM, 3 MGUS and 3 healthy subjects by gene expression profile, we identified a total of 551 upregulated and 343 downregulated genes in MM-HDN, involved in chemokine signaling pathway and FC-gamma receptor mediated phagocytosis conveying in the activation of STAT proteins. (bvsalud.org)
  • In TGF-beta-treated MCF10A mammary epithelial cells overexpressing HER2 and by chromatin immunoprecipitation, we identified novel Smad targets including protein tyrosine phosphatase receptor type kappa (PTPRK). (nih.gov)
  • Receptor-type tyrosine-protein phosphatase C OS=Mus musculus GN=Ptprc PE=1 SV=2, Leukocyte common an. (yeastrc.org)
  • HER2 is a tyrosine kinase receptor growth-promoting protein expressed on the surface of many types of tumors including breast, gastric, lung and colorectal cancers. (biospace.com)
  • HER2 overexpression may be associated with a specific HER2 gene alteration known as HER2 amplification and is often associated with aggressive disease and poor prognosis in breast cancer. (biospace.com)
  • 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)
  • 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)
  • 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)
  • Patients with a strong overexpression of the HER2 protein (IHC3+) specifically benefited from the treatment, with a median overall survival of 17.9 mo. (wjgnet.com)
  • Before the advent of tyrosine kinase inhibitors (TKIs), the outcome of Ph+ ALL patients not eligible for allogeneic stem cell transplant (allo-SCT) was characterized by an extremely poor prognosis, a weak response to most chemotherapy combinations, short remission durations, and poor survival rates. (hindawi.com)
  • Universal protein resource accession number P41240 for "Tyrosine-protein kinase CSK" at UniProt. (wikipedia.org)
  • Orthologous to human ABL2 (ABL proto-oncogene 2, non-receptor tyrosine kinase). (nih.gov)
  • A pseudogene located on chromosome 3 has been identified for this gene. (thermofisher.com)
  • This chromosome results from the faulty fusion of two genes - Bcr from chromosome 22, and Abl on chromosome 9. (rxwiki.com)
  • 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)
  • We selected 17 patients clinically and his- is encoded by a single gene located on the tologically proven to be suffering from PV short arm of chromosome 11 [ 6 ]. (who.int)
  • Anaplastic lymphoma kinase (ALK) protein may be detected in most cases (60-70%) of systemic ALCL by immunohistochemistry. (medscape.com)
  • The JAK2 gene provides instructions for making a protein that promotes the growth and division (proliferation) of cells. (medlineplus.gov)
  • TYRO3 or AXL gene knockdown reduced cell proliferation/colony formation. (nature.com)
  • Protein tyrosine kinase inhibitors inhibit both proliferation and chemotaxis of vascular smooth muscle cells. (researchmap.jp)
  • Protein kinase C-mediated inhibition of vascular smooth muscle cell proliferation : The isoform that may mediate G1/S inhibition. (researchmap.jp)
  • 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)
  • Tyrosine-protein kinase CSK also known as C-terminal Src kinase is an enzyme that, in humans, is encoded by the CSK gene. (wikipedia.org)
  • Role of the planar cell polarity gene Protein tyrosine kinase 7 in neural tube defects in humans. (cdc.gov)
  • Phosphatidylinositol 3-kinase is required for growth factor-induced amino acid uptake by vascular smooth muscle cells. (researchmap.jp)
  • Upon immobilization sAxl advertised cell migration and induced the phosphorylation of Axl and phosphatidylinositol 3-kinase. (exposed-skin-care.net)
  • Binds to phosphatidylinositol 3'-kinase (PI3k) from T lymphocytes through its SH3 domain and to the tyrosine phosphorylated form of khdrbs1/p70 through its SH2 domain. (lu.se)
  • Organic dust induces inflammatory gene expression in lung epithelial cells via ROS-dependent STAT-3 activation. (cdc.gov)
  • Houston, Texas oncologist, Atisha Manhas, M.D., told dailyRx, 'Imatinib and other medications in its class (tyrosine kinase inhibitors) revolutionized the treatment of CML. (rxwiki.com)
  • Ongoing work is focused on understanding the biochemical and physiologic functions of the three mammalian Cbl proteins in epithelial cells and elucidating the differences in their specificity and/or function. (cancer.gov)
  • Our previous studies revealed that the levels of protein tyrosine phosphorylation regulate a balance between cell-cell and cell-ECM adhesions in epithelial cells (7) . (aacrjournals.org)
  • Using oncogene-transformed mammary epithelial cells, we showed that elevated tyrosine kinase activity weakens cell-cell contacts and promotes ECM adhesions (7) . (aacrjournals.org)
  • FLT3 ( FMS -related tyrosine kinase 3) acts as an oncogene in myeloid neoplasms which is associated with several signal transduction pathways. (hindawi.com)
  • Activation of this gene may be an important early step in cell growth and intracellular signal transduction pathways triggered in response to certain neural peptides or to cell interactions with the extracellular matrix. (genetex.com)
  • Phosphorylation of Syk Activation Loop Tyrosines Is Essential for Syk Function. (crossref.org)
  • Activation of receptor tyrosine kinases in these tumour areas by growth factors expressed by surrounding stromal cells phosphorylate β-catenin at tyrosine residues, which is thought to increase β-catenin nuclear translocation and tumour invasiveness. (eur.nl)
  • The Abl-related gene (Arg) requires its F-actin-microtubule cross-linking activity to regulate lamellipodial dynamics during fibroblast adhesion. (nih.gov)
  • This protein can also down-regulate p53 function and thus modulate cell growth and apoptosis. (cancerindex.org)
  • The mutant proteins often retain some of their capabilities but are no longer sensitive to the controls that regulate the normal form of the protein. (cancerquest.org)
  • 1) We study Cbl proteins, a family of ubiquitin ligases that negatively regulate signaling by receptor tyrosine kinases. (cancer.gov)
  • Understanding the mechanisms that regulate signaling by these kinases should uncover new ways to inhibit cancer cell growth. (cancer.gov)
  • We are investigating the function of Cbl proteins, a family of proteins that regulate tyrosine kinase activity. (cancer.gov)
  • In general, mRNA levels of ECM and collagen genes have been found to be downregulated in both the adult mouse sclera [ 6 ] and cornea [ 7 ] when compared with samples from an earlier developmental stage. (molvis.org)
  • This interaction inhibits its tyrosine-kinase activity. (lu.se)
  • Elevated levels of protein tyrosine phosphorylation contribute to a malignant phenotype, although the tyrosine kinases that are responsible for this signaling remain largely unknown. (aacrjournals.org)
  • Malignant cells often have increased interactions with surrounding ECM 3 proteins, which provide linkages and signals that promote several aspects of metastasis (6) . (aacrjournals.org)
  • The JAK2 protein is especially important for controlling the production of blood cells from hematopoietic stem cells. (medlineplus.gov)
  • To overcome these difficulties, scientists are working on an approach that would target another protein - the so-called JAK2 kinase. (rxwiki.com)
  • As a member of the ERM protein family, this protein serves as an intermediate between the plasma membrane and the actin cytoskeleton. (thermofisher.com)
  • Cbl proteins belong to the RING finger class of ubiquitin protein ligases (E3s) and function as E3s for activated tyrosine kinases. (cancer.gov)
  • This first category also includes genes that contribute to tumor growth by inhibiting cell death. (cancerquest.org)
  • The encoded protein is a member of the FAK subfamily of protein tyrosine kinases but lacks significant sequence similarity to kinases from other subfamilies. (genetex.com)
  • This Non-receptor tyrosine-protein kinase plays an important role in the regulation of cell growth, differentiation, migration and immune response. (wikipedia.org)
  • Regulation of MT dynamics via direct binding of an Abl family kinase. (nih.gov)
  • Ion channels, located on the membrane of T cells, are the effectors which link antigen recognition to T cell function and gene regulation by controlling calcium homeostasis. (uc.edu)
  • The online tools DAVID, Reactome, and AmiGO were employed for annotation, visualization, and integration of DEGs related to HT and PTC, and the STRING database and Cytoscape software were applied to predict and visualize protein-protein networks (PPIs) for DEG-encoded proteins. (medsci.org)
  • What pathways are this gene/protein implicaed in? (cancerindex.org)
  • The aim of this study was to identify the genes and pathways underlying the growth of the mouse sclera during postnatal development. (molvis.org)
  • This protein plays a key role in cell surface structure adhesion, migration and organization, and it has been implicated in various human cancers. (thermofisher.com)
  • To identify tyrosine kinases that control tumor cell adhesion, we developed novel technologies to generate monoclonal antibodies against tyrosine kinases in cancer cells (8) . (aacrjournals.org)
  • 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)
  • The CD34 protein is a hematopoietic progenitor cell antigen that occurs in a variety of mesenchymal tumors. (medscape.com)
  • CSK acts by suppressing the activity of the Src family of protein kinases by phosphorylation of Src family members at a conserved C-terminal tail site in Src. (wikipedia.org)
  • Upon phosphorylation by other kinases, Src-family members engage in intramolecular interactions between the phosphotyrosine tail and the SH2 domain that result in an inactive conformation. (wikipedia.org)
  • The protein encoded by this gene belongs to the histone deacetylase/acuc/apha family. (cancerindex.org)
  • 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)
  • 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)
  • Belongs to the tyr protein kinase family. (lu.se)
  • Wnts are a family of genes that have been implicated in many human tumours, so far mainly studied in colorectal cancer where activated Wnt signalling occurs in a vast majority of tumours. (lu.se)
  • receptor tyrosine kinase exists like a transmembrane protein and as a soluble molecule. (exposed-skin-care.net)
  • It was suggested that Tgfβ1 could possibly act as a signaling molecule in controlling collagen gene expression and modulate ECM during ocular growth. (molvis.org)
  • Brain and muscle Arnt-like protein-1 ( BMAL1 ) knockout mice exhibit accelerated aging, abnormal glucose metabolism, and impaired adipocyte differentiation, among other phenotypes, which are effects associated with the BMAL1 gene. (go.jp)
  • Analysis of polymorphisms of genes associated with folate-mediated one-carbon metabolism and neural tube defects in Chinese Han Population. (cdc.gov)
  • 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)
  • Perilipin 1 binds to aquaporin 7 in human adipocytes and controls its mobility via protein kinase A mediated phosphorylation. (lu.se)
  • We further demonstrated that suppression of autophagy using either pharmacological inhibitors or RNA interference of essential autophagy genes enhanced cell death induced by IM in cell lines and primary CML cells. (lu.se)
  • Le pourcentage de CD44 dans les lymphocytes T périphériques était significativement plus élevé chez les patients que chez les témoins, comme détecté par la cytométrie en flux. (who.int)
  • En outre, il y avait une aug- mentation significative de la forme soluble du c-kit dans le sérum des patients atteints de pemphigus vulgaire actif par rapport aux témoins. (who.int)
  • Furthermore, patients with tumours expressing both Wnt-5a and Syk had a significantly better prognosis as compared with those displaying loss of either of or both proteins. (lu.se)
  • Search the gene expression profiles from curated DataSets in the Gene Expression Omnibus (GEO) repository. (cancerindex.org)
  • R software was used in this study to identify DEGs in HT and PTC using data in Gene Expression Omnibus (GEO). (medsci.org)
  • The TAM receptor and ligand expression was evaluated in LMS cell lines and 358 sarcoma samples by either gene expression or immunohistochemistry. (nature.com)
  • Microarray gene expression performed in 251 sarcomas revealed significantly higher expression of TYRO3 and GAS6 in LMS than other sarcomas. (nature.com)
  • In the search for signals that cause breast cancer, many lines of investigation have linked cancer with elevated expression or altered function of receptor tyrosine kinases (1) . (aacrjournals.org)
  • Changes of gene expression by lysophosphatidylcholine in vascular endothelial cells, 12 upregulated distinct genes including 5 cell growth-related, 3 thrombosis-related. (researchmap.jp)
  • Protein tyrosines and protein kinase C are required for gene expression of monocyte chemoattractant protein-1 in human monocytes. (researchmap.jp)
  • Protein kinase C-mediated inhibition of cyclin A expression in human vascular endothelial cells. (researchmap.jp)
  • The gene expression of Ppargc1a varied during scleral growth from week 1 to 2, week 2 to 3, week 3 to 6, and week 6 to 8 and was found to interact with a different set of genes at different scleral growth stages. (molvis.org)
  • Gene expression of eye diseases should be studied as early as postnatal weeks 1-2 to ensure that any changes in gene expression pattern during disease development are detected. (molvis.org)
  • We found that Wnt-5a protein expression is reduced in many invasive breast carcinomas and that reduced Wnt-5a expression in the primary tumour strongly correlates with an increased risk of metastatic disease and shorter survival. (lu.se)
  • The expression of Wnt-5a protein co-variates with that of Syk, a tyrosine kinase that is lost in up to 30% of invasive breast carcinomas and associated with poor prognosis. (lu.se)
  • Despite the co-expression, loss of Wnt-5a and Syk protein appear to be regulated at the translational and transcriptional levels, respectively. (lu.se)