AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesDisciplines and OccupationsInformation Science
Neuregulin-1NeuregulinsReceptor, erbB-3Receptor, erbB-2Genes, erbBReceptor, Epidermal Growth FactorEpidermal Growth FactorOncogene Proteins v-erbBGenes, erbB-2Signal TransductionBreast NeoplasmsCell Line, TumorQuinazolinesPhosphorylationMucin-4Proto-Oncogene Proteins c-aktGene Expression Regulation, NeoplasticDimerizationLigandsPhosphatidylinositol 3-KinasesProto-Oncogene ProteinsCell ProliferationMammary Neoplasms, ExperimentalAntineoplastic AgentsGRB7 Adaptor ProteinTyrphostinsTumor Cells, CulturedTransforming Growth Factor alphaAntibodies, Monoclonal, HumanizedGene AmplificationProtein Kinase InhibitorsDrug Resistance, NeoplasmMammary Glands, AnimalCell Transformation, NeoplasticHSP90 Heat-Shock ProteinsSchwann CellsProtein BindingMice, TransgenicIntercellular Signaling Peptides and ProteinsBenzothiazolesEnzyme ActivationNonheme Iron ProteinsReceptor Protein-Tyrosine KinasesAntibodies, MonoclonalImmunohistochemistryCell DivisionTyrosineTransfectionBlotting, WesternRNA, MessengerDown-RegulationProtein Structure, TertiaryCell LineCell MovementCell SurvivalProtein IsoformsMolecular Sequence DataApoptosisReverse Transcriptase Polymerase Chain ReactionRNA, Small InterferingMammary Glands, HumanAdaptor Proteins, Signal TransducingExtracellular Signal-Regulated MAP KinasesImmunoprecipitationMice, NudeMutationXenograft Model Antitumor AssaysCell Growth ProcessesTranscription Factor AP-2Amino Acid SequenceNeoplasm InvasivenessEstrogen Receptor Modulators
KinaseEpidermalHER2EGFRMembers of the ERBB familySignaling pathwayOverexpressionAntibodiesAntibodyTumorGenesApoptosisPhosphorylationInhibitorCancersExtracellularTyrosine residuesTargetsAvianPrognosisHumanHeterodimerNode-positive breast cancerActivationLigandKinasesMutationsPolymerase Chain ReAmplificationCellTherapeuticPurification
Kinase19
  • 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)
  • Receptor tyrosine-protein kinase erbB-2 is a protein that normally resides in the membranes of cells and is encoded by the ERBB2 gene. (wikipedia.org)
  • lacks kinase domain), and erbB-4. (wikipedia.org)
  • Signaling pathways activated by HER2 include: mitogen-activated protein kinase (MAPK) phosphoinositide 3-kinase (PI3K/Akt) phospholipase C γ protein kinase C (PKC) Signal transducer and activator of transcription (STAT) In summary, signaling through the ErbB family of receptors promotes cell proliferation and opposes apoptosis, and therefore must be tightly regulated to prevent uncontrolled cell growth from occurring. (wikipedia.org)
  • Receptor tyrosine-protein kinase erbB-2, also known as HER2/Neu (human epidermal growth factor receptor 2), is a member of the human epidermal growth factor receptor family. (meridianbioscience.com)
  • Canertinib (CI-1033, PD 183805) is a pan-erbB tyrosine kinase inhibitor. (lclabs.com)
  • It selectively inhibits erbB1 (epidermal growth factor receptor), erbB2, erbB3, and erbB4 without blocking tyrosine kinase activity of many other receptors such as platelet-derived growth factor receptor, fibroblast growth factor receptor, and insulin receptor. (lclabs.com)
  • The degradative pathway of ErbB receptor tyrosine kinases stimulated by tyrosine kinase inhibitors appears to be chaperone mediated, and thus is similar to the pathways activated by the heat shock protein 90 (Hsp90) antagonist geldanamycin and by stress-induced mechanisms. (lclabs.com)
  • Phosphorylation of EGFR at certain residues is also mediated by Src-non-receptor kinase. (thermofisher.com)
  • A cell surface protein-tyrosine kinase receptor that is overexpressed in a variety of ADENOCARCINOMAS. (bvsalud.org)
  • We found that this genetic dependency could be elicited with the clinical BTK/ERBB2 kinase inhibitor, ibrutinib. (icr.ac.uk)
  • However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. (arigobio.com)
  • Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. (arigobio.com)
  • Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) have been emerged as the standard selection in non-small cell lung cancer (NSCLC) patients with EGFR sensitive mutations. (biomedcentral.com)
  • Owing to the well-established beneficial outcomes of clinical trials, epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), have been approved as the standard regimens in patients with non-small cell lung cancer (NSCLC) harboring EGFR sensitive mutations [ 1 ]. (biomedcentral.com)
  • 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)
  • 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)
  • Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. (drugcentral.org)
  • Antibody-drug conjugates targeting receptor tyrosine-protein kinase erbB-2 ( ERBB2, HER2 ) have emerged as promising targeted options for HER2 -mutant NSCLC. (egfrcancer.org)
Epidermal12
HER218
  • Detects human ErbB2/Her2 in direct ELISAs. (rndsystems.com)
  • Detection of ErbB2/Her2 in MCF-7 human cell line by Flow Cytometry. (rndsystems.com)
  • MCF-7 human cell line was stained with Human Anti-Human ErbB2/Her2 (Research Grade Trastuzumab Biosimilar) Alexa Fluor® 700-conjugated Monoclonal Antibody (Catalog # FAB9589N, filled histogram) or irrelevant antibody (open histogram). (rndsystems.com)
  • Recombinant human ErB2 / Her2 (1129-ER) blocks anti-ErbB2 mediated inhibition of SK-BR-3 human breast cancer proliferation. (novusbio.com)
  • 875. The ED 50 for this effect is 0.3-1.2 μg/mL in the presence of 0.6 µg/mL Anti-Human ErbB2/Her2 Monoclonal Antibody (Trastuzumab, Catalog # MAB9589 ). (novusbio.com)
  • But contrary to other members of the ERBB family, HER2 does not directly bind ligand. (wikipedia.org)
  • HER2 activation results from heterodimerization with another ERBB member or by homodimerization when HER2 concentration are high, for instance in cancer. (wikipedia.org)
  • Molecular cloning of the gene showed that HER2, Neu, and ErbB-2 are all encoded by the same orthologs. (wikipedia.org)
  • HER2 can heterodimerise with any of the other three receptors and is considered to be the preferred dimerisation partner of the other ErbB receptors. (wikipedia.org)
  • HER2 proteins have been shown to form clusters in cell membranes that may play a role in tumorigenesis. (wikipedia.org)
  • Synthetic peptide around the C-terminus of Human HER2 / ErbB2. (arigobio.com)
  • Immunohistochemistry: Formalin-fixed and paraffin-embedded Human breast cancer tissue stained with ARG66357 anti-ERBB2 / HER2 antibody [SQab1890] at 1:500 dilution. (arigobio.com)
  • Confocal immunofluorescent analysis of MDA-MB-453 cells (left) and MDA-MB-231 cells (right), using HER2/ErbB2 (29D8) Rabbit mAb (green). (cellsignal.com)
  • Flow cytometric analysis of MDA-MB-468 cells (blue) and SKBR3 cells (green) using HER2/ErbB2 (29D8) Rabbit mAb (solid lines) or a concentration-matched Rabbit (DA1E) mAb IgG XP ® Isotype Control #3900 (dashed lines). (cellsignal.com)
  • Western blot analysis of cell extracts from various cell lines, using HER2/ErbB2 (29D8) Rabbit mAb. (cellsignal.com)
  • Immunohistochemical analysis of paraffin-embedded human breast carcinoma, using HER2/ErbB2 (29D8) Rabbit mAb. (cellsignal.com)
  • Immunohistochemical analysis of paraffin-embedded human breast carcinoma using HER2/ErbB2 (29D8) RmAb in the presence of control peptide (left) or HER2/ErbB2 Blocking Peptide #1059 (right). (cellsignal.com)
  • Immunohistochemical analysis of paraffin-embedded SKBr3 (high HER2) (left), MDA-MB-453 (moderate HER2) (middle) and MDA-MB-468 (low HER2) (right), using HER2/ErbB2 (29D8) Rabbit mAb. (cellsignal.com)
EGFR9
  • It inhibits both ERBB2 and EGFR activity. (antibodyguide.com)
  • ErbB-2 was named for its similarity to ErbB (avian erythroblastosis oncogene B), the oncogene later found to code for EGFR. (wikipedia.org)
  • In the current study, we examined the effects of recombinant ERRP on the growth and ligand-induced activation of multiple members of erbB family in three pancreatic cancer cell lines that express varying levels of EGFR and other member(s) of its family, specifically HER-2. (aacrjournals.org)
  • ERRP also inhibited ligand-induced activation of EGFR, HER-2, and HER-3 (ErbB3). (aacrjournals.org)
  • In contrast, Erbitux and Herceptin only partially or modestly inhibited activation of EGFR, HER-2, and HER-3. (aacrjournals.org)
  • EGFR belongs to the HER/ERbB family of proteins that includes three other receptor tyrosine kinases, ERbB2, ERbB3, ERbB4. (thermofisher.com)
  • Phosphorylation of EGFR at Y1086 specifically allows binding of the adaptor protein GRB2, leading to activation of the MAPK pathway. (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)
Members of the ERBB family1
  • Discovering a specific agent, which targets multiple members of the erbB family, would be important in pancreatic cancer therapy. (aacrjournals.org)
Signaling pathway1
  • Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. (arigobio.com)
Overexpression5
  • 32 % of patients exhibited overexpression of HER-2/neu. (thieme-connect.de)
  • Prospective studies correlating HER-2/neu overexpression with prognosis might provide additional data. (thieme-connect.de)
  • c-erbB-2 protein overexpression in breast cancer is a risk factor in patients with involved and uninvolved lymph nodes. (thieme-connect.de)
  • Amplification of the ErbB-2 gene and overexpression of its product has been detected in almost 40% of primary human breast tumors, which correlates with poor prognosis in node positive breast cancer. (activemotif.com)
  • ErbB-2 overexpression is also observed in ovarian, gastric, salivary and non-small cell lung carcinomas. (activemotif.com)
Antibodies6
  • We have obtained monoclonal antibodies to the human neu protein by immunizing a Balb/c mouse with a Balb/c cell line expressing the human neu gene by transfection. (prinsesmaximacentrum.nl)
  • The monoclonal antibodies reacted with neu protein on intact cells by immunofluorescence and immunoprecipitated neu in metabolically labeled cells, also in the presence of tunicamycin. (prinsesmaximacentrum.nl)
  • We tested possible down-modulating effects of these monoclonal antibodies on SKBR-3 mammary tumor cells, which express high levels of wild-type human neu protein. (prinsesmaximacentrum.nl)
  • In contrast, the antibodies induced 50-65% down-modulation in NIH3T3 cells expressing the mutated human neu protein and could inhibit these cells to form colonies in soft agar. (prinsesmaximacentrum.nl)
  • Sensitivity of HER-2/neu antibodies in archival tissue samples of invasive breast carcinomas. (thieme-connect.de)
  • Each FACE ErbB-2 Kit provides 96 rxns each of 2 antibodies that enable you to monitor and compare the levels of both phosphorylated and total ErbB-2. (activemotif.com)
Antibody11
  • Trastuzumab (Herceptin) is an antibody that targets ERBB2 and has been approved for the treatment of breast cancer. (antibodyguide.com)
  • Immunogen: This Mouse Erbb2 antibody is generated from rabbits immunized with a KLH conjugated synthetic peptide between 531-559 amino acids from the Central region of mouse Erbb2. (hatinhibitor.com)
  • Purification: This antibody is purified through a protein A column, followed by peptide affinity purification. (hatinhibitor.com)
  • For continuous use, store undiluted antibody at 2-8°C for up to a week. (arigobio.com)
  • The Y877 kit contains phospho-ErbB-2 antibody that recognizes ErbB-2 only when phosphorylated at Tyr877, while the Y1248 kit provides a phospho-antibody that recognizes ErbB-2 only when phosphorylated at Tyr1248. (activemotif.com)
  • Each kit contains a total-ErbB-2 antibody that recognizes ErbB-2 regardless of its phosphorylation state. (activemotif.com)
  • The FACE ErbB-2 (Y877) Kit contains a phospho-ErbB-2 antibody that was raised in rabbit against a synthetic phospho-peptide corresponding to residues surrounding phosphorylated Tyr877 of human ErbB-2 and recognizes ErbB-2 only when phosphorylated at Tyr877. (activemotif.com)
  • The total-ErbB-2 antibody supplied in the FACE ErbB-2 Kits recognizes ErbB-2 protein regardless of its phosphorylation site. (activemotif.com)
  • Each well is then incubated with a primary antibody specific for the activated protein of interest. (activemotif.com)
  • FACE Kits also contain primary antibody specific for the native inactive protein, so you can monitor both native and activated protein levels in the same experiment. (activemotif.com)
  • Anti-rabbit IgG (H+L), F(ab')2 Fragment (Alexa Fluor ® 488 Conjugate) #4412 was used as a secondary antibody. (cellsignal.com)
Tumor1
  • 5 Beckmann M W, Niederacher D, Schnurch H G, Bender H G. The erbB gene family: significance for tumor development, prognosis and new therapeutic modalities. (thieme-connect.de)
Genes1
  • Involved in the transcription of rRNA genes by RNA Pol I and enhances protein synthesis and cell growth. (arigobio.com)
Apoptosis2
  • Canertinib inhibited erbB receptor phosphorylation and induced growth inhibition and apoptosis at concentrations of 1 µM or more. (lclabs.com)
  • In both MYC and ERBB2 amplified tumour cells, ibrutinib downregulated ERK-mediated signal transduction, cMYC Ser-62 phosphorylation and levels of MYC protein, and elicited G1 cell cycle arrest and apoptosis, suggesting that this drug could be used to treat biomarker-selected groups of patients with oesophageal cancer. (icr.ac.uk)
Phosphorylation4
  • It not only inhibits tyrosine phosphorylation but also enhances ubiquitinylation and accelerates endocytosis and subsequent intracellular destruction of ErbB-2 molecules. (lclabs.com)
  • Essential erbB family phosphorylation in osteosarcoma as a target for CI-1033 inhibition. (lclabs.com)
  • 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)
Inhibitor1
  • Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo. (lclabs.com)
Cancers2
  • Amplification, also known as the over-expression of the ERBB2 gene, occurs in approximately 15-30% of breast cancers. (wikipedia.org)
  • The erbB family of receptor tyrosine kinases plays critical roles in human cancers, including pancreatic cancer. (aacrjournals.org)
Extracellular1
  • It binds to the extracellular domain of ERBB2 and inhibits its activity. (antibodyguide.com)
Tyrosine residues2
  • Dimerisation results in the autophosphorylation of tyrosine residues within the cytoplasmic domain of the receptors and initiates a variety of signaling pathways. (wikipedia.org)
  • Autophosphorylation occurs in trans, i.e. one subunit of the dimeric receptor phosphorylates tyrosine residues on the other subunit (Probable). (arigobio.com)
Targets3
  • Lapatinib (Tykerb) is another drug that targets ERBB2. (antibodyguide.com)
  • A database to provide information about the known and explored therapeutic protein and nucleic acid targets, the targeted disease, pathway information and the corresponding drugs directed at each of these targets. (idrblab.net)
  • Because of this, ErbB-2 is one of the major drug targets for breast cancer and other cancer treatments. (activemotif.com)
Avian1
  • ERBB is abbreviated from erythroblastic oncogene B, a gene originally isolated from the avian genome. (wikipedia.org)
Prognosis1
  • The HER-2/neu onkogene may play a role in the prognosis and management of patients with breast cancer. (thieme-connect.de)
Human5
  • Measured by its ability to block anti-ErbB2 mediated inhibition of SK‑BR‑3 human breast cancer cell proliferation. (novusbio.com)
  • ERBB2, a known proto-oncogene, is located at the long arm of human chromosome 17 (17q12). (wikipedia.org)
  • We also used NIH3T3 cells transfected with either a normal or a mutated human neu gene, encoding a protein with a valine to glutamic acid substitution in the transmembrane domain. (prinsesmaximacentrum.nl)
  • 2 Barnes D M, Lammie G A, Millis R R, Gullick W L, Allen D S, Altman D G. An immunohistochemical evaluation of c-erbB-2 expression in human breast carcinoma. (thieme-connect.de)
  • 14 King C R, Kraus M H, Aaronson S A. Amplification of a novel v-erbB-related gene in a human mammary carcinoma. (thieme-connect.de)
Heterodimer1
  • Activation of the erbB-2 receptor occurs through heterodimer formation with a ligand-bound erbB receptor family member. (bvsalud.org)
Node-positive breast cancer1
  • HER-2/neu amplification predicts poor survival in node-positive breast cancer. (thieme-connect.de)
Activation1
  • Following stimulation, the cells are fixed rapidly, which preserves activation-specific protein modifications. (activemotif.com)
Ligand4
  • GP30 is a potential ligand for this receptor. (hatinhibitor.com)
  • Furthermore, diverse structural alterations have been identified that cause ligand-independent firing of this receptor, doing so in the absence of receptor over-expression. (wikipedia.org)
  • Substitution of a valine for a glutamic acid or a glutamine in the transmembrane domain can result in the constitutive dimerisation of this protein in the absence of a ligand. (wikipedia.org)
  • This protein has no ligand binding domain of its own and therefore cannot bind growth factors. (arigobio.com)
Kinases2
  • The ErbB family consists of four individual plasma membrane-bound receptor tyrosine kinases. (wikipedia.org)
  • Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. (lclabs.com)
Mutations1
  • Scope includes mutations and abnormal protein expression. (cancerindex.org)
Polymerase Chain Re1
Amplification1
  • 7 Borg A, Baldetorp B, Ferno M, Killander D, Olsson H, Sigurdsson H. ERBB2 amplification in breast cancer with a high rate of proliferation. (thieme-connect.de)
Cell1
Therapeutic1
  • ERBB2 has been identified as a therapeutic target for breast cancer therapy. (antibodyguide.com)
Purification1