• Recently, we isolated a novel negative regulator of epidermal growth factor receptor (EGFR), termed EGFR-related protein (ERRP), whose expression attenuates EGFR activation. (aacrjournals.org)
  • HER-2 (ErbB2) is a 185-kDa transmembrane tyrosine kinase with extensive homology to the epidermal growth factor receptor (EGFR). (touchoncology.com)
  • Gene Ontology (GO) analysis indicated that these DEGs were significantly related to the positive regulation of epidermal growth factor-activated receptor activity, the positive regulation of the ERBB (erb-b2 receptor tyrosine kinase) signaling pathway, the differentiation of trophoblast giant cells, oxygen transport, immune-related pathways, and inflammation-related pathways. (ankylosingspondylitistreatmentreport.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)
  • HER2 positive breast cancer is identified by the overexpression of human epidermal growth factor receptor-2 (HER2) protein in tumor tissue and results in an increased rate of cell proliferation. (her2support.org)
  • Interestingly reduces tumourigenesis in vivo4 5 These findings have spurred interest in supplementing clinical TH287 Erb1 (also known as epidermal growth factor receptor (EGFR)) inhibition with synergistic targeting of ADAM171. (bioskinrevive.com)
  • Binding of epidermal growth factor to EGFR induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation, differentiation, motility, and cell survival (1). (signalchem.com)
  • 1. Wang K, et al: Epidermal growth factor receptor-deficient mice have delayed primary endochondral ossification because of defective osteoclast recruitment. (signalchem.com)
  • Tyrosine kinases are mainly classified as receptor tyrosine kinases and non-receptor tyrosine kinases, including crucial members.Epidermal growth factor receptor (EGFR) belongs to the ERBB family of receptor tyrosine kinases along with three other closely related receptors, namely HER-2, HER-3 and HER-4. (frontiersin.org)
  • R&D Systems offers a wide selection of tools to Epidermal Growth Factor (EGF) Family members and their EGF R/ErbB receptors. (rndsystems.com)
  • It is also frequently called HER2 (from human epidermal growth factor receptor 2 ) or HER2/neu . (iiab.me)
  • HER2 is a member of the human epidermal growth factor receptor (HER/EGFR/ERBB) family. (iiab.me)
  • HER2 is so named because it has a similar structure to human epidermal growth factor receptor, or HER1. (iiab.me)
  • Renal epidermal growth factor receptor (EGFR) signaling is activated in models of diabetic nephropathy (DN), and inhibition of the EGFR signaling pathway protects against the development of DN. (diabetesjournals.org)
  • Lung cancer with epidermal growth factor receptor (EGFR)-activating mutations responds favorably to the EGFR tyrosine kinase inhibitors gefitinib and erlotinib. (aacrjournals.org)
  • Tyrosine kinase inhibitors (TKIs) against the human epidermal growth factor receptor (EGFR) are now standard treatment in the clinic for patients with advanced EGFR mutant non-small-cell lung cancer (NSCLC). (researchgate.net)
  • The epidermal growth factor receptor (EGFR) is among the most well-studied signaling pathways in cancer progression. (bio-biz-navi.com)
  • Introduction Epidermal development element receptor (EGFR) was the 1st discovered from the ErbB category of receptor tyrosine kinases with a total of four users: Erbb1/EGFR, ErbB2/Her2, ErbB3 and ErbB4. (bio-biz-navi.com)
  • 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)
  • Here, we report the synthesis, good biocompatibility, and in vivo evaluation of a new small molecule near-infrared (NIR) fluorescence probe by the conjugation of Lapatinib to S0456 (LP-S). We show that like Lapatinib, LP-S binds to the epidermal growth factor receptor (EGFR) resulting in high quality fluorescence imaging of metastatic lymph nodes in OSCC mouse models. (bvsalud.org)
  • Fulvestrant (F), lapatinib (L), and paclitaxel (P) are hydrophobic, anticancer drugs used in the treatment of estrogen receptor (ER) and epidermal growth factor receptor (EGFR)-positive breast cancer. (bvsalud.org)
  • The identification of EGFR mutations and the discovery of their exquisite sensitivity to epidermal growth factor receptor (EGFR) inhibitors dramatically changed the therapeutic routine for lung adenocarcinoma (LADC) patients 1 , 2 , 3 . (nature.com)
  • This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. (nih.gov)
  • The epidermal growth factor receptor (EGFR) tyrosine kinase (TK) plays an important role in the pathogenesis of NSCLC. (bmj.com)
  • Alterations in receptor tyrosine kinases (TKs), such as the epidermal growth factor receptor (EGFR) and insulin-like growth factor receptor 1, include overexpression, amplification or mutations. (bmj.com)
  • Novel therapeutic agents, in particular those that specifically target members of the human epidermal growth factor receptor (HER (ErbB1)) pathway, have shown encouraging therapeutic efficacy. (bmj.com)
  • Mice lacking the epidermal growth factor receptor (EGFR) develop epithelial defects and a neurodegenerative disease and die within the first month of birth. (silverchair.com)
  • This family, which includes epidermal growth factor receptor (EGFR), plays a pivotal role in normal cell growth, lineage determination, repair, and functional differentiation. (medscape.com)
  • 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)
  • In head and neck squamous cell carcinoma (HNSCC) cancer, DNAJA3 suppresses cell proliferation, anchorage-independent growth, cell motility, and cell invasion by attenuating EGFR and, downstream the signaling pathway, AKT. (wikipedia.org)
  • Neratinib is an investigational, orally administered, irreversible inhibitor of the ErbB1 (EGFR), ErbB2 (HER2) and ErbB4 (HER4) kinases. (her2support.org)
  • We demonstrate that TH287 PACS-2 controls ADAM17 cell-surface availability shedding of ErbB ligands and EGFR activity in vivo. (bioskinrevive.com)
  • EGFR is the receptor for members of the EGF family and is a transmembrane glycoprotein that has tyrosine kinase activity. (signalchem.com)
  • Activation of EGFR triggers mitogenic signaling in gastrointestinal mucosa, and its expression is upregulated in colon cancers and most neoplasms (2). (signalchem.com)
  • Activation of EGFR triggers activation of the ERK-signaling pathway in normal gastric epithelial and colon cancer cell lines. (signalchem.com)
  • 2. Kobayashi S, et al: EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. (signalchem.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)
  • EGFR and HER-2, lead to autophosphorylation of the intracellular domain through tyrosine kinase activity and subsequent stimulation of downstream cascade that may result in proliferation, suppression of apoptosis, metastasis and angiogenesis. (frontiersin.org)
  • They have mainly been identified as important targets for several types of cancer such as EGFR for non-small-cell lung cancer, glioma and colorectal cancer, HER-2 for breast and colorectal cancers and Abl for chronic myeloid leukemia. (frontiersin.org)
  • Aberrant activity of tyrosine kinases, in particular EGFR and Abl, have been reported to induce apoptosis and cell cycle arrest in response to a wide range of stimuli resulting in neurodegeneration and neuroinflammation. (frontiersin.org)
  • ErbB-2 was named for its similarity to ErbB (avian erythroblastosis oncogene B), the oncogene later found to code for EGFR. (iiab.me)
  • We have now determined that in cultured podocytes, high glucose led to increases in activation of EGFR signaling but decreases in autophagy activity as indicated by decreased beclin-1 and inhibition of LC3B autophagosome formation as well as increased rubicon (an autophagy inhibitor) and SQSTM1 (autophagy substrate). (diabetesjournals.org)
  • Here, we showed that hepatocyte growth factor (HGF), a ligand of MET oncoprotein, induces gefitinib resistance of lung adenocarcinoma cells with EGFR -activating mutations by restoring the phosphatidylinositol 3-kinase/Akt signaling pathway via phosphorylation of MET, but not EGFR or ErbB3. (aacrjournals.org)
  • First-generation EGFR TKIs, binding competitively and reversibly to the ATP-binding site of the EGFR tyrosine kinase domain, have resulted in a significant improvement in outcome for NSCLC patients with activating EGFR mutations (L858R and Del19). (researchgate.net)
  • Although they exhibited promising anti-T790M activity in the laboratory, their clinical activity among T790M+ NSCLC was poor mainly because of dose-limiting toxicity due to simultaneous inhibition of wild-type EGFR. (researchgate.net)
  • General, we help with the hypothesis that fundamental adjustments in EGFR signaling between main and metastatic tumors, an activity we term the EGFR paradox, donate to the medically observed inherent level of resistance to EGFRi. (bio-biz-navi.com)
  • 2 Since its finding, EGFR continues to be characterized like a mediator of a multitude of signal transduction occasions that control cell proliferation, migration and success. (bio-biz-navi.com)
  • 7 Another setting of EGFR activation in malignancy is usually activating somatic mutations that bring about constitutive kinase activity, and they are especially common in NSCLC (examined in Morgensztern examined the effectiveness of merging gefitinib with docetaxel in metastatic BC in comparison with docetaxel only. (bio-biz-navi.com)
  • Sinalização aumentada através do receptor do fator de crescimento epitelial (EGFR), sistema de quinases proteicas ativadas por mitógenos (MAPK) e via da fosfatidilinositol 3-quinase (PI3K) assim como estimulação do complexo de início de tradução (CIT) foram caracterizados em linhagens celulares e amostras tumorais de CCR. (usp.br)
  • Signaling intensification through epithelial growth factor receptor (EGFR), mitogenactivated protein kinase (MAPK) pathway, Phosphatidylinositol 3-kinase (PI3K) pathway and overactivation of the translation initiation complex (TIC) has been previously characterized in RCC cell lines and tumor samples. (usp.br)
  • We demonstrate that EGFR G724S limits the activity of third-generation EGFR inhibitors both in vitro and in vivo. (nature.com)
  • Systematic inhibitor screening and in-depth kinetic profiling validate these findings and show that second-generation EGFR inhibitors retain kinase affinity and overcome EGFR G724S -mediated resistance. (nature.com)
  • Alternative by-pass mechanisms involving MET amplification or activation of the MAPK pathway may also play a role in the development of resistance to third-generation EGFR inhibitors 14 , 15 , 17 . (nature.com)
  • 3 The development of molecular targeted therapies aimed at these molecular alterations has generated great optimism for the treatment of cancers such as NSCLC, and drugs targeting the EGFR tyrosine kinase domain are now available. (bmj.com)
  • Selective compounds have been developed that target either the extracellular ligand-binding region of the EGFR (including a number of monoclonal antibodies [MAbs], immunotoxins, and ligand-binding cytotoxic agents) or the intracellular tyrosine kinase region (including various small-molecule inhibitors). (medscape.com)
  • Binding of Sema4D to plexin-B1 stimulates the intrinsic tyrosine kinase activity of ErbB-2, resulting in the phosphorylation of both plexin-B1 and ErbB-2. (rupress.org)
  • Our data indicate that ErbB-2 is an important component of the plexin-B receptor system and that ErbB-2-mediated phosphorylation of plexin-B1 is critically involved in Sema4D-induced RhoA activation, which underlies cellular phenomena downstream of plexin-B1, including axonal growth cone collapse. (rupress.org)
  • Another disease, psoriasis, is a chronic inflammatory skin disease that results from the absence of DNAJA3 activity, which then results in the activation of MK5, increased phosphorylation of HSP27, increased actin cytoskeleton organization, and hyperthickened skin. (wikipedia.org)
  • It not only inhibits tyrosine phosphorylation but also enhances ubiquitinylation and accelerates endocytosis and subsequent intracellular destruction of ErbB-2 molecules. (lclabs.com)
  • Canertinib inhibited erbB receptor phosphorylation and induced growth inhibition and apoptosis at concentrations of 1 µM or more. (lclabs.com)
  • Essential erbB family phosphorylation in osteosarcoma as a target for CI-1033 inhibition. (lclabs.com)
  • Each kit contains a total-ErbB-2 antibody that recognizes ErbB-2 regardless of its phosphorylation state. (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)
  • 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)
  • Downstream signaling from these receptors proceeds TSPAN10 via tyrosine phosphorylation. (bio-biz-navi.com)
  • The ER is activated by estrogen binding and also by phosphorylation through the PI3K/Akt pathway ( 4 ). (iiarjournals.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)
  • In this study, we provide multiple lines of evidence showing that the post-translational phosphorylation of MSY3 by Akt kinase modulates the MSY3 repression of myogenin. (biomedcentral.com)
  • Skeletal muscle and myogenic C2C12 cells were used to study the effects of MSY3 phosphorylation in vivo and in vitro on its sub-cellular localization and activity, by blocking the IGF1/PI3K/Akt pathway, by Akt depletion and over-expression, and by mutating potential MSY3 phosphorylation sites. (biomedcentral.com)
  • In C2C12 myogenic cells, blocking the IGF1/PI3K/Akt pathway using LY294002 inhibitor reduced MSY3 phosphorylation levels resulting in its accumulation in the nuclei. (biomedcentral.com)
  • MSY3 phosphorylation by Akt in vitro impaired its binding at the MyogHCE element, while blocking Akt increased MSY3 binding activity. (biomedcentral.com)
  • These results support the hypothesis that MSY3 phosphorylation by Akt interferes with MSY3 repression of myogenin circuit activity during muscle development. (biomedcentral.com)
  • The metalloproteinase ADAM17 activates ErbB signalling by releasing ligands from the cell surface a key step underlying epithelial development growth and tumour progression. (bioskinrevive.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)
  • Among one of the actionable targets is the fibroblast growth factor receptor (FGFR) pathway, triggered by specific ligands. (123dok.org)
  • The FGFR family is characterized by four receptors, binding to 18 ligands called fibroblast growth factors (FGFs), employing heparin as a co-factor [2-4]. (123dok.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)
  • The final cleavage is performed by -secretase, whose substrates include all four Notch receptors and their ligands as well as -amyloid precursor protein, E-cadherin, CD44, ErbB-4, and ephrin-B1 [2-8]. (scienceexhibitions.org)
  • The ERBB family of type 1 receptor tyrosine kinases and their ligands have crucial functions during mammopoiesis, but the signaling networks that ultimately regulate ERBB activity in the breast have remained elusive. (silverchair.com)
  • While it has been recognised for some time that overexpression of HER-2 is a poor prognostic factor in breast cancer, it was the advent of trastuzumab, a humanised monoclonal antibody directed against the extracellular domain of HER-2, that has allowed clinicians to better understand the natural history of HER-2-positive metastatic breast cancer. (touchoncology.com)
  • 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)
  • 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)
  • published on the web 30 OctoberINTRODUCTION The important mechanisms that cause a constitutive activation of the PI3KAkt pathway are mutations and overexpression of upstream receptor tyrosine kinases which include erbB family members members, activating mutations of PIK3CA or RAS along with the loss of tumor suppressor protein phosphatase and tensin homolog (PTEN).1 Akt, also referred to as protein kinase B (PKB), consists of three isoforms: PKBAkt1, PKBAkt2 and PKBAkt3. (bet-bromodomain.com)
  • While ADAM17 may act in intracellular compartments its major shedding activity appears to require localization to the cell surface6-9. (bioskinrevive.com)
  • All four contain an extracellular ligand binding domain, a transmembrane domain, and an intracellular domain that can interact with a multitude of signaling molecules and exhibit both ligand-dependent and ligand-independent activity. (iiab.me)
  • FGFRs are a class of receptor tyrosine kinase (RTK) and are single-pass membrane proteins made of N-terminal extracellular (EC) domains with three immunoglobulin-like subdomains (D1, D2 and D3), a transmembrane (TM) domain with a single α-helix, and an intracellular (IC) region which includes tyrosine kinase motifs, a juxta-membrane domain and a carboxyl-terminal tail [12-14]. (123dok.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)
  • Inhibition of -secretase activity was measured by both immunoblotting and immunofluorescent microscopy in order to detect active Notch1 intracellular domain. (scienceexhibitions.org)
  • Ligand-induced Notch receptor activation requires at least two cleavages that release the intracellular domain from the cytomembrane and allow it to translocate into the nucleus where it activates its target genes [1]. (scienceexhibitions.org)
  • 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)
  • 25 Furthermore to kinase inhibitors, medical tests have also examined the addition of the ligand obstructing monoclonal antibody cetuximab towards the DNA-alkylating agent carboplatin. (bio-biz-navi.com)
  • The four currently recognized classes of endocrine-therapeutic agents available for treatment are antiestrogens, aromatase inhibitors (AI), luteinizing hormone-releasing hormone (LH-RH) agonists and progestins ( 2 ). (iiarjournals.org)
  • 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)
  • Furthermore, we observed that Z-LLNle-CHO could inhibit proteasome activity and the relative cellular sensitivity of these six breast cancer cell lines to Z-LLNle-CHO was the same as observed for three proteasome inhibitors. (scienceexhibitions.org)
  • In this study, we compared the activity and cytotoxic effects of Z-LLNle-CHO with those of two other widely used and highly specific GSIs, DAPT and L-685,458, and with those of three structurally unrelated proteasome inhibitors, MG132, lactacystin, and bortezomib. (scienceexhibitions.org)
  • The cyclin-dependent kinase (CDK) inhibitors p21 and p16 inhibit the activity of CDKs, such as CDK4. (medscape.com)
  • Another important class of tumor suppressor genes involved in cell cycle control and in the generation of human cancers is the cyclin-dependent kinase (CDK) inhibitors. (medscape.com)
  • 2) We investigate induction of apoptosis in breast cancer cells by TRAIL receptor agonists. (cancer.gov)
  • In a second project we are investigating the induction of apoptosis by activation of death receptors for the ligand TRAIL in breast and ovarian cancer cells. (cancer.gov)
  • We have shown that most breast and ovarian cancer cell lines are resistant to the induction of apoptosis by TRAIL, the ligand for the death receptors DR4 and DR5. (cancer.gov)
  • We have demonstrated that resistance to TRAIL-induced apoptosis can be overcome by co-incubation of the cells with chemotherapeutic agents, semi-synthetic retinoids (such as 4HPR), or molecularly targeted agents (such as anti-ErbB-2 antibodies). (cancer.gov)
  • 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. (iiab.me)
  • Miller JL, Velmurugan K, Cowan M, Briken V: The Type I NADH Dehydrogenase of Mycobacterium Tuberculosis Counters Phagosomal NOX2 Activity to Inhibit TNF-α-mediated Host Cell Apoptosis. (tgf-betasignal.com)
  • Involvement of C/EBPβ-related signaling pathway in methamphetamine-induced neuronal autophagy and apoptosis. (cancerindex.org)
  • Alterations in gene sequence or expression can occur in the cell-signalling and regulatory pathways involved in cell-cycle control, apoptosis, proteosome regulation and angiogenesis. (bmj.com)
  • Inhibited HER2 activities include downstream signal transduction events and cell cycle regulatory pathways, such as the cell division cycle, ultimately resulting in decreased cell proliferation. (her2support.org)
  • Breast cancer tumors that do not express hormone receptors or have amplification of Her2/Neu (so called triple-negative tumors) have a poor prognosis and no validated molecular targets. (cancer.gov)
  • Molecular cloning of the gene showed that HER2, Neu, and ErbB-2 are all encoded by the same orthologs. (iiab.me)
  • [10] [11] HER2 can heterodimerise with any of the other three receptors and is considered to be the preferred dimerisation partner of the other ErbB receptors. (iiab.me)
  • To further understand electrotactic migration of tumor cells, we performed RNA-sequencing for pathway discovery to identify signaling that is differentially affected by the exposure of direct-current electrical fields. (nature.com)
  • Persons with the most common pediatric brain malignancy, medulloblastoma, fare only slightly better than average, with a 71.9% 5-year survival, though the most common adult brain tumor, glioblastoma multiforme (GBM), incurs a mere 5.1% 5-year survival rate 2 . (nature.com)
  • When unregulated, members of this family and their receptors are known to be involved in tumor formation. (rndsystems.com)
  • We aimed to determine the signaling pathway regulating cell metabolism and the mechanism related to the regulation of human tumor-associated macrophages (TAMs) in gastric cancer (GC). (cancerindex.org)
  • Because the expression of the estrogen receptor (ER) in patients with primary breast cancer is one of the most powerful indicators of response to adjuvant hormonal therapy, the effects of endocrine-therapeutic agents strongly depend on whether tumor cell growth remains estrogen responsive ( 3 ). (iiarjournals.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)
  • 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)
  • After local injection of LP-S into the tumor, the lymphatic drainage pathway and lymph nodes can be clearly identified by NIR fluorescence imaging. (bvsalud.org)
  • In this study, glycidylated PAMAM G4 dendrimers, substituted with F, L, and/or P and targeting tumor cells, were synthesized and characterized, and their antitumor activity against glioma U-118 MG and non-small cell lung cancer A549 cells was tested comparatively with human non-tumorogenic keratinocytes (HaCaT). (bvsalud.org)
  • Like sorafenib, lapatinib is a protein kinase inhibitor shown to decrease tumor-causing breast cancer stem cells. (hmdb.ca)
  • Some of the new approaches depend on tumor biology and aim specifically to inhibit tumor growth and metastasis by targeting the tumor microenvironment or vasculature (leaving normal cells unaffected) or focusing on specific protein or signal transduction pathways. (medscape.com)
  • The HER (erbB) family of transmembrane receptor tyrosine kinases is one of the cytostatic targets in tumor cell growth and survival. (medscape.com)
  • ErbB2 belongs to the ErbB family of receptor tyrosine kinases, which has been implicated in a variety of human cancers , including cancers of the breast. (her2support.org)
  • We find that U87 mg electrotaxis is abolished under pharmacological inhibition of PI3Kγ, mTOR, AKT and ErbB2 signaling, whereas DAOY cell electrotaxis was not attenuated by these or other pathways evaluated. (nature.com)
  • Receptor tyrosine-protein kinase erbB-2 , also known as CD340 (cluster of differentiation 340), proto-oncogene Neu , Erbb2 (rodent), or ERBB2 (human), is a protein that in humans is encoded by the ERBB2 gene. (iiab.me)
  • On the other hand, c-Abl (Abl-1) is a non-receptor tyrosine kinase, which is also essential in the regulation of several antiapoptotic and proliferative signal transduction pathways. (frontiersin.org)
  • My laboratory studies signal transduction pathways that regulate growth and programmed cell death in epithelial cancer cells, with a focus on breast and ovarian cancer. (cancer.gov)
  • The amplification of the HER-2 oncogene occurs in ~25% of breast cancer patients and is associated with diminished disease-free and overall survival. (touchoncology.com)
  • In addition to plexins, various other proteins have been implicated either as receptors for semaphorins or as components of the semaphorin receptor complex ( Pasterkamp and Kolodkin, 2003 ). (rupress.org)
  • 1) We study Cbl proteins, a family of ubiquitin ligases that negatively regulate signaling by receptor tyrosine kinases. (cancer.gov)
  • We are investigating the function of Cbl proteins, a family of proteins that regulate tyrosine kinase activity. (cancer.gov)
  • Cbl proteins belong to the RING finger class of ubiquitin protein ligases (E3s) and function as E3s for activated tyrosine kinases. (cancer.gov)
  • RAS family proteins mediate extracellular signals, transduced through their receptors, with multiple signaling pathways, and consequently regulate a wide array of cellular processes [ 8 ] . (encyclopedia.pub)
  • RAS family proteins play a vital role in the modulation of cell survival, proliferation, and differentiation by signaling through a set of molecular pathways [ 10 ] . (encyclopedia.pub)
  • MSY3 (MSY4, YB-2, CSDA, dbpA, ZONAB) is a member of the cold shock domain (CSD) family of proteins also known as Y-box proteins, which are evolutionarily conserved proteins that function as transcription factors and regulators of RNA metabolism and protein synthesis. (biomedcentral.com)
  • SARS-CoV-2 has a single-stranded RNA genome encoding both structural and non-structural proteins. (news-medical.net)
  • Purpose: To determine the maximum tolerated dose (MTD), safety, pharmacokinetics, pharmacodynamics, and preliminary evidence of antitumor activity of the PI3K/mTOR inhibitor PF-04691502, administered orally once daily. (researchgate.net)
  • Methods: Escalating doses of PF-04691502 were administered to 23 patients with advanced solid tumors in sequential cohorts across the following dose levels: 2 mg, 4 mg, 8 mg, and 11 mg. 14 additional patients were enrolled in an expansion cohort at the MTD to ensure at least five matched pre- and post-treatment biopsies for biomarkers of PI3K activity. (researchgate.net)
  • Gefitinibe foi capaz de bloquear a sinalização iniciada por EGF na via de PI3K em todas as linhagens wt-PTEN e de bloquear a sinalização através de ERK1/2 e ERK5 ao menos parcialmente em todas as linhagens celulares. (usp.br)
  • 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)
  • ADAM17 is regulated by trafficking steps including control of endoplasmic reticulum (ER) exit by iRhom1/212-14 proteolytic maturation by removal of the ADAM17 prodomain in the trans-Golgi network (TGN) by furin10 and stimulation of ADAM17 surface translocation by mitogen-activated protein kinases (MAPKs)15 16 Once at the cell surface ADAM17 can be activated rapidly through conformational alterations17-19. (bioskinrevive.com)
  • However, it is unclear how the activity of plexin-B1 and its downstream effectors is regulated by its ligand Sema4D. (rupress.org)
  • Among the several options to block Notch signaling, inhibition ON123300 of -secretase by small molecules offers a promising approach and has been used extensively to study the downstream targets of the Notch signaling pathway [13,14]. (scienceexhibitions.org)
  • Among such actionable targets in BC is the fibroblast growth factor receptor (FGFR). (123dok.org)
  • 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)
  • Tyrosine kinases, which catalyze the transfer of a phosphate from ATP to a hydroxyl group of a tyrosine residue, play a plethora of roles in the regulation of diverse functions in normal cells including cell growth, motility, differentiation, and metabolism. (frontiersin.org)
  • RAS protein plays a vital role in the modulation of cell survival, proliferation, and differentiation by molecular pathway signaling. (encyclopedia.pub)
  • In the ovarian cycle, repeated patterns of specific cellular proliferation, differentiation, and transformation occur that accompany the process of follicular development and the formation and function of the corpus luteum [ 2 ] . (encyclopedia.pub)
  • Heterodimerization leads to the activation of pathways which lead to cell proliferation or differentiation. (nih.gov)
  • The results revealed significant differences in the behavior and coordination of RNA editing events, biomolecules, and multiple signaling pathways which beyond any speculations from the findings in the process of carcinogenesis. (fortunejournals.com)
  • Results Genome-wide screen identifies PACS-2 as an ADAM17 regulator To identify genes that regulate ADAM17-mediated shedding we screened a whole-genome human siRNA library (see Supplementary Information for an extensive description of the screen). (bioskinrevive.com)
  • Understanding the mechanisms that regulate signaling by these kinases should uncover new ways to inhibit cancer cell growth. (cancer.gov)
  • Additionally, reproductive hormones regulate RAS activity in the cellular physiological function of ovarian follicles during pre-ovulatory maturation and ovulation. (encyclopedia.pub)
  • Amino acid deficiencies also up-regulate the expression of p27 using some components of this pathway. (biomedcentral.com)
  • Human epithelial malignancies frequently display deregulated tyrosine kinase activity. (cancer.gov)
  • There is a total of seven signalling receptors, encoded by four FGFR genes, FGFR1-4 [15]. (123dok.org)
  • In line with our results, Western, our analysis revealed that the genes play a series of repressed genes in K562 cells together Gleevectreated were within the JAK / STAT signaling pathway grouped. (mi-rna.com)
  • The erbB family of receptor tyrosine kinases plays critical roles in human cancers, including pancreatic cancer. (aacrjournals.org)
  • As the understanding of how key molecular pathways work in cancers has increased, so have more-sophisticated therapies been introduced, often used conjunction with the traditional slash, burn and poison approaches. (anti-agingfirewalls.com)
  • However, the specific molecular pathways underlying this condition remain unclear. (ankylosingspondylitistreatmentreport.com)
  • Pathogen-associated molecular patterns released by infecting organisms not only bind immune receptors on inflammatory cells but also bind receptors on cells in the heart ( 8 ). (frontiersin.org)
  • The Fibroblast Growth Factor Receptors/Fibroblast Growth Factors (FGFRs/FGFs) axis offers interesting molecular targets to be pursued in clinical development. (123dok.org)
  • This blog entry is concerned with another "smart" approach: simultaneously targeting multiple molecular pathways in cancer cells to defeat their protective responses. (anti-agingfirewalls.com)
  • 2 The pathogenesis of lung cancer involves the accumulation of several molecular abnormalities over time. (bmj.com)
  • [ 3 ] In an attempt to improve outcomes in HNSCC, most research in the field is now focusing on the molecular biology of HNSCC in an attempt to target select pathways involved in carcinogenesis. (medscape.com)
  • With the increased understanding of molecular mechanisms and basic pathways in the pathogenesis of squamous cell cancer of the head and neck , these pathways may be modified, and rational approaches in cancer therapy at the molecular level may be created. (medscape.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. (iiab.me)
  • Furthermore, immunoglobulin-like subdomains D2 and D3 are necessary and sufficient for ligand binding, whereas the aminoterminal part of the receptor-including D1-has an auto-inhibitory function [16]. (123dok.org)
  • 1 ErbB users type homo- and heterodimeric cell-surface receptors with original extracellular domains yielding ligand-binding specificity. (bio-biz-navi.com)
  • 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)
  • Canertinib (CI-1033, PD 183805) is a pan-erbB tyrosine kinase inhibitor. (lclabs.com)
  • Canertinib is an irreversible tyrosine kinase inhibitor. (lclabs.com)
  • Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo. (lclabs.com)
  • Z-LLNle-CHO, as a derivative of a widely used proteasome inhibitor MG-132, has been reported to inhibit chymotryptic protease activity, a core function of the proteasome [17]. (scienceexhibitions.org)
  • MicroRNA-30c expression was suppressed by hypoxia-inducible factor-1α activation and related to decreased mTOR activity as well as glycolysis in human GC TAMs. (cancerindex.org)
  • The Part 1 post was concerned principally with interventions that address the mTOR pathway, a growth pathway also of great interest from the viewpoint of longevity. (anti-agingfirewalls.com)
  • Here, we show that plexin-B family members stably associate with the receptor tyrosine kinase ErbB-2. (rupress.org)
  • Discovering a specific agent, which targets multiple members of the erbB family, would be important in pancreatic cancer therapy. (aacrjournals.org)
  • DNAJA3 is a member of the DNAJ/Hsp40 protein family, which stimulates the ATPase activity of Hsp70 chaperones and plays critical roles in protein folding, degradation, and multiprotein complex assembly. (wikipedia.org)
  • The activity of EGF family members is mediated by the EGF R/ErbB receptor tyrosine kinases. (rndsystems.com)
  • The ErbB family consists of four plasma membrane-bound receptor tyrosine kinases. (iiab.me)
  • 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)
  • 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)
  • However, it does form heterodimers with other EGF receptor family members which do have kinase activity. (nih.gov)
  • Introduction Notch is a family of single-pass type I transmembrane protein receptors that, in mammals, includes four homologs, Notch1 to 4 [1]. (scienceexhibitions.org)
  • The FACE ErbB-2 (Y1248) and ErbB-2 (Y877) Kits were used to assay the levels of total and phosphorylated ErbB-2 contained within untreated or EGF treated A-431 cells. (activemotif.com)
  • To address this question, the effects of various nutritional and chemopreventive anti-cancer agents on the activity of the proximal 5'-upstream region of p27 gene were investigated by transient transfection assay. (biomedcentral.com)
  • Proteasome inhibition was determined by using a cell-based proteasome activity assay kit, by immunoblotting to detect accumulation of polyubiquitylated protein, and by immunofluorescent microscopy to detect redistribution of cellular ubiquitin. (scienceexhibitions.org)
  • Cancer Res (2006) 66 (2): 1025-1032. (aacrjournals.org)
  • The use of trastuzumab when given with chemotherapy improves response rates and progression-free and overall survival of patients with HER-2-positive metastatic breast cancer. (touchoncology.com)
  • It soon became clear that patients with HER-2-overexpressing metastatic breast cancer were at high risk of developing CNS involvement. (touchoncology.com)
  • Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. (lclabs.com)
  • While many factors are involved in the etiology of cancer, it has been clearly established that diet significantly impacts risk of this disease [ 1 , 2 , 3 ]. (mdpi.com)
  • Because of this, ErbB-2 is one of the major drug targets for breast cancer and other cancer treatments. (activemotif.com)
  • HER-2 is over-expressed in approximately 7-34% of patients with gastric cancer [20] [21] and in 30% of salivary duct carcinomas. (iiab.me)
  • However, adjuvant TAM is effective in some ER-negative breast cancer patients who express progesterone receptor (PgR), an ERG. (iiarjournals.org)
  • We have identified anti-cancer effects of Huaier, and its unique characteristics of 1) no side effects or toxicity, 2) in dose dependent manner, 3) causing specific cancer cell death with simultaneous tissue regeneration, 4) miRNA-mediated transcriptional control on the rescue of multiple signal transduction, by dependent on individual genomic potential. (fortunejournals.com)
  • Recent advancement in technology enabled to cultivate those useful species in quantity, and quality-controlled distribution in the conventional granule forms has begun since 1970's, and currently Huaier is recognized widely as the patent anti-cancer drug in China (Chinese administration license No. Z-20000109) [2, 4, 5]. (fortunejournals.com)
  • 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)
  • HER3- A key survival pathway and an emerging therapeutic target in metastatic colorectal cancer and pancreatic ductal adenocarcinoma. (nih.gov)
  • This Part 2 post is concerned with anti-cancer drug and other interventions that simultaneously address multiple growth pathways. (anti-agingfirewalls.com)
  • Results We found that blocking -secretase activity by DAPT and L-685,458 had no effect on the survival and proliferation of a panel of six breast cancer cell lines while Z-LLNle-CHO could cause cell death even at concentrations that inhibited -secretase activity less efficiently. (scienceexhibitions.org)
  • An important development in cancer research over the past 2 decades has been the recognition that genetic changes drive the pathogenesis of tumors of both adulthood and childhood. (medscape.com)
  • 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)
  • Toll-like receptors are transmembrane glycoproteins, which recognize many PAMPs with extracellular domains and aggravate the exaggerated inflammatory response to bacterial infection through activating nuclear factor (NF)-κB ( 12 ). (frontiersin.org)
  • Dimerisation results in the autophosphorylation of tyrosine residues within the cytoplasmic domain of the receptors and initiates a variety of signaling pathways. (iiab.me)
  • In neuromuscular junctions, only the short isoform clusters acetylcholine receptors for efficient synaptic transmission. (wikipedia.org)
  • some are promiscuous, such as FGF1, and bind to multiple receptors, while others, such as FGF7, tether only one receptor isoform [11]. (123dok.org)
  • This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. (nih.gov)
  • In FACE, cells are cultured in 96-well plates and stimulated to induce the pathway of interest. (activemotif.com)
  • Alternatively interference with the subcellular localization of ADAM17 could provide a novel approach to selectively controlling its activity. (bioskinrevive.com)
  • ERBB is abbreviated from erythroblastic oncogene B, a gene isolated from avian genome. (iiab.me)
  • What pathways are this gene/protein implicaed in? (cancerindex.org)
  • 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)
  • A new study reports the activity of one such protein, the non-structural protein 14 (NSP14), which activates the inflammatory mediator NF-κB to trigger intense inflammation. (news-medical.net)
  • A dominant-negative form of ErbB-2 blocks Sema4D-induced RhoA activation as well as axonal growth cone collapse in primary hippocampal neurons. (rupress.org)