Protein tyrosine kinase kinase activity receptor erbb 2. Medical search. Frequent questions

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)
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)
The molecular mechanism underlying its development is complex, but its carcinogenesis has been proposed to occur with cell proliferation and resistance to apoptosis, driven by the signaling activity of abundant EGFR and receptor tyrosine-protein kinase erbB-2. (bvsalud.org)
The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4). (wikipedia.org)
In many cancer types, mutations affecting EGFR expression or activity could result in cancer. (wikipedia.org)
Deficient signaling of the EGFR and other receptor tyrosine kinases in humans is associated with diseases such as Alzheimer's, while over-expression is associated with the development of a wide variety of tumors. (wikipedia.org)
Interruption of EGFR signalling, either by blocking EGFR binding sites on the extracellular domain of the receptor or by inhibiting intracellular tyrosine kinase activity, can prevent the growth of EGFR-expressing tumours and improve the patient's condition[citation needed]. (wikipedia.org)
Epidermal growth factor receptor (EGFR) is a transmembrane protein that is activated by binding of its specific ligands, including epidermal growth factor and transforming growth factor alpha (TGF-α). (wikipedia.org)
In addition to forming homodimers after ligand binding, EGFR may pair with another member of the ErbB receptor family, such as ErbB2/Her2/neu, to create an activated heterodimer. (wikipedia.org)
EGFR dimerization stimulates its intrinsic intracellular protein-tyrosine kinase activity. (wikipedia.org)
As a result, autophosphorylation of several tyrosine (Y) residues in the C-terminal domain of EGFR occurs. (wikipedia.org)
Additionally, the kinase domain of the EGFR can cross-phosphorylate the tyrosine residues of other receptors with which it is aggregated and thereby activate itself. (wikipedia.org)
Neratinib is an investigational, orally administered, irreversible inhibitor of the ErbB1 (EGFR), ErbB2 (HER2) and ErbB4 (HER4) kinases. (her2support.org)
The ErbB-2 proto-oncogene, also called Neu, EGFR-2 or HER-2, is a member of the transmembrane receptor tyrosine kinase family, which also includes EGF receptor and EGFR-3 (HER-3 or ErbB-3). (activemotif.com)
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)
In our prior research of epidermal development aspect receptor (EGFR) dimerization dynamics at a single-molecule level, we demonstrated that receptor activation by ligand binding is certainly spatially asymmetric on cells overexpressing EGFR (ref. 13). (president2010.info)
This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. (nih.gov)
Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). (adooq.com)
Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR. (adooq.com)
CO-1686 is a novel, oral, targeted covalent (irreversible) inhibitor of the cancer-causing mutant forms of epidermal growth factor receptor (EGFR) currently being studied for the treatment of non-small cell lung cancer (NSCLC). (adooq.com)
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. (adooq.com)
Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). (adooq.com)
BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. (adooq.com)
Defective signaling of EGFR and other receptor tyrosine kinases in humans has been linked to diseases such as Alzheimer's disease, while overexpression has been linked to the development of various tumors. (promab.com)
Disruption of EGFR signaling by blocking the EGFR-binding site on the extracellular domain of the receptor or inhibiting intracellular tyrosine kinase activity prevents the growth of EGFR-expressing tumors and improves patient outcomes. (promab.com)
The anti-EGFR CAR in this product is approximately 56 kD and consists of anti-EGFR scFv (single-chain variable fragment) linked to a second-generation CAR (chimeric antigen receptor) containing the CD8 hinge and transmembrane domain and 4-1BB and CD3ζ signaling domains. (promab.com)
HER2 is a member of the human epidermal growth factor receptor (HER/EGFR/ERBB) family. (iiab.me)
ErbB-2 was named for its similarity to ErbB (avian erythroblastosis oncogene B), the oncogene later found to code for EGFR. (iiab.me)
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)
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)
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)
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)
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)
The epidermal growth factor receptor (EGFR) is among the most well-studied signaling pathways in cancer progression. (bio-biz-navi.com)
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)
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)
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)
Improved EGFR proteins and transcript amounts correlate with poor prognosis in a variety of epithelial cancers, such as for example colorectal malignancy (CRC), 4 non-small cell lung malignancy (NSCLC), 5 endometrial malignancy, 6 and squamous-cell carcinoma of the top and throat (SCCHN). (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)
Several members of the Epidermal Growth Factor Receptor (EGFR) family, have been identified in the nucleus and nucleolus of many cancer cells, but their function in these compartments remains unexplored. (biomedcentral.com)
We focused our research on the nucleolar function that a specific member of EGFR family, the ErbB3 receptor, plays in glioblastoma, a tumor without effective therapies. (biomedcentral.com)
Since the EGFR signalling promotes proliferation in tumor the EGFR receptors often represent a marker of resistance with poor prognosis. (biomedcentral.com)
To date, cetuximab is the only anti‑epidermal growth factor receptor (EGFR) monoclonal antibody (mAb) approved for the targeted therapy of head and neck squamous cell carcinoma (HNSCC). (spandidos-publications.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)
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)

HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands. (wikipedia.org)
Epidermal growth factor and its receptor was discovered by Stanley Cohen of Vanderbilt University. (wikipedia.org)
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)
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 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)
capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy including an anthracycline, a taxane, and trastuzumab . (hdkino.org)
It is also frequently called HER2 (from human epidermal growth factor receptor 2 ) or HER2/neu . (iiab.me)
HER2 is so named because it has a similar structure to human epidermal growth factor receptor, or HER1. (iiab.me)
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)
Chapman CH, Saba NF and Yom SS: Targeting epidermal growth factor receptor for head and neck squamous cell carcinoma: Still lost in translation? (spandidos-publications.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)
Endogenous RPTPkappa associated with EGF receptor and HER2, resulting in suppression of basal and ErbB ligand-induced proliferation and receptor phosphorylation. (nih.gov)
In MCF10A/HER2 cells, TGF-beta enhanced cell motility, FAK phosphorylation, F-actin assembly, and focal adhesion formation and inhibited RhoA activity. (nih.gov)
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)
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)
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)
HER2 BC cells using a 3+ immunohistochemistry (IHC) rating display high basal degrees of receptor kinase activity and phosphorylation, and these induce CAY10471 Racemate constitutive activation from the mitogen-activated proteins phosphatidylinositol and kinase 3-kinase/Akt pathways8. (president2010.info)
It therefore can bind this ligand but not convey the signal into the cell through protein phosphorylation. (nih.gov)
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)
Downstream signaling from these receptors proceeds TSPAN10 via tyrosine phosphorylation. (bio-biz-navi.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)
Recently, highly targeted small-molecule agents, such as tyrosine kinase inhibitors (TKI), open a new avenue for RA therapy with improved clinical responses ( Koenders and Van DenBerg, 2015 ). (frontiersin.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)
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)
Blaszczak W, Barczak W, Wegner A, Golusinski W and Suchorska WM: Clinical value of monoclonal antibodies and tyrosine kinase inhibitors in the treatment of head and neck squamous cell carcinoma. (spandidos-publications.com)
Sacco AG and Worden FP: Molecularly targeted therapy for the treatment of head and neck cancer: A review of the ErbB family inhibitors. (spandidos-publications.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)

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)
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)
This membrane deformation will not need receptor signalling actions, but outcomes from the high degrees of HER2 in the cell surface area. (president2010.info)
HER2 is certainly a CAY10471 Racemate known person in the ErbB/HER receptor tyrosine kinase family members1,2,3. (president2010.info)
These features of HER2 overexpression had been acquired from several ensemble experiments, where receptor actions are averaged more than an extremely large numbers of cells typically. (president2010.info)
A lot of area points of specific HER2s had been obtained by monitoring one receptors (for 100?s in a 10.72?Hz acquisition price) labelled with anti-HER2 Fab:QD (H2Fab:QD) conjugates using total inner reflection fluorescence microscopy (TIRFM)13. (president2010.info)
We initial likened the receptor distribution patterns inside the same cell type where HER2 appearance levels had been artificially changed. (president2010.info)
BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity. (adooq.com)
letrozole for the treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated. (hdkino.org)
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)
The HER2 receptor does not bind to any known ligands, however, its dimerization arm is innately positioned in an open conformation. (plos.org)

Like sorafenib, lapatinib is a protein kinase inhibitor shown to decrease tumor-causing breast cancer stem cells. (hmdb.ca)
When unregulated, members of this family and their receptors are known to be involved in tumor formation. (rndsystems.com)
Taking advantage of the diverse γδ TCR repertoire or other ligand-receptor interactions, γδ T cells can recognize a broad spectrum of tumor-associated antigens (TAAs) in a major histocompatibility complex (MHC)-independent manner, thereby activating downstream pleiotropic effects. (explorationpub.com)
Tumor-infiltrated macrophages were isolated from human GC tissues using magnetic beads, gene transcription was determined by real-time PCR, protein expression was monitored using western blots, metabolites were determined using HPLC, and transcriptional regulation was analyzed by the luciferase-based reporter gene system. (cancerindex.org)
Inhibitory Fc receptors modulate in vivo cytotoxicity t t towards tumor targets. (mirnamimics.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)
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)
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)
Tumor suppressors, oncogenes and alternatively deregulated upstream signalling pathways can directly influence the RNA polymerase I activity inducing hyper activation of rRNA transcription in cancer cells. (biomedcentral.com)
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)
[ 1 ] His prediction was subsequently supported by the cloning of the retinoblastoma tumor suppressor gene ( RB1 ) and by functional studies of the retinoblastoma protein, Rb. (medscape.com)
Like Rb protein, many of the proteins encoded by tumor suppressor genes act at specific points in the cell cycle. (medscape.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)
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)
The overexpression of the erbB-2 proto-oncogene is associated with an aggressive human adenocarcinomas, mainly breast and ovarian tumours. (australbiologicals.com)
Gene amplification and overexpression of the proteins in breast malignancies (BCs) anticipate poor disease final result due to raised metastatic potentials4,5,6,7. (president2010.info)
Amplification of this gene and/or overexpression of its protein have been reported in numerous cancers, including prostate, bladder, and breast tumors. (nih.gov)
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)

These downstream signaling proteins initiate several signal transduction cascades, principally the MAPK, Akt and JNK pathways, leading to DNA synthesis and cell proliferation. (wikipedia.org)
Important biological events associated with plasma membranes, such as signal transduction, cell adhesion, and protein trafficking, are mediated through the membrane microdomains. (mdpi.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)
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)

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)
AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling. (adooq.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)
However, this therapy has left an eloquent number of patients with recurrence and local or/and distance failures, which are associated with Erb‑B2 receptor tyrosine kinase 2 (ERBB2) signaling. (spandidos-publications.com)

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)
Free shipping on inhibitor and protein orders over $500. (adooq.com)
Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. (adooq.com)
p27(Kip1) is a cyclin-dependent kinase inhibitor. (biomedcentral.com)
The cyclin-dependent kinase (CDK) inhibitor p27(Kip1) is a key cell-cycle regulator of G1-to-S phase transition [ 1 ]. (biomedcentral.com)
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)
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)
The p16INK4A protein is a cell-cycle inhibitor that acts by inhibiting activated cyclin D:CDK4/6 complexes, which play a crucial role in the control of the cell cycle by phosphorylating Rb protein. (medscape.com)

Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. (biossusa.com)
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 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 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)
Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. (biossusa.com)
Dimerisation results in the autophosphorylation of tyrosine residues within the cytoplasmic domain of the receptors and initiates a variety of signaling pathways. (iiab.me)

These results highlight the potential role for the nucleolar ErbB3 receptor, as a new target in glioblastoma. (biomedcentral.com)

Drug-induced ubiquitination and degradation erbB receptor tyrosine kinases. (mirnamimics.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)

Such proteins modulate phenotypes such as cell migration, adhesion, and proliferation. (wikipedia.org)
erbB 2 antisense oligonucleotides inhibit proliferation of breast cancer cells with erbB oncogene amplification rkungsfaktorsteuerung second Br J Cancer. (mirnamimics.com)
60 identical and the kinase domains are a lot more than 85 identical.three Catalytically active Akt regulates the function of numerous substrates involved in cell survival, development, proliferation, metabolism and protein synthesis (reviewed in Manning, Cantley4). (bet-bromodomain.com)
Nucleolar activity is also influenced by the interaction between pathways activated from extracellular signals in order to coordinate ribosome synthesis and cell proliferation [ 6 ]. (biomedcentral.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)

Generally, these receptors explain their function on the cell membrane where, after the binding with growth factors or neuregulin undergo to homo or hetero oligomerization with the activation of the intrinsic tyrosine kinase activity and the subsequent recruitment of proteins involved in the cytoplasmic signalling pathways. (biomedcentral.com)

Familial AD (FAD) cases are caused by autosomal dominant mutations in the genes for amyloid precursor protein (APP) and the presenilins (PS1 and PS2) ( Sisodia and St George-Hyslop, 2002 ). (jneurosci.org)
Scope includes mutations and abnormal protein expression. (cancerindex.org)

In this context, during any sort of stress condition the alternative reading frame protein p14ARF subtracts MDM2, an E3 ubiquitin ligase, from the interaction with p53 in manner to free and stabilise p53 level in the nucleolus of the cell where it inhibits RNA polymerase I activity [ 3 ]. (biomedcentral.com)
MDM2 binds to and inhibits TP53 activity. (medscape.com)

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)

Understanding the mechanisms that regulate signaling by these kinases should uncover new ways to inhibit cancer cell growth. (cancer.gov)
Taken together, our present study identified umbelliferone and scopoletin as two major anti-rheumatic components from SL that may bind and inhibit tyrosine kinases and subsequently inactivate NF-κB in RA-FLSs. (frontiersin.org)
Lastly, knockdown studies revealed that the depletion of endogenous Akt1 and Akt3, but not Akt2, inhibit clonogenic activity and repair of ionizing radiation (IR)induced DNA DSBs, top to radiosensitization. (bet-bromodomain.com)

Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. (lclabs.com)
This apparent increase in p27 protein expression might have been due to either increased synthesis or decreased degradation, or a combination of both [ 1 ]. (biomedcentral.com)

The erbB family of receptor tyrosine kinases plays critical roles in human cancers, including pancreatic cancer. (aacrjournals.org)
Discovering a specific agent, which targets multiple members of the erbB family, would be important in pancreatic cancer therapy. (aacrjournals.org)
Here, we show that plexin-B family members stably associate with the receptor tyrosine kinase ErbB-2. (rupress.org)
The activity of EGF family members is mediated by the EGF R/ErbB receptor tyrosine kinases. (rndsystems.com)
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)
C-erbB-2 oncoprotein is a 185 kDa type I membrane tyrosine kinase receptor and belongs to the EGF receptor family. (australbiologicals.com)
However, it does form heterodimers with other EGF receptor family members which do have kinase activity. (nih.gov)
The ErbB family consists of four plasma membrane-bound receptor tyrosine kinases. (iiab.me)
All family members share an EGF-like domain that interacts with the ErbB family of tyrosine kinase receptors. (bio-techne.com)
Brand TM, Iida M, Luthar N, Wleklinski MJ, Starr MM, Wheeler DL (2013) Mapping C-Terminal Transactivation Domains of the Nuclear HER Family Receptor Tyrosine Kinase HER3. (plos.org)
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)
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)

1, 2 Most studies of MUC1 expression in breast carcinomas have shown that increased membrane MUC1 mucin expression on the apical cell surface is associated with a better prognosis (reviewed in Rahn and colleagues 2 ), whereas circumferential staining in tumour cell cytoplasm is associated with a worse prognosis. (bmj.com)
No important variations inside the K Occurred physique fat, blood Figure 4 Inhibition of ACAT activity of t Within the membrane fraction of mouse macrophages and mouse liver microsomes of beauveriolides I and III. (mirnamimics.com)
ACAT activity T was in an assay mixture, which tested two.5 mg ml BSA in buffer A and 20 M Ls Ure with beauveriolide I or III, and the microsomal fraction or the membrane fraction. (mirnamimics.com)
This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. (nih.gov)
This form acts to modulate the activity of the membrane-bound form. (nih.gov)

However, it is unclear how the activity of plexin-B1 and its downstream effectors is regulated by its ligand Sema4D. (rupress.org)
This autophosphorylation elicits downstream activation and signaling by several other proteins that associate with the phosphorylated tyrosines through their own phosphotyrosine-binding SH2 domains. (wikipedia.org)
The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. (biossusa.com)
Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. (biossusa.com)
As an indicator of downstream apoptotic events in response to bortezomib treatment, the protein expression of BIM splice variant was increased upon bortezomib treatment. (mi-rna.com)

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)

The protein encoded by this gene is a member of the Tyro3-Axl-Mer (TAM) receptor tyrosine kinase subfamily. (cancerindex.org)

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)
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)
[ 2 ] Targeted disruption of TP53 in the mouse leads to the development of various tumors (see image below). (medscape.com)

What pathways are this gene/protein implicaed in? (cancerindex.org)
This Part 2 post is concerned with anti-cancer drug and other interventions that simultaneously address multiple growth pathways. (anti-agingfirewalls.com)

Cbl proteins belong to the RING finger class of ubiquitin protein ligases (E3s) and function as E3s for activated tyrosine kinases. (cancer.gov)
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)

acetylcholine receptor inducing activity, ARIA), type II (glial growth factor, GGF) and type III (sensory and motor neuron-derived factor, SMDF) isoforms. (bio-techne.com)

Because of this, ErbB-2 is one of the major drug targets for breast cancer and other cancer treatments. (activemotif.com)
NH 2-terminally truncated HER-2/neu SA: Vergie no partnership with extracellular Ren Ren Cathedral and prognostic components for breast cancer. (mirnamimics.com)
Preliminary studies using either N -methyl- N -nitrosourea (MNU)-induced rat breast cancer model or human breast cancer cell lines in vitro had suggested, but not proved, that nutritional and chemopreventive anti-cancer agents increase p27 protein expression. (biomedcentral.com)
In recent years the protein has become an important biomarker and target of therapy for approximately 30% of breast cancer patients. (iiab.me)

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)

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)

Akt isoforms possess a Nterminal PH (pleckstrin homology) domain in addition to a kinase domain, which are separated by a 39aminoacid hinge area.two The PH domains are approx. (bet-bromodomain.com)

Substitution of a valine for a glutamic acid in the transmembrane domain can result in the constitutive dimerisation of this protein in the absence of a ligand. (iiab.me)

For example, the TP53 gene, located on chromosome 17, encodes a 53-kd nuclear protein that functions as a cell cycle checkpoint. (medscape.com)
The CDK4-cyclinD complex normally phosphorylates the retinoblastoma protein (Rb protein), leading to release of the E2F transcription factor and cell cycle progression. (medscape.com)
The p19ARF protein, which is encoded by the same locus as p16, also leads to cell cycle arrest by inhibiting the ability of MDM2 to inactivate TP53. (medscape.com)

Human epithelial malignancies frequently display deregulated tyrosine kinase activity. (cancer.gov)
AXL, a tyrosine kinase receptor, is commonly overexpressed in several solid tumours and numerous hematopoietic malignancies including acute myeloid leukaemia, acute lymphocytic leukaemia, chronic myeloid leukaemia, chronic lymphocytic leukaemia and multiple myeloma. (cancerindex.org)

Dose-dependent-Dependent manner with IC50 values of six.0 and 5.5 m, as well as the activity of t Mouse ACAT liver microsomes in the dose-Dependent manner Vargatef ic50 with IC50 values of one.five M for two compounds. (mirnamimics.com)
Also, inhibited the ACAT activity t in microsomes of human Caco 2 cells Hnlichen IC50 values. (mirnamimics.com)

Network pharmacology analysis and molecular docking analysis jointly revealed that umbelliferone and scopoletin act on multiple targets, mostly tyrosine kinases, in combating RA. (frontiersin.org)

Activation of the receptor is important for the innate immune response in human skin. (wikipedia.org)

Canertinib alkylates a cysteine residue specific to ErbB receptors. (lclabs.com)

Following stimulation, the cells are fixed rapidly, which preserves activation-specific protein modifications. (activemotif.com)

Anatomy18

Organisms6

Diseases1

Chemicals and Drugs174

Analytical, Diagnostic and Therapeutic Techniques and Equipment13

Phenomena and Processes39

Disciplines and Occupations1

Information Science3

EGFR49

Epidermal10

Phosphorylation15

Inhibitors10

Her213

Tumor14

Overexpression7

Signal Transduction4

ErbB24

Inhibitor10

Ligands3

Residues3

ErbB31

Ubiquitination and degradation1

Apoptosis5

Proliferation5

Intrinsic1

Mutations2

Inhibits2

Phosphoinositide1

Inhibit3

Degradation2

Family13

Membrane5

Downstream5

Antibodies1

Subfamily1

Tumors3

Pathways2

Ubiquitin2

Acetylcholine receptor1

Breast cancer4

Potent1

Ligand-induced1

Isoforms1

Constitutive1

Cell cycle3

Malignancies2

IC502

Targets1

Innate immune r1

Canertinib1

Specific protein1