Relation Results

Summary

Name ErbB receptor family
Primary ID SIGNOR-PF36
Type protein family
Formed by EGFR, ERBB2, ERBB3, ERBB4
Relations 15
Pathways ErbB receptors in cancer, Non-small-cell lung cancer (NSCLC), Pancreatic ductal adenocarcinoma (PDA)

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Type: Score: Layout: SPV 
0.9060.80.9040.6120.20.80.7270.6580.7730.80.20.891NeuregulinErbB receptor familysapitinibNRG1ERBB2SHC3afatinibLRIG1EGFRPI3KdacomitinibGRB2EREG

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Relations
Regulator
Mechanism
target
score ℹ
+ Neuregulinup-regulates activity img/direct-activation.png binding ErbB receptor family 0.906
Identifier Residue Sequence Organism Cell Line
SIGNOR-256161 Homo sapiens
pmid sentence
The neuregulin family consists of four genes, NRG1-4 which can each encode products containing a domain related to the epidermal growth factor family of ligands. they may be released by regulated proteolysis to act as soluble proteins which can interact and activate members of the EGF receptor family of receptor tyrosine kinases
Publications: 1 Organism: Homo Sapiens
Pathways:ErbB receptors in cancer
+ sapitinibdown-regulates img/direct_inhibition.png chemical inhibition ErbB receptor family 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-269874 Homo sapiens Lung Cancer Cell
pmid sentence
In vivo, azd8931 inhibited xenograft growth in a range of models while significantly affecting egfr, erbb2, and erbb3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation.
Publications: 1 Organism: Homo Sapiens
+ NRG1up-regulates img/direct-activation.png binding ErbB receptor family 0.904
Identifier Residue Sequence Organism Cell Line
SIGNOR-269870 Homo sapiens
pmid sentence
The neuregulins (also called heregulins and neu differentiation factors) nrg-1 and nrg-2 bind erbb-3 and erbb-4;and nrg-3 and nrg-4 bind erbb-4.
Publications: 1 Organism: Homo Sapiens
+ ERBB2up-regulates activity img/direct-activation.png phosphorylation ErbB receptor family 0.612
Identifier Residue Sequence Organism Cell Line
SIGNOR-269875 in vitro
pmid sentence
 Y1023 and Y1248, Y1139 and Y1222 also serve as autophosphorylation sites of HER2.
Publications: 1 Organism: In Vitro
+ ErbB receptor familyup-regulates img/direct-activation.png relocalization SHC3 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-269962 Homo sapiens
pmid sentence
Like erbb1, erbb4 recruits grb2, shc and stat5.
Publications: 1 Organism: Homo Sapiens
+ afatinibdown-regulates activity img/direct_inhibition.png chemical inhibition ErbB receptor family 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259441 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Identifier Residue Sequence Organism Cell Line
SIGNOR-259442 Homo sapiens Breast Cancer Cell
pmid sentence
Afatinib is an oral, erbb family blocker, which covalently binds and irreversibly blocks all kinase-competent erbb family members.
Identifier Residue Sequence Organism Cell Line
SIGNOR-259443 Homo sapiens Non-small Cell Lung Cancer Cell
pmid sentence
This manuscript comprehensively reviews the preclinical data on afatinib, an irreversible inhibitor of the tyrosine kinase activity of members of the epidermal growth factor receptor family (ErbB) including EGFR, HER2 and ErbB4. Afatinib covalently binds to cysteine 797 of the EGFR and the corresponding cysteines 805 and 803 in HER2 and ErbB4, respectively.
Identifier Residue Sequence Organism Cell Line
SIGNOR-259440 Homo sapiens Lung Cancer Cell
pmid sentence
Afatinib, an irreversible erbb-family blocker, has shown preclinical activity when tested in egfr mutant models with mutations that confer resistance to egfr tyrosine-kinase inhibitors.
Publications: 4 Organism: In Vitro, Homo Sapiens
+ LRIG1down-regulates img/direct_inhibition.png ubiquitination ErbB receptor family 0.727
Identifier Residue Sequence Organism Cell Line
SIGNOR-269872 Homo sapiens
pmid sentence
We report upregulation of lrig1 transcript and protein upon egf stimulation, and physical association of the encoded protein with the four egfr orthologs of mammals. Upregulation of lrig1 is followed by enhanced ubiquitylation and degradation of egfr. The underlying mechanism involves recruitment of c-cbl, an e3 ubiquitin ligase that simultaneously ubiquitylates egfr and lrig1 and sorts them for degradation.
Publications: 1 Organism: Homo Sapiens
+ EGFRup-regulates img/direct-activation.png binding ErbB receptor family 0.658
Identifier Residue Sequence Organism Cell Line
SIGNOR-269876 Homo sapiens
pmid sentence
These results demonstrate that egfr-erbb2 oligomers are potent activators of mapk and akt, and this signaling does not require egfr kinase activity
Publications: 1 Organism: Homo Sapiens
Pathways:Non-small-cell lung cancer (NSCLC), Pancreatic ductal adenocarcinoma (PDA)
+ ErbB receptor familyup-regulates activity img/direct-activation.png binding PI3K 0.773
Identifier Residue Sequence Organism Cell Line
SIGNOR-256168 Homo sapiens
pmid sentence
Another phospholipid modifying signaling pathway activated by RTKs is the PI3K pathway. This heterodimeric enzyme comprises two subunits, the p85 regulatory subunit harboring two SH2 domains, and the p110 catalytic subunit. PI3K activation may be achieved by binding of its p85 regulatory subunit to an activated receptor. Alternatively, RTK signaling may activate the small G protein Ras, which in turn recruits PI3K to the plasma membrane and induces a stimulatory conformational change in the lipid kinase
Publications: 1 Organism: Homo Sapiens
Pathways:ErbB receptors in cancer, Non-small-cell lung cancer (NSCLC), Pancreatic ductal adenocarcinoma (PDA), RTKs in cancer
+ dacomitinibdown-regulates img/direct_inhibition.png chemical inhibition ErbB receptor family 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-269871 Homo sapiens
pmid sentence
The goal of this study was to compare dacomitinib (pf-00299804), a next generation small molecule tyrosine kinase inhibitor that irreversibly blocks multiple her family receptors (her-1 (egfr), her-2 and her-4 tyrosine kinases), to cetuximab, the current fda approved anti-egfr medication for hnscc and erlotinib, an egfr specific small molecule tyrosine kinase inhibitor.
Publications: 1 Organism: Homo Sapiens
+ ErbB receptor familyup-regulates activity img/direct-activation.png binding GRB2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-256162 Homo sapiens
pmid sentence
All erbb ligands and receptors couple to activation of the ras-mapk pathway, either directly through sh2 domain-mediated recruitment of grb-2 or indirectly through ptb domain-mediated binding of the shc adaptor
Publications: 1 Organism: Homo Sapiens
Pathways:ErbB receptors in cancer, Non-small-cell lung cancer (NSCLC), RTKs in cancer
+ EREGup-regulates img/direct-activation.png binding ErbB receptor family 0.891
Identifier Residue Sequence Organism Cell Line
SIGNOR-269873 Homo sapiens
pmid sentence
For example, betacellulin binds to and activates both erbb1 and erbb4, whereas epiregulin binds to erbb1, erbb3 and erbb4.
Publications: 1 Organism: Homo Sapiens
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