Activating Compound | Comment | Organism | Structure |
---|---|---|---|
AG1478 | increases HER2 phosphorylation in the presence of heregulin. Phosphorylation of HER2 is greater by heregulin beta and heregulin beta-1 in the presence of AG 1478 | Homo sapiens | |
betacellulin | activates HER3 and HER4 via HER2 | Homo sapiens | |
betacellulin | activates HER3 via HER2 | Homo sapiens | |
Epidermal growth factor | induces phosphorylation | Homo sapiens | |
heregulin | activates HER3 and HER4 via HER2 | Homo sapiens | |
heregulin | activates HER3 via HER2 | Homo sapiens | |
Iressa | acute treatment with 0.001 mM iressa induces a significant increase in HER2 phosphorylation | Homo sapiens |
Application | Comment | Organism |
---|---|---|
medicine | role of drug-induced autocrine events leading to the activation of alternative HER receptors in maintaining HER2 phosphorylation and in mediating resistance to EGFR tyrosine kinase inhibitors in breast cancer cells, and hence specify treatment opportunities to overcome resistance in patients | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
AG1478 | specific tyrosine kinase inhibitor of EGFR, does not inhibit epidermal growth factor-induced or heregulin beta-induced HER2 phosphorylation. Cleavage of HER4 and dimerization of HER4/HER2 occur together with reactivation of HER3 via HER2/HER3, leading to persistent HER2 phosphorylation in the now resistant, surviving cells; specific tyrosine kinase inhibitor of EGFR. It decreases HER3 phosphorylation through the inhibition of EGFR/HER3 dimerization. Cleavage of HER4 and dimerization of HER4/HER2 occur together with reactivation of HER3 via HER2/HER3, leading to persistent HER2 phosphorylation in the now resistant, surviving cells; specific tyrosine kinase inhibitor of EGFR, whifh decreases EGFR phosphorylation through the inhibition of EGFR/HER3 dimerization | Homo sapiens | |
herceptin | combined therapy with herceptin and iressa exerts a greater suppression in EGFR activation; combined therapy with herceptin and iressa exerts a greater suppression in HER2 activation | Homo sapiens | |
Iressa | gefitinib, specific tyrosine kinase inhibitor of EGFR. Decreases HER3 phosphorylation through the inhibition of EGFR/HER3 dimerization. Cleavage of HER4 and dimerization of HER4/HER2 occur together with reactivation of HER3 via HER2/HER3, leading to persistent HER2 phosphorylation in the now resistant, surviving cells; gefitinib, specific tyrosine kinase inhibitor of EGFR, does not abolish basal HER2 phosphorylation, but decreases EGFR and HER3 phosphorylation through the inhibition of EGFR/HER3 dimerization. Combined therapy with herceptin and iressa exerts a greater suppression in EGFR activation; gefitinib, specific tyrosine kinase inhibitor of EGFR, does not abolish basal HER2 phosphorylation. Cleavage of HER4 and dimerization of HER4/HER2 occur together with reactivation of HER3 via HER2/HER3, leading to persistent HER2 phosphorylation in the now resistant, surviving cells. Combined therapy with herceptin and iressa exerts a greater suppression in HER2 activation | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P00533 | - |
- |
Homo sapiens | P04626 | - |
- |
Homo sapiens | P21860 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
A-431 cell | overexpresses EGFR | Homo sapiens | - |
MCF-7 cell | - |
Homo sapiens | - |
MDA-MB-453 cell | HER2 over-expressing | Homo sapiens | - |
SK-BR-3 cell | HER2 over-expressing | Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
Egfr | - |
Homo sapiens |
HER2 | - |
Homo sapiens |
HER3 | - |
Homo sapiens |