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Literature summary for 2.7.10.1 extracted from

  • Kong, A.; Calleja, V.; Leboucher, P.; Harris, A.; Parker, P.J.; Larijani, B.
    HER2 oncogenic function escapes EGFR tyrosine kinase inhibitors via activation of alternative HER receptors in breast cancer cells (2008), PLoS ONE, 3, e2881.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.10.1

Activating Compound

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

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

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

Organism UniProt Comment Textmining
Homo sapiens P00533
-
-
Homo sapiens P04626
-
-
Homo sapiens P21860
-
-

Source Tissue

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

Synonyms Comment Organism
Egfr
-
 Homo sapiens
HER2
-
 Homo sapiens
HER3
-
 Homo sapiens