Title : Inhibition of Lapatinib-Induced Kinome Reprogramming in ERBB2-Positive Breast Cancer by Targeting BET Family Bromodomains.

Pub. Date : 2015 Apr 21

PMID : 25865888






2 Functional Relationships(s)
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1 Adaptive responses leading to lapatinib resistance involve reprogramming of the kinome through reactivation of ERBB2/ERBB3 signaling and transcriptional upregulation and activation of multiple tyrosine kinases. Lapatinib erb-b2 receptor tyrosine kinase 3 Homo sapiens
2 Genetic and chemical inhibition of BET bromodomain chromatin readers suppresses transcription of many lapatinib-induced kinases involved in resistance, including ERBB3, IGF1R, DDR1, MET, and FGFRs, preventing downstream SRC/FAK signaling and AKT reactivation. Lapatinib erb-b2 receptor tyrosine kinase 3 Homo sapiens