Article
A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor.
The Journal of biological chemistry - 27 Sept 2013
Anastassiadis Theonie, Duong-Ly Krisna C, Deacon Sean W, Lafontant Alec, Ma Haiching, Devarajan Karthik, Dunbrack Roland L, Wu Jinhua, Peterson Jeffrey R
Abstract excerpt
Dual inhibitors of the closely related receptor tyrosine kinases insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) are promising therapeutic agents in cancer. Here, we report an unusually selective class of dual inhibitors of IGF-1R and IR identified in a parallel screen of known kinase inhibitors against a panel of 300 human protein kinases. Biochemical and structural studies indicate that...
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