Article
Small-molecule inhibition and activation-loop trans-phosphorylation of the IGF1 receptor.
The EMBO journal - 23 Jul 2008
Wu Jinhua, Li Wanqing, Craddock Barbara P, Foreman Kenneth W, Mulvihill Mark J, Ji Qun-sheng, Miller W Todd, Hubbard Stevan R
Abstract excerpt
The insulin-like growth factor-1 receptor (IGF1R) is a receptor tyrosine kinase (RTK) that has a critical role in mitogenic signalling during embryogenesis and an antiapoptotic role in the survival and progression of many human tumours. Here, we present the crystal structure of the tyrosine kinase domain of IGF1R (IGF1RK), in its unphosphorylated state, in complex with a novel compound,...
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