RET kinases are involved in the onset and development of various types of cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Starting from our previously identified dual cKIT/PDGFRβ inhibitor, we report the development of a novel multi-cKIT/wtRET/V804MRET inhibitor.
Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead
Marzaro, G.
2017-01-01
Abstract
RET kinases are involved in the onset and development of various types of cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Starting from our previously identified dual cKIT/PDGFRβ inhibitor, we report the development of a novel multi-cKIT/wtRET/V804MRET inhibitor.
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