Article
Identification of a Non-Gatekeeper Hot Spot for Drug-Resistant Mutations in mTOR Kinase.
Cell reports - 21 Apr 2015
Wu Tzung-Ju, Wang Xiaowen, Zhang Yanjie, Meng Linghua, Kerrigan John E, Burley Stephen K, Zheng X F Steven
Abstract excerpt
Protein kinases are therapeutic targets for human cancer. However, "gatekeeper" mutations in tyrosine kinases cause acquired clinical resistance, limiting long-term treatment benefits. mTOR is a key cancer driver and drug target. Numerous small-molecule mTOR kinase inhibitors have been developed, with some already in human clinical trials. Given our clinical experience with targeted therapeutics, acquired drug...
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