Article
A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations.
International journal of molecular sciences - 23 Aug 2017
Liu Hong-Li, Zhong Hai-Yang, Song Tian-Qing, Li Jia-Zhong
Abstract excerpt
Hydroxyflutamide (HF), an active metabolite of the first generation antiandrogen flutamide, was used in clinic to treat prostate cancer targeting androgen receptor (AR). However, a drug resistance problem appears after about one year's treatment. AR T877A is the first mutation that was found to cause a resistance problem. Then W741C_T877A and F876L_T877A mutations were also reported to cause resistance to HF,...
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