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Article

A partially open conformation of an androgen receptor ligand-binding domain with drug-resistance mutations.

Acta crystallographica. Section F, Structural biology communications - 1 Apr 2023

Doamekpor Selom K, Peng Panfeng, Xu Ruo, Ma Liandong, Tong Youzhi, Tong Liang

Abstract excerpt

Mutations in the androgen receptor (AR) ligand-binding domain (LBD) can cause resistance to drugs used to treat prostate cancer. Commonly found mutations include L702H, W742C, H875Y, F877L and T878A, while the F877L mutation can convert second-generation antagonists such as enzalutamide and apalutamide into agonists. However, pruxelutamide, another second-generation AR antagonist, has no agonist activity with the...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 36995121
DOI: 10.1107/S2053230X23002224
PMCID: PMC10071832

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