Article
Allosteric conversation in the androgen receptor ligand-binding domain surfaces.
Molecular endocrinology (Baltimore, Md.) - 1 Jul 2012
Grosdidier Solène, Carbó Laia R, Buzón Víctor, Brooke Greg, Nguyen Phuong, Baxter John D, Bevan Charlotte, Webb Paul, Estébanez-Perpiñá Eva, Fernández-Recio Juan
Abstract excerpt
Androgen receptor (AR) is a major therapeutic target that plays pivotal roles in prostate cancer (PCa) and androgen insensitivity syndromes. We previously proposed that compounds recruited to ligand-binding domain (LBD) surfaces could regulate AR activity in hormone-refractory PCa and discovered several surface modulators of AR function. Surprisingly, the most effective compounds bound preferentially to a surface...
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