Title : Structural basis for accommodation of nonsteroidal ligands in the androgen receptor.

Pub. Date : 2005 Nov 11

PMID : 16129672






3 Functional Relationships(s)
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1 Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. hydroxyflutamide androgen receptor Homo sapiens
2 Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. hydroxyflutamide androgen receptor Homo sapiens
3 We have shown that changes induced to the positions of Trp-741, Thr-877, and Met-895 allow for ligand accommodation within the AR binding pocket and that a water-mediated hydrogen bond to the backbone oxygen of Leu-873 and the ketone of hydroxyflutamide is present when bound to the T877A AR variant. hydroxyflutamide androgen receptor Homo sapiens