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Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226

Acta Cryst. (2006). F62, 1067-1071 [doi:10.1107/S1744309106039340]

[androgen receptor]Superposition comparison between the ligands of LGD2226 and R1881 in ligand–AR LBD complexes. Part of the LGD2226–AR LBD complex is shown in red; part of the R1881–AR LBD complex are shown in blue.
The androgen receptor (AR) is a ligand-inducible steroid hormone receptor that mediates androgen action, determining male sexual phenotypes and promoting spermatogenesis. LGD2226 is a synthetic non-steroidal ligand and a novel selective AR modulator. Here we reported the crystal structure of the complex of LGD2226 with the androgen receptor ligand-binding domain (AR LBD) at 2.1 Å and compared it with the structure of the AR LBD–R1881 complex. It will aid in further explaining the selectivity of LGD2226 and in developing more selective and effective therapeutic agents.
F. Wang, X. Liu, H. Li, K. Liang, J.N. Miner, M. Hong, E.A. Kallel, A. van Oeveren, L. Zhi and T. Jiang