Author/Authors :
Esther Y.H. Chao، نويسنده , , Jon L. Collins، نويسنده , , Stéphanie Gaillard، نويسنده , , Aaron B. Miller، نويسنده , , Liping Wang، نويسنده , , Lisa A. Orband-Miller، نويسنده , , Robert T. Nolte، نويسنده , , Donald P. McDonnell، نويسنده , , Timothy M. Willson and Shawn P. Williams، نويسنده , , William J. Zuercher، نويسنده ,
Abstract :
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor γ and the classical estrogen receptor α demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRγ LBD confirms the molecular basis of the selectivity.
