Title of article
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRγ
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
821
To page
824
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.
Keywords
Orphan nuclear receptor , ERR? chemical tool
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796468
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