Benzopyrans Are Selective Estrogen Receptor Agonists with Novel Activity in Models of Benign Prostatic Hyperplasia

Autor: H. Norman, Bryan, A. Dodge, Jeffrey, I. Richardson, Timothy, S. Borromeo, Peter, W. Lugar, Charles, A. Jones, Scott, Chen, Keyue, Wang, Yong, L. Durst, Gregory, J. Barr, Robert, Montrose-Rafizadeh, Chahrzad, E. Osborne, Harold, M. Amos, Robert, Guo, Sherry, Boodhoo, Amechand, Krishnan, Venkatesh
Zdroj: Journal of Medicinal Chemistry; October 2006, Vol. 49 Issue: 21 p6155-6157, 3p
Abstrakt: Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor (ER) in vitro assays. X-ray crystal structures of SERBA-1 in ER and help explain observed -selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ER effect), while having no effect on gonadal hormone levels (ER effect) at 10× the efficacious dose, consistent with in vitro properties of this molecule.
Databáze: Supplemental Index