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Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.

Abstract：

:Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help explain observed beta-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERbeta effect), while having no effect on gonadal hormone levels (ERalpha effect) at 10x the efficacious dose, consistent with in vitro properties of this molecule.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Norman BH,Dodge JA,Richardson TI,Borromeo PS,Lugar CW,Jones SA,Chen K,Wang Y,Durst GL,Barr RJ,Montrose-Rafizadeh C,Osborne HE,Amos RM,Guo S,Boodhoo A,Krishnan V

doi

10.1021/jm060491j

subject

Has Abstract

pub_date

2006-10-19 00:00:00

pages

6155-7

issue

21

eissn

0022-2623

issn

1520-4804

journal_volume

49

pub_type

杂志文章

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