2i0g

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Image:2i0g.gif

2i0g, resolution 2.500Å

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Benzopyrans are Selective Estrogen Receptor beta Agonists (SERBAs) with Novel Activity in Models of Benign Prostatic Hyperplasia

Overview

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.

About this Structure

2I0G is a Single protein structure of sequence from Homo sapiens with I0G as ligand. Full crystallographic information is available from OCA.

Reference

Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia., 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, J Med Chem. 2006 Oct 19;49(21):6155-7. PMID:17034120

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