2I0G: Benzopyrans Are Selective Estrogen Receptor Beta Agonists (serbas) With Novel Activity In Models Of Benign Prostatic Hyperplasia

Citation:
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.
PDB ID: 2I0GDownload
MMDB ID: 42297
PDB Deposition Date: 2006/8/10
Updated in MMDB: 2006/11
Experimental Method:
x-ray diffraction
Resolution: 2.5  Å
Source Organism:
Similar Structures:
Biological Unit for 2I0G: dimeric; determined by author and by software (PISA)
Molecular Components in 2I0G
Label Count Molecule
Proteins (2 molecules)
2
Estrogen Receptor Beta(Gene symbol: ESR2)
Molecule annotation
Chemicals (2 molecules)
1
2
* Click molecule labels to explore molecular sequence information.

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