2pog | pdb_00002pog
Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.
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| 2pog, resolution 1.840Å | |||||||||||||
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| Ligands: | WST | ||||||||||||
| Gene: | ESR1 (Homo sapiens) | ||||||||||||
| Related: | 2I0G
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Overview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe structure-activity relationship studies that led to the discovery of bezopyran 5b. X-ray crystal structures of 5b and a non-selective analog 5c in ERalpha help explain the observed selectivity of the benzopyran platform.
About this Structure
2POG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold., Richardson TI, Norman BH, Lugar CW, Jones SA, Wang Y, Durbin JD, Krishnan V, Dodge JA, Bioorg Med Chem Lett. 2007 Jul 1;17(13):3570-4. Epub 2007 Apr 25. PMID:17485205
Page seeded by OCA on Mon Mar 31 04:38:42 2008
