2z4b: Difference between revisions
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|ACTIVITY= | |ACTIVITY= | ||
|GENE= ESR2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= ESR2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
|DOMAIN= | |||
|RELATEDENTRY=[[2q70|2Q70]], [[2i0g|2I0G]], [[2i0j|2I0J]] | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2z4b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2z4b OCA], [http://www.ebi.ac.uk/pdbsum/2z4b PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2z4b RCSB]</span> | |||
}} | }} | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Wang, Y.]] | [[Category: Wang, Y.]] | ||
[[Category: nuclear receptor ligand binding domain]] | [[Category: nuclear receptor ligand binding domain]] | ||
[[Category: transcription]] | [[Category: transcription]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:18:25 2008'' | ||
Revision as of 05:18, 31 March 2008
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| , resolution 2.34Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | ESR2 (Homo sapiens) | ||||||
| Related: | 2Q70, 2I0G, 2I0J
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand
OverviewOverview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe the syntheses of cyclopentanone and cyclohexanone intermediates for SAR studies of the C-ring on the benzopyran scaffold. Modification of the C-ring disrupts binding to ERalpha, thus improving ERbeta selectivity up to 100-fold. X-ray cocrystal structures confirm previously observed binding modes.
About this StructureAbout this Structure
2Z4B is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification., Richardson TI, Dodge JA, Durst GL, Pfeifer LA, Shah J, Wang Y, Durbin JD, Krishnan V, Norman BH, Bioorg Med Chem Lett. 2007 Sep 1;17(17):4824-8. Epub 2007 Jun 20. PMID:17614275
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