2jj3
From Proteopedia
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|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1x7b|1X7B]], [[1x7j|1X7J]], [[1yy4|1YY4]], [[2fsz|2FSZ]], [[1l2j|1L2J]], [[1nde|1NDE]], [[1qkm|1QKM]], [[1u3q|1U3Q]], [[1u3r|1U3R]], [[1u3s|1U3S]], [[1u9e|1U9E]], [[1x76|1X76]], [[1x78|1X78]], [[1yye|1YYE]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2jj3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2jj3 OCA], [http://www.ebi.ac.uk/pdbsum/2jj3 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2jj3 RCSB]</span> | ||
}} | }} | ||
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[[Category: Ryter, K T.]] | [[Category: Ryter, K T.]] | ||
[[Category: Wang, Y.]] | [[Category: Wang, Y.]] | ||
| - | [[Category: JJ3]] | ||
[[Category: alternative splicing]] | [[Category: alternative splicing]] | ||
[[Category: dna-binding]] | [[Category: dna-binding]] | ||
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[[Category: zinc-finger]] | [[Category: zinc-finger]] | ||
| - | ''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 03:58:59 2008'' |
Revision as of 00:59, 31 March 2008
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| , resolution 2.28Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | |||||||
| Ligands: | |||||||
| Related: | 1X7B, 1X7J, 1YY4, 2FSZ, 1L2J, 1NDE, 1QKM, 1U3Q, 1U3R, 1U3S, 1U9E, 1X76, 1X78, 1YYE
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
ESTROGEN RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH A BENZOPYRAN AGONIST
Overview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER receptor subtypes alpha and beta in opposite orientations. We have used structure based drug design to show that this unique phenomena can be exploited via substitution at the 8-position of the benzopyran A-ring to disrupt binding to ERalpha, thus improving ERbeta subtype selectivity. X-ray cocrystal structures with ERalpha and ERbeta are supportive of this approach to improve selectivity in this structural class.
About this Structure
2JJ3 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 4: functionalization of the benzopyran A-ring., Norman BH, Richardson TI, Dodge JA, Pfeifer LA, Durst GL, Wang Y, Durbin JD, Krishnan V, Dinn SR, Liu S, Reilly JE, Ryter KT, Bioorg Med Chem Lett. 2007 Sep 15;17(18):5082-5. Epub 2007 Jul 13. PMID:17662603
Page seeded by OCA on Mon Mar 31 03:58:59 2008
Categories: Homo sapiens | Single protein | Dinn, S R. | Dodge, J A. | Durbin, J D. | Durst, G L. | Krishnan, V. | Liu, S. | Norman, B H. | Pfeifer, L A. | Reilly, J E. | Richardson, T I. | Ryter, K T. | Wang, Y. | Alternative splicing | Dna-binding | Ligand binding domain | Lipid-binding | Metal-binding | Nuclear receptor | Nucleus | Phosphorylation | Receptor | Steroid-binding | Transcription | Transcription regulation | Zinc | Zinc-finger
