2jj3
From Proteopedia
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| - | [[Image:2jj3. | + | [[Image:2jj3.jpg|left|200px]]<br /><applet load="2jj3" size="450" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2jj3" size="450" color="white" frame="true" align="right" spinBox="true" | + | |
caption="2jj3, resolution 2.28Å" /> | caption="2jj3, resolution 2.28Å" /> | ||
'''ESTROGEN RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH A BENZOPYRAN AGONIST'''<br /> | '''ESTROGEN RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH A BENZOPYRAN AGONIST'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2JJ3 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with JJ3 as [http://en.wikipedia.org/wiki/ligand ligand]. | + | 2JJ3 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with JJ3 as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Jj3 Binding Site For Chain B'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2JJ3 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: zinc-finger]] | [[Category: zinc-finger]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 20:12:24 2007'' |
Revision as of 18:02, 18 December 2007
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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 with JJ3 as ligand. Known structural/functional Site: . 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 Jul 13;. PMID:17662603
Page seeded by OCA on Tue Dec 18 20:12:24 2007
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. | JJ3 | Alternative splicing | Dna-binding | Ligand binding domain | Lipid-binding | Metal-binding | Nuclear receptor | Nucleus | Phosphorylation | Receptor | Steroid-binding | Transcription | Transcription regulation | Zinc | Zinc-finger
