2nv7: Difference between revisions
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==Overview== | ==Overview== | ||
A series of 4'-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared | A series of 4'-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high affinity (4nM) and modest selectivity (39-fold) for estrogen receptor-beta (ERbeta). Substitution of one of the core rings of the scaffold based around these novel ligands further expanded our knowledge in the quest toward achieving high affinity and selectivity for ERbeta. An X-ray co-crystal of structure 11 revealed that the oxime moiety was mimicking the C-ring of genistein, as previously predicted by SAR and docking studies. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Bowen, M | [[Category: Bowen, M S.]] | ||
[[Category: Cohn, S | [[Category: Cohn, S T.]] | ||
[[Category: Harris, H | [[Category: Harris, H A.]] | ||
[[Category: Manas, E | [[Category: Manas, E S.]] | ||
[[Category: Mewshaw, R | [[Category: Mewshaw, R E.]] | ||
[[Category: RSGI, RIKEN | [[Category: RSGI, RIKEN Structural Genomics/Proteomics Initiative.]] | ||
[[Category: Xu, Z | [[Category: Xu, Z B.]] | ||
[[Category: 555]] | [[Category: 555]] | ||
[[Category: agonist]] | [[Category: agonist]] | ||
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[[Category: transcription factor]] | [[Category: transcription factor]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:11:26 2008'' | ||
Revision as of 19:11, 21 February 2008
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Crystal Structure of Estrogen Receptor Beta Complexed with WAY-555
OverviewOverview
A series of 4'-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high affinity (4nM) and modest selectivity (39-fold) for estrogen receptor-beta (ERbeta). Substitution of one of the core rings of the scaffold based around these novel ligands further expanded our knowledge in the quest toward achieving high affinity and selectivity for ERbeta. An X-ray co-crystal of structure 11 revealed that the oxime moiety was mimicking the C-ring of genistein, as previously predicted by SAR and docking studies.
About this StructureAbout this Structure
2NV7 is a Protein complex structure of sequences from Homo sapiens with as ligand. Active as Histone acetyltransferase, with EC number 2.3.1.48 Full crystallographic information is available from OCA.
ReferenceReference
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives., Mewshaw RE, Bowen SM, Harris HA, Xu ZB, Manas ES, Cohn ST, Bioorg Med Chem Lett. 2007 Feb 15;17(4):902-6. Epub 2006 Dec 1. PMID:17188490
Page seeded by OCA on Thu Feb 21 18:11:26 2008
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Histone acetyltransferase
- Homo sapiens
- Protein complex
- Bowen, M S.
- Cohn, S T.
- Harris, H A.
- Manas, E S.
- Mewshaw, R E.
- RSGI, RIKEN Structural Genomics/Proteomics Initiative.
- Xu, Z B.
- 555
- Agonist
- Er
- Er-beta
- Estrogen
- Estrogen receptor
- Estrogen receptor beta
- National project on protein structural and functional analyses
- Nppsfa
- Nuclear receptor
- Riken structural genomics/proteomics initiative
- Rsgi
- Structural genomics
- Transcription factor