2giu
From Proteopedia
| Line 4: | Line 4: | ||
|PDB= 2giu |SIZE=350|CAPTION= <scene name='initialview01'>2giu</scene>, resolution 2.2Å | |PDB= 2giu |SIZE=350|CAPTION= <scene name='initialview01'>2giu</scene>, resolution 2.2Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=FBR:( | + | |LIGAND= <scene name='pdbligand=FBR:(9AS)-4-BROMO-9A-BUTYL-7-HYDROXY-1,2,9,9A-TETRAHYDRO-3H-FLUOREN-3-ONE'>FBR</scene> |
|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= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2giu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2giu OCA], [http://www.ebi.ac.uk/pdbsum/2giu PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2giu RCSB]</span> | ||
}} | }} | ||
| Line 24: | Line 27: | ||
[[Category: Fitzgerald, P M.D.]] | [[Category: Fitzgerald, P M.D.]] | ||
[[Category: Sharma, N.]] | [[Category: Sharma, N.]] | ||
| - | [[Category: FBR]] | ||
[[Category: agonist]] | [[Category: agonist]] | ||
[[Category: er-beta]] | [[Category: er-beta]] | ||
| Line 30: | Line 32: | ||
[[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 Mon Mar 31 03:17:16 2008'' |
Revision as of 00:17, 31 March 2008
| |||||||
| , resolution 2.2Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | ESR2 (Homo sapiens) | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Human estrogen receptor beta ligand-binding domain in complex with compound 45
Overview
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
About this Structure
2GIU is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands., Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2. PMID:16632357
Page seeded by OCA on Mon Mar 31 03:17:16 2008
