1yim

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[[Image:1yim.gif|left|200px]]
[[Image:1yim.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1yim |SIZE=350|CAPTION= <scene name='initialview01'>1yim</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_1yim", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CM4:(2R,3R,4S)-3-(4-HYDROXYPHENYL)-4-METHYL-2-[4-(2-PYRROLIDIN-1-YLETHOXY)PHENYL]CHROMAN-6-OL'>CM4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= ESR1, ESR, NR3A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1yim| PDB=1yim | SCENE= }}
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|RELATEDENTRY=[[1yin|1YIN]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yim FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yim OCA], [http://www.ebi.ac.uk/pdbsum/1yim PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yim RCSB]</span>
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}}
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'''Human estrogen receptor alpha ligand-binding domain in complex with compound 4'''
'''Human estrogen receptor alpha ligand-binding domain in complex with compound 4'''
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[[Category: Fitzgerald, P M.]]
[[Category: Fitzgerald, P M.]]
[[Category: Sharma, N.]]
[[Category: Sharma, N.]]
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[[Category: antagonist]]
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[[Category: Antagonist]]
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[[Category: er-alpha]]
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[[Category: Er-alpha]]
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[[Category: nuclear receptor]]
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[[Category: Nuclear receptor]]
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[[Category: transcription factor]]
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[[Category: Transcription factor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:21:50 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:08:36 2008''
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Revision as of 13:21, 3 May 2008

Image:1yim.gif

Template:STRUCTURE 1yim

Human estrogen receptor alpha ligand-binding domain in complex with compound 4


Overview

The discovery, synthesis, and SAR of chromanes as ER alpha subtype selective ligands are described. X-ray studies revealed that the origin of the ER alpha-selectivity resulted from a C-4 trans methyl substitution to the cis-2,3-diphenyl-chromane platform. Selected compounds from this class demonstrated very potent in vivo antagonism of estradiol in an immature rat uterine weight assay, effectively inhibited ovariectomy-induced bone resorption in a 42 days treatment paradigm, and lowered serum cholesterol levels in ovx'd adult rat models. The best antagonists 8F and 12F also exhibited potent inhibition of MCF-7 cell growth and were shown to be estrogen receptor down-regulators (SERDs).

About this Structure

1YIM is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs., Tan Q, Blizzard TA, Morgan JD 2nd, Birzin ET, Chan W, Yang YT, Pai LY, Hayes EC, DaSilva CA, Warrier S, Yudkovitz J, Wilkinson HA, Sharma N, Fitzgerald PM, Li S, Colwell L, Fisher JE, Adamski S, Reszka AA, Kimmel D, DiNinno F, Rohrer SP, Freedman LP, Schaeffer JM, Hammond ML, Bioorg Med Chem Lett. 2005 Mar 15;15(6):1675-81. PMID:15745820 Page seeded by OCA on Sat May 3 16:21:50 2008

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OCA

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