2ayr

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[[Image:2ayr.gif|left|200px]]<br /><applet load="2ayr" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2ayr.gif|left|200px]]
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caption="2ayr, resolution 1.900&Aring;" />
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'''A SERM Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats'''<br />
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{{Structure
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|PDB= 2ayr |SIZE=350|CAPTION= <scene name='initialview01'>2ayr</scene>, resolution 1.900&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=L4G:6-(4-METHYLSULFONYL-PHENYL)-5-[4-(2-PIPERIDIN-1-YLETHOXY)PHENOXY]NAPHTHALEN-2-OL'>L4G</scene>
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|ACTIVITY=
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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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'''A SERM Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2AYR 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 <scene name='pdbligand=L4G:'>L4G</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2AYR OCA].
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2AYR is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2AYR OCA].
==Reference==
==Reference==
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A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats., Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA, J Med Chem. 2005 Nov 3;48(22):6772-5. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16250633 16250633]
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A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats., Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA, J Med Chem. 2005 Nov 3;48(22):6772-5. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16250633 16250633]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: transcription regulation]]
[[Category: transcription regulation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:32:31 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:55:31 2008''

Revision as of 13:55, 20 March 2008

Image:2ayr.gif


PDB ID 2ayr

Drag the structure with the mouse to rotate
, resolution 1.900Å
Ligands:
Gene: ESR1, ESR, NR3A1 (Homo sapiens)
Coordinates: save as pdb, mmCIF, xml



A SERM Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats


Contents

Overview

The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors alpha and beta (ERalpha and ERbeta, respectively) and is a potent uterine antagonist with minimal effects on the ovaries as determined by serum biomarkers and histologic evaluation.

Disease

Known diseases associated with this structure: Atherosclerosis, susceptibility to OMIM:[133430], Breast cancer OMIM:[133430], Estrogen resistance OMIM:[133430], HDL response to hormone replacement, augmented OMIM:[133430], Migraine, susceptibility to OMIM:[133430], Myocardial infarction, susceptibility to OMIM:[133430]

About this Structure

2AYR is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats., Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA, J Med Chem. 2005 Nov 3;48(22):6772-5. PMID:16250633

Page seeded by OCA on Thu Mar 20 15:55:31 2008

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