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1sqn

From Proteopedia

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[[Image:1sqn.gif|left|200px]]
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{{STRUCTURE_1sqn| PDB=1sqn | SCENE= }}
{{STRUCTURE_1sqn| PDB=1sqn | SCENE= }}
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'''Progesterone Receptor Ligand Binding Domain with bound Norethindrone'''
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===Progesterone Receptor Ligand Binding Domain with bound Norethindrone===
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==Overview==
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Although progesterone, the natural ligand of the progesterone receptor (PR), has a hydrogen atom at the 17alpha position, other potent steroid agonists such as norethindrone and mometasone furoate have larger substituents at this position that are accommodated by the PR ligand binding pocket. Crystallographic analysis of PR ligand binding domain complexes clearly demonstrated that these moieties were accommodated by local shifts of the protein main chain and by adoption of alternative side chain rotamer conformations of ligand-proximal amino acids. These conformational changes imparted a ligand-specific volume to the binding pocket, from 490 A3 in the metribolone complex to 520 A3 in the norethindrone complex, 565 A3 in the progesterone complex, and 730 A3 in the mometasone furoate complex. Despite these marked alterations in binding pocket volume, critical interactions essential for establishment of an active AF2 conformation were maintained.
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(as it appears on PubMed at http://www.pubmed.gov), where 15189034 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15189034}}
==About this Structure==
==About this Structure==
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[[Category: Progesterone receptor]]
[[Category: Progesterone receptor]]
[[Category: Steroid receptor]]
[[Category: Steroid receptor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:01:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 15:12:07 2008''

Revision as of 12:12, 27 July 2008

Image:1sqn.png

Template:STRUCTURE 1sqn

Progesterone Receptor Ligand Binding Domain with bound Norethindrone

Template:ABSTRACT PUBMED 15189034

About this Structure

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

Reference

Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes., Madauss KP, Deng SJ, Austin RJ, Lambert MH, McLay I, Pritchard J, Short SA, Stewart EL, Uings IJ, Williams SP, J Med Chem. 2004 Jun 17;47(13):3381-7. PMID:15189034

Page seeded by OCA on Sun Jul 27 15:12:07 2008

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