1sr7: Difference between revisions
New page: left|200px<br /> <applet load="1sr7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1sr7, resolution 1.46Å" /> '''Progesterone Recept... |
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[[Image:1sr7.gif|left|200px]]<br /> | [[Image:1sr7.gif|left|200px]]<br /><applet load="1sr7" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="1sr7, resolution 1.46Å" /> | caption="1sr7, resolution 1.46Å" /> | ||
'''Progesterone Receptor Hormone Binding Domain with Bound Mometasone Furoate'''<br /> | '''Progesterone Receptor Hormone Binding Domain with Bound Mometasone Furoate'''<br /> | ||
==Overview== | ==Overview== | ||
Although progesterone, the natural ligand of the progesterone receptor | 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. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
1SR7 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 SO4, MOF and GOL as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | 1SR7 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=SO4:'>SO4</scene>, <scene name='pdbligand=MOF:'>MOF</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SR7 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Austin, R | [[Category: Austin, R J.]] | ||
[[Category: Deng, S | [[Category: Deng, S J.]] | ||
[[Category: Lambert, M | [[Category: Lambert, M H.]] | ||
[[Category: Madauss, K | [[Category: Madauss, K P.]] | ||
[[Category: McLay, I.]] | [[Category: McLay, I.]] | ||
[[Category: Pritchard, J.]] | [[Category: Pritchard, J.]] | ||
[[Category: Short, S | [[Category: Short, S A.]] | ||
[[Category: Stewart, E | [[Category: Stewart, E L.]] | ||
[[Category: Uings, I | [[Category: Uings, I J.]] | ||
[[Category: Williams, S | [[Category: Williams, S P.]] | ||
[[Category: GOL]] | [[Category: GOL]] | ||
[[Category: MOF]] | [[Category: MOF]] | ||
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[[Category: progesterone receptor]] | [[Category: progesterone receptor]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:04:22 2008'' | ||
Revision as of 16:04, 21 February 2008
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Progesterone Receptor Hormone Binding Domain with Bound Mometasone Furoate
OverviewOverview
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.
DiseaseDisease
Known disease associated with this structure: Progesterone resistance, 264080 (2) OMIM:[607311]
About this StructureAbout this Structure
1SR7 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Full crystallographic information is available from OCA.
ReferenceReference
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
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