1p8d: Difference between revisions
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New page: left|200px<br /> <applet load="1p8d" size="450" color="white" frame="true" align="right" spinBox="true" caption="1p8d, resolution 2.8Å" /> '''X-Ray Crystal Struct... |
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[[Image:1p8d.gif|left|200px]]<br /> | [[Image:1p8d.gif|left|200px]]<br /><applet load="1p8d" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1p8d" size=" | |||
caption="1p8d, resolution 2.8Å" /> | caption="1p8d, resolution 2.8Å" /> | ||
'''X-Ray Crystal Structure of LXR Ligand Binding Domain with 24(S),25-epoxycholesterol'''<br /> | '''X-Ray Crystal Structure of LXR Ligand Binding Domain with 24(S),25-epoxycholesterol'''<br /> | ||
==Overview== | ==Overview== | ||
The x-ray crystal structures of the human liver X receptor beta ligand | The x-ray crystal structures of the human liver X receptor beta ligand binding domain complexed to sterol and nonsterol agonists revealed a perpendicular histidinetryptophan switch that holds the receptor in its active conformation. Hydrogen bonding interactions with the ligand act to position the His-435 imidazole ring against the Trp-457 indole ring, allowing an electrostatic interaction that holds the AF2 helix in the active position. The neutral oxysterol 24(S),25-epoxycholesterol accepts a hydrogen bond from His-435 that positions the imidazole ring of the histidine above the pyrrole ring of the tryptophan. In contrast, the acidic T0901317 hydroxyl group makes a shorter hydrogen bond with His-435 that pulls the imidazole over the electron-rich benzene ring of the tryptophan, possibly strengthening the electrostatic interaction. Point mutagenesis of Trp-457 supports the observation that the ligand-histidine-tryptophan coupling is different between the two ligands. The lipophilic liver X receptor ligand-binding pocket is larger than the corresponding steroid hormone receptors, which allows T0901317 to adopt two distinct conformations. These results provide a molecular basis for liver X receptor activation by a wide range of endogenous neutral and acidic ligands. | ||
==About this Structure== | ==About this Structure== | ||
1P8D is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CO1 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 1P8D is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CO1:'>CO1</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1P8D OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Bledsoe, R | [[Category: Bledsoe, R K.]] | ||
[[Category: Boggs, S.]] | [[Category: Boggs, S.]] | ||
[[Category: Collins, J | [[Category: Collins, J L.]] | ||
[[Category: Lambert, M | [[Category: Lambert, M H.]] | ||
[[Category: McKee, D | [[Category: McKee, D D.]] | ||
[[Category: Miller, A | [[Category: Miller, A B.]] | ||
[[Category: Moore, J.]] | [[Category: Moore, J.]] | ||
[[Category: Moore, L.]] | [[Category: Moore, L.]] | ||
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[[Category: Watson, M.]] | [[Category: Watson, M.]] | ||
[[Category: Williams, S.]] | [[Category: Williams, S.]] | ||
[[Category: Willson, T | [[Category: Willson, T M.]] | ||
[[Category: Wisely, B.]] | [[Category: Wisely, B.]] | ||
[[Category: CO1]] | [[Category: CO1]] | ||
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[[Category: transcription]] | [[Category: transcription]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:26:14 2008'' | ||
