1p8d
From Proteopedia
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| - | + | {{STRUCTURE_1p8d| PDB=1p8d | SCENE= }} | |
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'''X-Ray Crystal Structure of LXR Ligand Binding Domain with 24(S),25-epoxycholesterol''' | '''X-Ray Crystal Structure of LXR Ligand Binding Domain with 24(S),25-epoxycholesterol''' | ||
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[[Category: Willson, T M.]] | [[Category: Willson, T M.]] | ||
[[Category: Wisely, B.]] | [[Category: Wisely, B.]] | ||
| - | [[Category: | + | [[Category: Epoxycholesterol]] |
| - | [[Category: | + | [[Category: Liver x receptor]] |
| - | [[Category: | + | [[Category: Lxr]] |
| - | [[Category: | + | [[Category: Nuclear receptor]] |
| - | [[Category: | + | [[Category: Steroid receptor]] |
| - | [[Category: | + | [[Category: Transcription]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:48:45 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 01:48, 3 May 2008
X-Ray Crystal Structure of LXR Ligand Binding Domain with 24(S),25-epoxycholesterol
Overview
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
1P8D is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
X-ray crystal structure of the liver X receptor beta ligand binding domain: regulation by a histidine-tryptophan switch., Williams S, Bledsoe RK, Collins JL, Boggs S, Lambert MH, Miller AB, Moore J, McKee DD, Moore L, Nichols J, Parks D, Watson M, Wisely B, Willson TM, J Biol Chem. 2003 Jul 18;278(29):27138-43. Epub 2003 May 7. PMID:12736258 Page seeded by OCA on Sat May 3 04:48:45 2008
Categories: Homo sapiens | Protein complex | Bledsoe, R K. | Boggs, S. | Collins, J L. | Lambert, M H. | McKee, D D. | Miller, A B. | Moore, J. | Moore, L. | Nichols, J. | Parks, D. | Watson, M. | Williams, S. | Willson, T M. | Wisely, B. | Epoxycholesterol | Liver x receptor | Lxr | Nuclear receptor | Steroid receptor | Transcription
