2acl
From Proteopedia
(New page: 200px<br /> <applet load="2acl" size="450" color="white" frame="true" align="right" spinBox="true" caption="2acl, resolution 2.8Å" /> '''Liver X-Receptor alp...) |
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| - | [[Image:2acl.gif|left|200px]]<br /> | + | [[Image:2acl.gif|left|200px]]<br /><applet load="2acl" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2acl" size=" | + | |
caption="2acl, resolution 2.8Å" /> | caption="2acl, resolution 2.8Å" /> | ||
'''Liver X-Receptor alpha Ligand Binding Domain with SB313987'''<br /> | '''Liver X-Receptor alpha Ligand Binding Domain with SB313987'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a | + | Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40 nM, profiles as an LXR agonist in functional assays, and activates LXR though a mechanism that is similar to first generation LXR agonists. |
==About this Structure== | ==About this Structure== | ||
| - | 2ACL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with L05 and REA as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 2ACL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=L05:'>L05</scene> and <scene name='pdbligand=REA:'>REA</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ACL OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Campobasso, N.]] | [[Category: Campobasso, N.]] | ||
| - | [[Category: Jaye, M | + | [[Category: Jaye, M C.]] |
| - | [[Category: Kerrigan, J | + | [[Category: Kerrigan, J J.]] |
| - | [[Category: Krawiec, J | + | [[Category: Krawiec, J A.]] |
[[Category: Lu, Q.]] | [[Category: Lu, Q.]] | ||
[[Category: Qiu, C.]] | [[Category: Qiu, C.]] | ||
| Line 26: | Line 25: | ||
[[Category: nuclear hormone receptor ligand binding domain transcription factor three layered a-helix fold]] | [[Category: nuclear hormone receptor ligand binding domain transcription factor three layered a-helix fold]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:26:07 2008'' |
Revision as of 14:26, 21 February 2008
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Liver X-Receptor alpha Ligand Binding Domain with SB313987
Overview
Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40 nM, profiles as an LXR agonist in functional assays, and activates LXR though a mechanism that is similar to first generation LXR agonists.
About this Structure
2ACL is a Protein complex structure of sequences from Homo sapiens and Mus musculus with and as ligands. Full crystallographic information is available from OCA.
Reference
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure., Jaye MC, Krawiec JA, Campobasso N, Smallwood A, Qiu C, Lu Q, Kerrigan JJ, De Los Frailes Alvaro M, Laffitte B, Liu WS, Marino JP Jr, Meyer CR, Nichols JA, Parks DJ, Perez P, Sarov-Blat L, Seepersaud SD, Steplewski KM, Thompson SK, Wang P, Watson MA, Webb CL, Haigh D, Caravella JA, Macphee CH, Willson TM, Collins JL, J Med Chem. 2005 Aug 25;48(17):5419-22. PMID:16107141
Page seeded by OCA on Thu Feb 21 16:26:07 2008
