2acl
From Proteopedia
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|PDB= 2acl |SIZE=350|CAPTION= <scene name='initialview01'>2acl</scene>, resolution 2.8Å | |PDB= 2acl |SIZE=350|CAPTION= <scene name='initialview01'>2acl</scene>, resolution 2.8Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=L05:1-BENZYL-3-(4-METHOXYPHENYLAMINO)-4-PHENYLPYRROLE-2,5-DIONE'>L05</scene> | + | |LIGAND= <scene name='pdbligand=L05:1-BENZYL-3-(4-METHOXYPHENYLAMINO)-4-PHENYLPYRROLE-2,5-DIONE'>L05</scene>, <scene name='pdbligand=REA:RETINOIC+ACID'>REA</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), Nr1h3, Lxra ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus]) | |GENE= RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), Nr1h3, Lxra ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2acl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2acl OCA], [http://www.ebi.ac.uk/pdbsum/2acl PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2acl RCSB]</span> | ||
}} | }} | ||
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[[Category: Qiu, C.]] | [[Category: Qiu, C.]] | ||
[[Category: Smallwood, A.]] | [[Category: Smallwood, A.]] | ||
| - | [[Category: L05]] | ||
| - | [[Category: REA]] | ||
[[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://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:50:50 2008'' |
Revision as of 22:50, 30 March 2008
| |||||||
| , resolution 2.8Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Gene: | RXRA, NR2B1 (Homo sapiens), Nr1h3, Lxra (Mus musculus) | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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 Mon Mar 31 01:50:50 2008
