4dk7 | pdb_00004dk7

Crystal structure of LXR ligand binding domain in complex with full agonist 1

spinqualitylabelsall models 4dk7, resolution 2.45Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4dk7 is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 0KS, ACT, CA, MSE Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [NR1H2_HUMAN] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity). Publication Abstract from PubMed Structural modification of a series of dual LXRalpha/beta agonists led to the identification of a new class of LXRbeta partial agonists. An X-ray co-crystal structure shows that a representative member of this series, pyrrole 5, binds to LXRbeta with a reversed orientation compared to 1. Discovery of a new binding mode for a series of liver X receptor agonists.,Kopecky DJ, Jiao XY, Fisher B, McKendry S, Labelle M, Piper DE, Coward P, Shiau AK, Escaron P, Danao J, Chai A, Jaen J, Kayser F Bioorg Med Chem Lett. 2012 Apr 1;22(7):2407-10. Epub 2012 Feb 20. PMID:22406115 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Liver X receptor

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