Structural highlights
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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ 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. Discovery of a new binding mode for a series of liver X receptor agonists. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2407-10. Epub 2012 Feb 20. PMID:22406115 doi:10.1016/j.bmcl.2012.02.028
