Discovery of a new binding mode for a series of liver X receptor agonists.

Article Details

Citation

Copy to clipboard

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. doi: 10.1016/j.bmcl.2012.02.028. Epub 2012 Feb 20.

PubMed ID

22406115 [ View in PubMed

]

Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
TO-901317	Oxysterols receptor LXR-alpha	IC 50 (nM)	100	N/A	N/A	Details