Discovery and optimization of a novel series of liver X receptor-alpha agonists.

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Li L, Liu J, Zhu L, Cutler S, Hasegawa H, Shan B, Medina JC

Discovery and optimization of a novel series of liver X receptor-alpha agonists.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1638-42. Epub 2005 Dec 28.

PubMed ID

16386417 [ View in PubMed

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Abstract

A novel series of hexafluorocarbinols were discovered as potent activators of the liver X receptor-alpha using a fluorescence polarization assay. Structure-activity relationship study led to the identification of compounds that are more potent agonists than the endogenous ligand, 24(S), 25-epoxycholesterol, with similar efficacy. Several compounds, including T0901317, were shown to have desirable pharmacokinetic profiles suitable for in vivo studies.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
TO-901317	Oxysterols receptor LXR-alpha	EC 50 (nM)	10	N/A	N/A	Details