Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.

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Hu B, Quinet E, Unwalla R, Collini M, Jetter J, Dooley R, Andraka D, Nogle L, Savio D, Halpern A, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J

Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):54-9. Epub 2007 Nov 9.

PubMed ID

18023179 [ View in PubMed

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Abstract

A series of potent and binding selective LXRbeta agonists was developed using the previously reported non-selective LXR ligand WAY-254011 as a structural template. With the aid of molecular modeling, it was found that 2,3-diMe-Ph, 2,5-diMe-Ph, and naphthalene substituted quinoline acetic acids (such as quinoline 33, 37, and 38) showed selectivity for LXRbeta over LXRalpha in binding assays.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
TO-901317	Oxysterols receptor LXR-alpha	EC 50 (nM)	135	N/A	N/A	Details
TO-901317	Oxysterols receptor LXR-alpha	IC 50 (nM)	13	N/A	N/A	Details