Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
Article Details
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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]
- 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