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Updated: Feb 15, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved
Sayaka Nomura1, Kaori Endo-Umeda2, Shinya Fujii1
1Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
Abstract:
LXRβ-selective agonists are promising candidates to improve atherosclerosis without increasing plasma or hepatic TG levels. We have reported a series of tetrachlorophthalimide analogs as an LXRβ-selective agonist. However, they exhibited poor aqueous solubility probably due to its high hydrophobicity and highly rigid and plane structure. In this report, we present further structural development of tetrachloro(styrylphenyl)phthalimides as the LXRβ-selective agonists with improved aqueous solubility.
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