Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) d-selective partial agonists by disruption of molecular planarity/symmetry

• Published in: Bioorganic & medicinal chemistry Vol. 18; no. 20; pp. 7164 - 7173
• Main Authors: Kasuga, Jun-Ichi, Ishikawa, Minoru, Yonehara, Mitsuhiro, Makishima, Makoto, Hashimoto, Yuichi, Miyachi, Hiroyuki
• Format: Journal Article
• Language: English
• Published: 15.10.2010
• Subjects: Biphenyl

To elucidate the molecular basis of peroxisome proliferator-activated receptor (PPAR) d partial agonism, X-ray crystal structures of complexes of the PPARd ligand-binding site with partial agonists are required. Unfortunately, reported PPARd partial agonists, biphenylcarboxylic acids 1 and 2, posses...