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Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) delta selective antagonists
Jun-ichi Kasuga1, Seiichi Ishida, Daisuke Yamasaki
1Institute of Molecular and Cellular Biosciences, The University of Tokyo, Tokyo 113-0032, Japan.
Abstract:
We designed and synthesized novel PPARdelta antagonists based on the crystal structure of the PPARdelta full agonist TIPP-204 bound to the PPARdelta ligand-binding domain, in combination with our nuclear receptor helix 12 folding modification hypothesis. Representative compound 3a exhibits PPARdelta-preferential antagonistic activity.
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