Indol-1-yl Acetic Acids as Peroxisome Proliferator-Activated Receptor Agonists: Design, Synthesis, Structural Biology, and Molecular Docking Studies
Journal of Medicinal Chemistry2006Vol. 49(3), pp. 1212–1216
Citations Over TimeTop 10% of 2006 papers
Neeraj Mahindroo, Chiung-Chiu Wang, Chun-Chen Liao, Chien-Fu Huang, I-Lin Lu, Tzu‐Wen Lien, Yi-Huei Peng, Wei‐Jan Huang, Ying‐Ting Lin, Ming‐Chen Hsu, Chia‐Hui Lin, Chia‐Hua Tsai, John T.-A. Hsu, Xin Chen, Ping‐Chiang Lyu, Yu‐Sheng Chao, Su‐Ying Wu, Hsing‐Pang Hsieh
Abstract
A series of novel indole-based PPAR agonists is described leading to discovery of 10k, a highly potent PPAR pan-agonist. The structural biology and molecular docking studies revealed that the distances between the acidic group and the linker, when a ligand was complexed with PPARgamma protein, were important for the potent activity. The hydrophobic tail part of 10k makes intensive hydrophobic interaction with the PPARgamma protein resulting in potent activity.
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