Indol-1-yl Acetic Acids as Peroxisome Proliferator-Activated Receptor Agonists: Design, Synthesis, Structural Biology, and Molecular Docking Studies
Neeraj Mahindroo(National Defense Medical Center), Chiung-Chiu Wang(National Tsing Hua University), Chun-Chen Liao(National Health Research Institutes), Chien-Fu Huang(National Tsing Hua University), I-Lin Lu(National Defense Medical Center), Tzu‐Wen Lien(National Tsing Hua University), Yi-Huei Peng(National Tsing Hua University), Wei‐Jan Huang(National Defense Medical Center), Ying‐Ting Lin(National Tsing Hua University), Ming‐Chen Hsu(National Defense Medical Center), Chia‐Hui Lin(National Tsing Hua University), Chia‐Hua Tsai(National Tsing Hua University), John T.-A. Hsu(National Health Research Institutes), Xin Chen(National Tsing Hua University), Ping‐Chiang Lyu(National Tsing Hua University), Yu‐Sheng Chao(National Health Research Institutes), Su‐Ying Wu(National Health Research Institutes), Hsing‐Pang Hsieh(National Health Research Institutes)
Cited by 71Open Access
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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