Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: Design, synthesis, structural biology, and molecular docking studies

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

研究成果: 雜誌貢獻文章同行評審

68 引文 斯高帕斯(Scopus)

摘要

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 PPARγ protein, were important for the potent activity. The hydrophobic tail part of 10k makes intensive hydrophobic interaction with the PPARγ protein resulting in potent activity.

原文英語
頁(從 - 到)1212-1216
頁數5
期刊Journal of Medicinal Chemistry
49
發行號3
DOIs
出版狀態已發佈 - 二月 9 2006
對外發佈

ASJC Scopus subject areas

  • 有機化學

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