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

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58 Citations (Scopus)

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 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.

Original languageEnglish
Pages (from-to)1212-1216
Number of pages5
JournalJournal of Medicinal Chemistry
Volume49
Issue number3
DOIs
Publication statusPublished - Feb 9 2006
Externally publishedYes

ASJC Scopus subject areas

  • Organic Chemistry

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  • Cite this

    Mahindroo, N., Wang, C. C., Liao, C. C., Huang, C. F., Lu, I. L., Lien, T. W., Peng, Y. H., Huang, W. J., Lin, Y. T., Hsu, M. C., Lin, C. H., Tsai, C. H., Hsu, J. T. A., Chen, X., Lyu, P. C., Chao, Y. S., Wu, S. Y., & Hsieh, H. P. (2006). Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: Design, synthesis, structural biology, and molecular docking studies. Journal of Medicinal Chemistry, 49(3), 1212-1216. https://doi.org/10.1021/jm0510373