| Literature DB >> 16451087 |
Neeraj Mahindroo1, 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.Entities:
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Year: 2006 PMID: 16451087 DOI: 10.1021/jm0510373
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446