Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists

  • J Med Chem. 2006 Oct 19;49(21):6421-4. doi: 10.1021/jm060663c.
Neeraj Mahindroo  1 ,  Yi-Hui Peng ,  Chia-Hui Lin ,  Uan-Kang Tan ,  Ekambaranellore Prakash ,  Tzu-Wen Lien ,  I-Lin Lu ,  Hong-Jen Lee ,  John Tsu-An Hsu ,  Xin Chen ,  Chun-Chen Liao ,  Ping-Chiang Lyu ,  Yu-Sheng Chao ,  Su-Ying Wu ,  Hsing-Pang Hsieh
Affiliations
  • 1. Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China.
PMID: 17034149 DOI: 10.1021/jm060663c
Abstract

Type 2 diabetes has rapidly reached an epidemic proportion becoming a major threat to global public health. PPAR agonists have emerged as a leading class of oral antidiabetic drugs. We report a structure biology analysis of novel indole-based PPAR agonists to explain the structure-activity relationships and present a critical analysis of reasons for change in selectivity with change in the orientation of the same scaffolds. The results would be helpful in designing novel PPAR agonists.

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