2. Academic Validation
  3. Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists

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

Affiliation

  • 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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