Structural Basis for the Structure−Activity Relationships of Peroxisome Proliferator-Activated Receptor Agonists

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 relations...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2006-10, Vol.49 (21), p.6421-6424
Main Authors: Mahindroo, Neeraj, Peng, Yi-Hui, Lin, Chia-Hui, Tan, Uan-Kang, Prakash, Ekambaranellore, Lien, Tzu-Wen, Lu, I-Lin, Lee, Hong-Jen, Hsu, John Tsu-An, Chen, Xin, Liao, Chun-Chen, Lyu, Ping-Chiang, Chao, Yu-Sheng, Wu, Su-Ying, Hsieh, Hsing-Pang
Format: Article
Language:English
Subjects:
Acetates - chemistry
Alkylation
Binding Sites
Biological and medical sciences
Crystallography, X-Ray
General and cellular metabolism. Vitamins
Humans
In Vitro Techniques
Indoles - chemical synthesis
Indoles - chemistry
Indoles - pharmacology
Ligands
Medical sciences
Models, Molecular
Molecular Structure
Naphthalenes - chemical synthesis
Naphthalenes - chemistry
Naphthalenes - pharmacology
Peroxisome Proliferator-Activated Receptors - agonists
Peroxisome Proliferator-Activated Receptors - chemistry
Peroxisome Proliferator-Activated Receptors - genetics
Pharmacology. Drug treatments
Propionates - chemistry
Structure-Activity Relationship
Thermodynamics
Transcriptional Activation - drug effects
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm060663c