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

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Mahindroo N, Peng YH, Lin CH, Tan UK, Prakash E, Lien TW, Lu IL, Lee HJ, Hsu JT, Chen X, Liao CC, Lyu PC, Chao YS, Wu SY, Hsieh HP

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

J Med Chem. 2006 Oct 19;49(21):6421-4.

PubMed ID

17034149 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-{5-[3-(6-BENZOYL-1-PROPYLNAPHTHALEN-2-YLOXY)PROPOXY]INDOL-1-YL}ETHANOIC ACID	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	70	N/A	N/A	Details
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	220	N/A	N/A	Details