2hwq

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spinqualitylabelsall models 2hwq, resolution 1.97Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

Overview

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.

Disease

Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[601487], Diabetes mellitus, insulin-resistant, with acanthosis nigricans and hypertension OMIM:[601487], Glioblastoma, susceptibility to OMIM:[601487], Insulin resistance, severe, digenic OMIM:[601487], Lipodystrophy, familial partial OMIM:[601487], Obesity, resistance to OMIM:[601487], Obesity, severe OMIM:[601487]

About this Structure

2HWQ is a Single protein structure of sequence from Homo sapiens with DRY as ligand. Full crystallographic information is available from OCA.

Reference

Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists., 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, J Med Chem. 2006 Oct 19;49(21):6421-4. PMID:17034149

Page seeded by OCA on Mon Nov 12 22:37:39 2007