2hwq
Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists
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OverviewOverview
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.
DiseaseDisease
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 StructureAbout this Structure
2HWQ is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
ReferenceReference
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
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