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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetates / chemistry
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Alkylation
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Binding Sites
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Crystallography, X-Ray
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Humans
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In Vitro Techniques
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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Ligands
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Models, Molecular
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Molecular Structure
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Naphthalenes / chemical synthesis
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Naphthalenes / chemistry
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Naphthalenes / pharmacology
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Peroxisome Proliferator-Activated Receptors / agonists*
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Peroxisome Proliferator-Activated Receptors / chemistry*
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Peroxisome Proliferator-Activated Receptors / genetics
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Propionates / chemistry
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Structure-Activity Relationship
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Thermodynamics
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Transcriptional Activation / drug effects
Substances
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Acetates
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Indoles
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Ligands
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Naphthalenes
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Peroxisome Proliferator-Activated Receptors
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Propionates