Structural biology-based exploration of subtype-selective agonists for peroxisome proliferator-activated receptors

HIGHLIGHTS

  • who: Hiroyuki Miyachi from the Lead Exploration Unit, Drug Discovery Initiative, The University of Tokyo, Hongo, Bunkyo-ku have published the article: Structural Biology-Based Exploration of Subtype-Selective Agonists for Peroxisome Proliferator-Activated Receptors, in the Journal: (JOURNAL)
  • what: The authors aimed to develop PPARα-selective agonists as anti-dyslipidemic agents by designing and synthesizing a series of substituted phenylpropanoic acid derivatives using as lead compound, KRP297, a unique TZD derivative with PPARγ/α dual agonist activity . The authors focused the attention on a hybrid type tether, i.e., -CO-NH-CH2 -, and found that . . .

     

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