4.5 Article

Truxillic acid derivatives act as peroxisome proliferator-activated receptor γ activators

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 9, Pages 2920-2923

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.03.026

Keywords

Nuclear receptors; PPAR gamma; Truxillic acid derivatives; Reporter gene assay; Molecular docking; Structure-activity relationships

Funding

  1. Else-Kroener-Fresenius-Stiftung
  2. FIRST (Frankfurt International Research School for Translational Biomedicine)
  3. Lipid Signaling Forschungszentrum Frankfurt (LiFF)

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In previous studies, we identified a truxillic acid derivative as selective activator of the peroxisome proliferator-activated receptor gamma, which is a member of the nuclear receptor family and acts as ligand-activated transcription factor of genes involved in glucose metabolism. Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis. (C) 2010 Elsevier Ltd. All rights reserved.

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