(Z)-2-(2-Bromophenyl)-3-{[4-(1-methyl-piperazine) amino] phenyl} acrylonitrile (DG172): An Orally Bioavailable PPARβ/δ-Selective Ligand with Inverse Agonistic …

S Lieber, F Scheer, W Meissner, S Naruhn…

Index: Lieber, Sonja; Scheer, Frithjof; Meissner, Wolfgang; Naruhn, Simone; Adhikary, Till; Mueller-Bruesselbach, Sabine; Diederich, Wibke E.; Mueller, Rolf Journal of Medicinal Chemistry, 2012 , vol. 55, # 6 p. 2858 - 2868

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Citation Number: 26

Abstract

The ligand-regulated nuclear receptor peroxisome proliferator-activated receptor β/δ (PPARβ/δ) is a potential pharmacological target due to its role in disease-related biological processes. We used TR-FRET-based competitive ligand binding and coregulator interaction assays to screen 2693 compounds of the Open Chemical Repository of the NCI/NIH Developmental Therapeutics Program for inhibitory PPARβ/δ ligands. One compound,(Z)- ...