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Updated: Aug 7, 2026

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
Published on: March 10, 2020
Studies towards the conception of new selective PPARbeta/delta ligands
Carine Ekambomé Basséne1, Franck Suzenet, Nathalie Hennuyer
1Institut de Chimie Organique et Analytique (ICOA), UMR-CNRS 6005, FR CNRS 2708, Université d'Orléans, France.
Abstract:
In order to define new PPARbeta/delta ligands, SAR study on the selective PPARbeta/delta activator L-165,041 led to the identification of one key functional group for selective PPARbeta/delta activation. Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARbeta/delta ligand GW501516, the conception of new ligands showing good affinity for PPARbeta/delta is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPARbeta/delta subtype selectivity.
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