{Reference Type}: Journal Article
{Title}: Azologs of the Fatty Acid Mimetic Drug Cinalukast Enable Light-Induced PPARα Activation.
{Author}: Sai M;van Herwijnen N;Merk D;
{Journal}: ChemMedChem
{Volume}: 0
{Issue}: 0
{Year}: 2024 Jun 19
{Factor}: 3.54
{DOI}: 10.1002/cmdc.202400327
{Abstract}: Photo-switchable nuclear receptor modulators ("photohormones") enable spatial and temporal control over transcription factor activity and are valuable precision tools for biological studies. We have developed a new photohormone chemotype by incorporating a light-switchable motif in the scaffold of a cinalukast-derived PPARα ligand and tuned light-controlled activity by systematic structural variation. An optimized photohormone exhibited PPARα agonism in its light-induced (Z)-configuration and strong selectivity over related lipid-activated transcription factors representing a valuable addition to the collection of light-controlled tools to study nuclear receptor activity.