Azologs of the Fatty Acid Mimetic Drug Cinalukast Enable Light‐Induced PPARα Activation

Sai, Minh; Herwijnen, Niels van und Merk, Daniel (2024): Azologs of the Fatty Acid Mimetic Drug Cinalukast Enable Light‐Induced PPARα Activation. In: ChemMedChem

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.

• Dokumententyp: Zeitschriftenartikel
• Fakultät: Chemie und Pharmazie > Department für Pharmazie - Zentrum für Pharmaforschung
• Themengebiete: 500 Naturwissenschaften und Mathematik > 540 Chemie ; 600 Technik, Medizin, angewandte Wissenschaften > 610 Medizin und Gesundheit
• ISSN: 1860-7179
• Sprache: Englisch