Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ(PPARγ)

Konstantin Hinnah, Sabine Willems, Johannes Morstein, Jan Heering, Felix W.W. Hartrampf, Johannes Broichhagen, Philipp Leippe, Daniel Merk, Dirk Trauner

Research output: Contribution to journalArticlepeer-review


Photopharmacology aims at the optical control of protein activity using synthetic photoswitches. This approach has been recently expanded to nuclear hormone receptors with the introduction of "photohormones"for the retinoic acid receptor, farnesoid X receptor, and estrogen receptor. Herein, we report the development and profiling of photoswitchable agonists for peroxisome proliferator-activated receptor γ(PPARγ). Based on known PPARγligands (MDG548, GW1929, and rosiglitazone), we have designed and synthesized azobenzene derivatives, termed AzoGW1929 and AzoRosi, which were confirmed to be active in cell-based assays. Subsequent computer-aided optimization of AzoRosi resulted in the photohormone AzoRosi-4, which bound and activated PPARγpreferentially in its light-activated cis-configuration.

Original languageEnglish (US)
Pages (from-to)10908-10920
Number of pages13
JournalJournal of Medicinal Chemistry
Issue number19
StatePublished - Oct 8 2020

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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