Dosing PPARγ Activation With Light Using Fast Relaxing Photoswitches
Publikation: Beitrag in Fachzeitschrift › Forschungsartikel › Beigetragen › Begutachtung
Beitragende
Abstract
The transcription factor PPARγ regulates glucose and lipid homeostasis, and its activation, e.g., with glitazones, has antidiabetic, insulin-sensitizing activity, but also adverse effects which possibly arise from overstimulation. Here we developed a novel high-precision tool to enable light-dosed PPARγ activation. Structure-guided incorporation of a photoswitchable diazene motif into a PPARγ ligand and molecular fine-tuning provided potent, light-activated PPARγ agonists with millisecond to multiple-hour half-lives, suitable for biological research applications. Phenotypic effects of light-dosed PPARγ activation in an in vitro model of adipogenesis suggested time-dependent importance of the receptor in adipocyte development and illustrated the unprecedented precision of controlling PPARγ activity with light-activated chemical tools.
Details
| Originalsprache | Englisch |
|---|---|
| Aufsatznummer | e7525141 |
| Fachzeitschrift | Angewandte Chemie International Edition |
| Jahrgang | 65 |
| Ausgabenummer | 40 |
| Publikationsstatus | Veröffentlicht - 28 Sept. 2026 |
| Peer-Review-Status | Ja |
Externe IDs
| Scopus | 105047755047 |
|---|