Dosing PPARγ Activation With Light Using Fast Relaxing Photoswitches
Research output: Contribution to journal › Research article › Contributed › peer-review
Contributors
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
| Original language | English |
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| Article number | e7525141 |
| Journal | Angewandte Chemie International Edition |
| Volume | 65 |
| Issue number | 40 |
| Publication status | Published - 28 Sept 2026 |
| Peer-reviewed | Yes |
External IDs
| Scopus | 105047755047 |
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