Keck, Maximilian and Hermann, Christian and Luetzel, Kyra and Gudermann, Thomas and Konrad, David B. and Mederos y Schnitzler, Michael and Storch, Ursula (2024) Photoswitchable TRPC6 channel activators evoke distinct channel kinetics reflecting different gating behaviors. ISCIENCE, 27 (10): 111008. ISSN 2589-0042
Full text not available from this repository. (Request a copy)Abstract
The non-selective transient receptor potential canonical6 6 (TRPC6) cation channels have several physiological and pathophysiological effects. They are activated by the lipid second messenger diacylglycerol (DAG) and by non-lipidic compounds such as GSK 1702934A (GSK). Advances in photopharmacology led to the development of photoswitchable activators such as PhoDAG, OptoDArG, and OptoBI-1 that can be switched ON and OFF with the spatiotemporal precision of light. We aimed to elucidate whether these photopharmaceuticals allow for a reliable determination of the ion channel current kinetics. We performed electrophysiological whole-cell measurements in the overexpression system and analyzed TRPC6 currents induced by photoswitching. We observed distinct activation, deactivation and inactivation current kinetics suggesting that each photoswitchable activator elicits a distinct active channel state. Notably, the current kinetics strongly depended on the intensity of the light source. Altogether, photo- pharmaceuticals are advantageous for an extended biophysical characterization of whole-cell currents and provide insight into their gating mechanism.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ENABLE OPTICAL CONTROL; CATION CHANNEL; DIACYLGLYCEROL; REVEALS; Photoswitchable activators; enable precise; kinetics; prerequisites; essential; Each photoswitchable; behavior |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Group Clinical Pharmacy (Dr. Dorn) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 14 Jan 2026 08:04 |
| Last Modified: | 14 Jan 2026 08:04 |
| URI: | https://pred.uni-regensburg.de/id/eprint/64324 |
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