Abstract
The non-selective transient receptor potential canonical 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, photopharmaceuticals are advantageous for an extended biophysical characterization of whole-cell currents and provide insight into their gating mechanism.
| Item Type: | Journal article |
|---|---|
| Form of publication: | Publisher's Version |
| Faculties: | Medicine > Walther Straub Institute of Pharmacology and toxicology |
| Subjects: | 600 Technology > 610 Medicine and health |
| URN: | urn:nbn:de:bvb:19-epub-133780-5 |
| ISSN: | 2589-0042 |
| Language: | English |
| Item ID: | 133780 |
| Date Deposited: | 30. Mar 2026 13:39 |
| Last Modified: | 30. Mar 2026 13:39 |
| DFG: | Gefördert durch die Deutsche Forschungsgemeinschaft (DFG) - 239283807 |
| DFG: | Gefördert durch die Deutsche Forschungsgemeinschaft (DFG) - 491502892 |
| DFG: | Gefördert durch die Deutsche Forschungsgemeinschaft (DFG) - 503157935 |
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