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Título : Lipid-independent control of endothelial and neuronal TRPC3 channels by light
Autor : Tiapko, Oleksandra 
Shrestha, Niroj 
Lindinger, Sonja 
Guedes de la Cruz, Gema 
Graziani, Annarita 
Klec, Christiane 
Butorac, Carmen 
Graier, Wolfgang F. 
Kubista, Helmut 
Freichel, Marc 
Birnbaumer, Lutz 
Romanin, Christoph 
Glasnov, Toma 
Groschner, Klaus 
Fecha de publicación : 2019
Editorial : Royal Society of Chemistry
Cita : Tiapko O, Shrestha N, Lindinger S, et al. Lipid-independent control of endothelial and neuronal TRPC3 channels by light [en línea]. Chemical Science. 2019;10(9):2837-2842. doi:10.1039/C8SC05536J Disponible en:
Resumen : Abstract: Lipid-gated TRPC channels are highly expressed in cardiovascular and neuronal tissues. Exerting precise pharmacological control over their activity in native cells is expected to serve as a basis for the development of novel therapies. Here we report on a new photopharmacological tool that enables manipulation of TRPC3 channels by light, in a manner independent of lipid metabolism and with higher temporal precision than lipid photopharmacology. Using the azobenzene photoswitch moiety, we modified GSK1702934A to generate light-controlled TRPC agonists. We obtained one light-sensitive molecule (OptoBI-1) that allows us to exert efficient, light-mediated control over TRPC3 activity and the associated cellular Ca2+ signaling. OptoBI-1 enabled high-precision, temporal control of TRPC3-linked cell functions such as neuronal firing and endothelial Ca2+ transients. With these findings, we introduce a novel photopharmacological strategy to control native TRPC conductances.
ISSN : 2041-6520
Disciplina: MEDICINA
DOI: 10.1039/c8sc05536j
Derechos: Acceso Abierto
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