Jump to main content
Jump to site search

Issue 9, 2019
Previous Article Next Article

Lipid-independent control of endothelial and neuronal TRPC3 channels by light

Author affiliations

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.

Graphical abstract: Lipid-independent control of endothelial and neuronal TRPC3 channels by light

Back to tab navigation

Supplementary files

Publication details

The article was received on 11 Dec 2018, accepted on 09 Jan 2019 and first published on 15 Jan 2019


Article type: Edge Article
DOI: 10.1039/C8SC05536J
Citation: Chem. Sci., 2019,10, 2837-2842
  • Open access: Creative Commons BY-NC license
  •   Request permissions

    Lipid-independent control of endothelial and neuronal TRPC3 channels by light

    O. Tiapko, N. Shrestha, S. Lindinger, G. Guedes de la Cruz, A. Graziani, C. Klec, C. Butorac, Wolfgang. F. Graier, H. Kubista, M. Freichel, L. Birnbaumer, C. Romanin, T. Glasnov and K. Groschner, Chem. Sci., 2019, 10, 2837
    DOI: 10.1039/C8SC05536J

    This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material and it is not used for commercial purposes.

    Reproduced material should be attributed as follows:

    • For reproduction of material from NJC:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
    • For reproduction of material from PCCP:
      [Original citation] - Published by the PCCP Owner Societies.
    • For reproduction of material from PPS:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
    • For reproduction of material from all other RSC journals:
      [Original citation] - Published by The Royal Society of Chemistry.

    Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.

Search articles by author

Spotlight

Advertisements