Optical control of L-type Ca2+ channels using a diltiazem photoswitch

Timm Fehrentz, Florian M.E. Huber, Nina Hartrampf, Tobias Bruegmann, James A. Frank, Nicholas H.F. Fine, Daniela Malan, Johann G. Danzl, Denis B. Tikhonov, Martin Sumser, Philipp Sasse, David J. Hodson, Boris S. Zhorov, Nikolaj Klöcker, Dirk Trauner

Research output: Contribution to journalArticle

Abstract

L-type Ca2+ channels (LTCCs) play a crucial role in excitation-contraction coupling and release of hormones from secretory cells. They are targets of antihypertensive and antiarrhythmic drugs such as diltiazem. Here, we present a photoswitchable diltiazem, FHU-779, which can be used to reversibly block endogenous LTCCs by light. FHU-779 is as potent as diltiazem and can be used to place pancreatic β-cell function and cardiac activity under optical control.

Original languageEnglish (US)
Pages (from-to)764-767
Number of pages4
JournalNature Chemical Biology
Volume14
Issue number8
DOIs
StatePublished - Aug 1 2018

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ASJC Scopus subject areas

  • Molecular Biology
  • Cell Biology

Cite this

Fehrentz, T., Huber, F. M. E., Hartrampf, N., Bruegmann, T., Frank, J. A., Fine, N. H. F., Malan, D., Danzl, J. G., Tikhonov, D. B., Sumser, M., Sasse, P., Hodson, D. J., Zhorov, B. S., Klöcker, N., & Trauner, D. (2018). Optical control of L-type Ca2+ channels using a diltiazem photoswitch. Nature Chemical Biology, 14(8), 764-767. https://doi.org/10.1038/s41589-018-0090-8