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

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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.

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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., Fine, N. H. F., ... Trauner, D. (Accepted/In press). Optical control of L-type Ca2+ channels using a diltiazem photoswitch. Nature Chemical Biology, 1-4. https://doi.org/10.1038/s41589-018-0090-8