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

doi:10.1038/s41589-018-0090-8

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

Chemistry

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	764-767
Number of pages	4
Journal	Nature Chemical Biology
Volume	14
Issue number	8
DOIs	https://doi.org/10.1038/s41589-018-0090-8
State	Published - Aug 1 2018

ASJC Scopus subject areas

Molecular Biology
Cell Biology

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10.1038/s41589-018-0090-8

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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

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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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AU - Fehrentz, Timm

AU - Huber, Florian M.E.

AU - Hartrampf, Nina

AU - Bruegmann, Tobias

AU - Frank, James A.

AU - Fine, Nicholas H.F.

AU - Malan, Daniela

AU - Danzl, Johann G.

AU - Tikhonov, Denis B.

AU - Sumser, Martin

AU - Sasse, Philipp

AU - Hodson, David J.

AU - Zhorov, Boris S.

AU - Klöcker, Nikolaj

AU - Trauner, Dirk

PY - 2018/8/1

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

Abstract

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