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

Timm Fehrentz; Florian  Huber; Nina Hartrampf; Tobias Bruegmann; James Frank; Nicholas Fine; Daniela Malan; Johann Danzl; Denis Tikhonov; Martin Sumser; Philipp Sasse; David Hodson; Boris Zhorov; Klocker Nikolaj; Dirk Trauner

doi:10.1038/s41589-018-0090-8

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

Timm Fehrentz
, Florian Huber
, Nina Hartrampf
, Tobias Bruegmann
, James Frank
, Nicholas Fine
, Daniela Malan
, Johann Danzl
, Denis Tikhonov
, Martin Sumser
, Philipp Sasse
, David Hodson
, Boris Zhorov
, Klocker Nikolaj
, Dirk Trauner

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

16 Citations (Scopus)

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Abstract

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

Original language	English
Pages (from-to)	764-767
Journal	Nature Chemical Biology
Volume	14
DOIs	https://doi.org/10.1038/s41589-018-0090-8
Publication status	Published - 16 Jul 2018

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Fehrentz_et_al_Optical_Control_Nature_Chemical_Biology_2018
Published in Nature Chemical Biology on 16/06/2018 DOI: 10.1038/s41589-018-0090-8
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Cite this

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title = "Optical control of L-Type Ca2+ channels using a diltiazem photoswitch",

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

author = "Timm Fehrentz and Florian Huber and Nina Hartrampf and Tobias Bruegmann and James Frank and Nicholas Fine and Daniela Malan and Johann Danzl and Denis Tikhonov and Martin Sumser and Philipp Sasse and David Hodson and Boris Zhorov and Klocker Nikolaj and Dirk Trauner",

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T1 - Optical control of L-Type Ca2+ channels using a diltiazem photoswitch

AU - Fehrentz, Timm

AU - Huber, Florian

AU - Hartrampf, Nina

AU - Bruegmann, Tobias

AU - Frank, James

AU - Fine, Nicholas

AU - Malan, Daniela

AU - Danzl, Johann

AU - Tikhonov, Denis

AU - Sumser, Martin

AU - Sasse, Philipp

AU - Hodson, David

AU - Zhorov, Boris

AU - Nikolaj, Klocker

AU - Trauner, Dirk

PY - 2018/7/16

Y1 - 2018/7/16

N2 - L-type Ca2+ channels (LTCCs) play a crucial role in excitation-contraction coupling and the release of hormones from secretory cells. They are targets of numerous antihypertensive and antiarrhythmic drugs such as diltiazem. Here, we present a photoswitchable derivative of diltiazem, FHU-779, which can be used to reversibly block endogenous LTCCs by light. FHU-779 is almost as potent as diltiazem itself, and can be used to place pancreatic b cell function and cardiac activity under optical control.

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

U2 - 10.1038/s41589-018-0090-8

DO - 10.1038/s41589-018-0090-8

M3 - Article

SN - 1552-4450

VL - 14

SP - 764

EP - 767

JO - Nature Chemical Biology

JF - Nature Chemical Biology

ER -

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

Abstract

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