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 journalArticlepeer-review

16 Citations (Scopus)
412 Downloads (Pure)

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 languageEnglish
Pages (from-to)764-767
JournalNature Chemical Biology
Volume14
DOIs
Publication statusPublished - 16 Jul 2018

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