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

Research output: Contribution to journalArticle

Authors

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

Colleges, School and Institutes

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.

Details

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