Optical control of L-type Ca2+ channels using a diltiazem photoswitch Journal Articles uri icon

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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.

authors

  • Fehrentz, Timm
  • Huber, Florian ME
  • Hartrampf, Nina
  • Bruegmann, Tobias
  • Frank, James A
  • Fine, Nicholas HF
  • Malan, Daniela
  • Danzl, Johann G
  • Tikhonov, Denis B
  • Sumser, Martin
  • Sasse, Philipp
  • Hodson, David J
  • Zhorov, Boris
  • Klöcker, Nikolaj
  • Trauner, Dirk

publication date

  • August 2018