Optical control of L-type Ca 2+ channels using a diltiazem photoswitch

Nat Chem Biol. 2018 Aug;14(8):764-767. doi: 10.1038/s41589-018-0090-8. Epub 2018 Jul 16.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium Channels, L-Type / chemistry
  • Calcium Channels, L-Type / metabolism*
  • Diltiazem / chemistry
  • Diltiazem / pharmacology*
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Heart / drug effects*
  • Humans
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / metabolism
  • Light
  • Optical Imaging*
  • Photochemical Processes

Substances

  • Calcium Channels, L-Type
  • Fluorescent Dyes
  • Diltiazem