Optical Control of TRPV1 Channels

Authors

  • M. Sc. Marco Stein,

    1. Department of Chemistry, Ludwig-Maximilians-University (LMU), Munich and Center of Integrated Protein Science, Butenandtstrasse 5–13, 81377 Munich (Germany)
    Search for more papers by this author
  • Dr. Andreas Breit,

    1. Walther-Straub-Institute for Pharmacology and Toxicology, LMU Munich, Goethestrasse 33, 80336 Munich (Germany)
    Search for more papers by this author
  • Dr. Timm Fehrentz,

    1. Department of Chemistry, Ludwig-Maximilians-University (LMU), Munich and Center of Integrated Protein Science, Butenandtstrasse 5–13, 81377 Munich (Germany)
    Search for more papers by this author
  • Prof. Thomas Gudermann,

    1. Walther-Straub-Institute for Pharmacology and Toxicology, LMU Munich, Goethestrasse 33, 80336 Munich (Germany)
    Search for more papers by this author
  • Prof. Dirk Trauner

    Corresponding author
    1. Department of Chemistry, Ludwig-Maximilians-University (LMU), Munich and Center of Integrated Protein Science, Butenandtstrasse 5–13, 81377 Munich (Germany)
    • Department of Chemistry, Ludwig-Maximilians-University (LMU), Munich and Center of Integrated Protein Science, Butenandtstrasse 5–13, 81377 Munich (Germany)
    Search for more papers by this author

  • We thank Dr. Peter Mayer (LMU Munich) for the determination of the X-ray structure and Dr. Martin Sumser (LMU Munich) for many helpful discussions. This work was supported by the European Science Foundation (ERC grant no. 268795 to D.T.) and the Fonds der Chemischen Industrie (PhD fellowship to M.S.).

Abstract

original image

Controlling pain with light: TRPV1 channels mediate the response to noxious heat and can be activated by capsaicin, the major ingredient of chili pepper. Novel azobenzene photoswitches can be used for the optical control of TRPV1. One of these compounds antagonizes capsaicin in a light-dependent fashion, demonstrating that a photoswitchable antagonist and an agonist can be applied in concert to modulate ion channel activity.

Ancillary