Optical control of L-type Ca2+ channels using a diltiazem photoswitch Journal Article


Author(s): Fehrentz, Timm; Huber, Florian M; Hartrampf, Nina; Bruegmann, Tobias; Frank, James A; Fine, Nicholas H; Malan, Daniela; Danzl, Johann G.; Tikhonov, Denis B; Sumser, Maritn; Sasse, Philipp; Hodson, David J; Zhorov, Boris S; Klocker, Nikolaj; Trauner, Dirk
Article Title: Optical control of L-type Ca2+ channels using a diltiazem photoswitch
Affiliation IST Austria
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.
Journal Title: Nature Chemical Biology
Volume: 14
Issue 8
ISSN: 1552-4469
Publisher: Nature Publishing Group  
Date Published: 2018-07-16
Start Page: 764
End Page: 767
DOI: 10.1038/s41589-018-0090-8
Open access: no