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

Fehrentz, Timm; Huber, Florian M. E.; Hartrampf, Nina; Bruegmann, Tobias; Frank, James A.; Fine, Nicholas H. F.; Malan, Daniela; Danzl, Johann G.; Tikhonov, Denis B.; Sumser, Martin; Sasse, Philipp; Hodson, David J.; Zhorov, Boris S.; Klocker, Nikolaj and Trauner, Dirk (2018): Optical control of L-type Ca2+ channels using a diltiazem photoswitch. In: Nature Chemical Biology, Vol. 14, No. 8: pp. 764-767

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 beta-cell function and cardiac activity under optical control.

• Item Type: Journal article
• Faculties: Chemistry and Pharmacy > Department of Chemistry
• Research Centers: Center for Integrated Protein Science Munich (CIPSM)
• Subjects: 500 Science > 540 Chemistry
• ISSN: 1552-4450
• Language: English