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 und Trauner, Dirk (2018): Optical control of L-type Ca2+ channels using a diltiazem photoswitch. In: Nature Chemical Biology, Bd. 14, Nr. 8: S. 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.

• Dokumententyp: Zeitschriftenartikel
• Fakultät: Chemie und Pharmazie > Department Chemie
• Fakultätsübergreifende Einrichtungen: Center for Integrated Protein Science Munich (CIPSM)
• Themengebiete: 500 Naturwissenschaften und Mathematik > 540 Chemie
• ISSN: 1552-4450
• Sprache: Englisch