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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,… Click to show full 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.A photoswitchable probe to control Ca2+ influx through L-type Ca2+ channels is useful in pancreatic β cells and can be employed to modulate beating rate in explanted hearts.
Journal Title: Nature Chemical Biology
Year Published: 2018
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