Optical control of L-type Ca 2+ channels using a diltiazem photoswitch

Nature chemical biology(2018)

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摘要
L-type Ca 2+ 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.
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关键词
Cardiovascular diseases,Chemical biology,Ion channels,Chemistry/Food Science,general,Biochemical Engineering,Biochemistry,Cell Biology,Bioorganic Chemistry
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