Abstract
L-type Ca2+ channels (LTCCs) play a crucial role in excitation-contraction coupling
and the release of hormones from secretory cells. They are targets of numerous
antihypertensive and antiarrhythmic drugs such as diltiazem. Here, we present a
photoswitchable derivative of diltiazem, FHU-779, which can be used to reversibly
block endogenous LTCCs by light. FHU-779 is almost as potent as diltiazem itself,
and can be used to place pancreatic b cell function and cardiac activity under optical control.
and the release of hormones from secretory cells. They are targets of numerous
antihypertensive and antiarrhythmic drugs such as diltiazem. Here, we present a
photoswitchable derivative of diltiazem, FHU-779, which can be used to reversibly
block endogenous LTCCs by light. FHU-779 is almost as potent as diltiazem itself,
and can be used to place pancreatic b cell function and cardiac activity under optical control.
Original language | English |
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Pages (from-to) | 764-767 |
Journal | Nature Chemical Biology |
Volume | 14 |
DOIs | |
Publication status | Published - 16 Jul 2018 |