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ACS Med Chem Lett. 2019 Aug 2;10(9):1341-1345. doi: 10.1021/acsmedchemlett.9b00298. eCollection 2019 Sep 12.

Photoswitchable Inhibitor of the Calcium Channel TRPV6.

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Department of Chemistry and Biochemistry, NCCR TransCure, University of Bern, Freiestrasse 3, 3012 Bern, Switzerland.
Institute of Biochemistry and Molecular Medicine, NCCR TransCure, University of Bern, Bühlstrasse 28, 3012 Bern, Switzerland & Department of Nephrology and Hypertension, University Hospital Bern, Inselspital, 3010 Bern, Switzerland.
Institute of Biophysics, Johannes Kepler University Linz, Gruberstrasse 40, 4020 Linz, Austria.


Herein we report the first photoswitchable inhibitor of Transient Receptor Potential Vanilloid 6 (TRPV6), a selective calcium channel involved in a number of diseases and in cancer progression. By surveying analogs of a previously reported TRPV6 inhibitor appended with a phenyl-diazo group, we identified a compound switching between a weak TRPV6 inhibitor in its dark, E-diazo stereoisomer (Z/E = 3:97, IC50 ≫ 10 μM) and a potent inhibitor as the Z-diazo stereoisomer accessible reversibly by UV irradiation at λ = 365 nm (Z/E = 3:1, IC50 = 1.7 ± 0.4 μM), thereby allowing precise spatiotemporal control of inhibition. This new tool compound should be useful to deepen our understanding of TRPV6.

[Available on 2020-09-12]

Conflict of interest statement

The authors declare no competing financial interest.

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