Photoswitchable Inhibitor of the Calcium Channel TRPV6.

R. Cunha, Micael; Bhardwaj, Rajesh; Lindinger, Sonja; Butorac, Carmen; Romanin, Christoph; Hediger, Matthias; Reymond, Jean-Louis (2019). Photoswitchable Inhibitor of the Calcium Channel TRPV6. ACS medicinal chemistry letters, 10(9), pp. 1341-1345. American Chemical Society 10.1021/acsmedchemlett.9b00298

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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.

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