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ID: ALA4304815
Journal: ACS Med Chem Lett
Title: Photoswitchable Inhibitor of the Calcium Channel TRPV6.
Authors: Cunha MR, Bhardwaj R, Lindinger S, Butorac C, Romanin C, Hediger MA, Reymond JL.
Abstract: 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.
CiteXplore: 31531207