Photoswitchable Inhibitor of the Calcium Channel TRPV6
Posted on 2019-08-07 - 21:29
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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Cunha, Micael
R.; Bhardwaj, Rajesh; Lindinger, Sonja; Butorac, Carmen; Romanin, Christoph; A. Hediger, Matthias; et al. (2019). Photoswitchable Inhibitor of the Calcium Channel TRPV6. ACS Publications. Collection. https://doi.org/10.1021/acsmedchemlett.9b00298
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AUTHORS (7)
MC
Micael
R. Cunha
RB
Rajesh Bhardwaj
SL
Sonja Lindinger
CB
Carmen Butorac
CR
Christoph Romanin
MA
Matthias A. Hediger
JR
Jean-Louis Reymond