Photoswitchable Inhibitor of the Calcium Channel TRPV6.
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ABSTRACT:
SUBMITTER: Cunha MR
PROVIDER: S-EPMC6746075 | biostudies-literature | 2019 Sep
REPOSITORIES: biostudies-literature
Publications
Photoswitchable Inhibitor of the Calcium Channel TRPV6.
Cunha Micael R MR Bhardwaj Rajesh R Lindinger Sonja S Butorac Carmen C Romanin Christoph C Hediger Matthias A MA Reymond Jean-Louis JL
ACS medicinal chemistry letters 20190802 9
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, <i>E</i>-diazo stereoisomer (<i>Z/E</i> = 3:97, IC<sub>50</sub> ≫ 10 μM) and a potent inhibitor as the <i>Z</i>-diazo stereoisome ...[more]
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