Work

Photoswitchable Inhibitor of the Calcium Channel TRPV6

Year: 2019

Type: article

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, IC 50 ≫ 10 μM) and a potent inhibitor as the Z -diazo stereoisomer accessible reversibly by UV irradiation at λ = 365 nm ( Z/E = 3:1, IC 50 = 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.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.9b00298

Authors: Micael R. Cunha, Rajesh Bhardwaj, Sonja Lindinger, Carmen Butorac, Christoph Romanin, Matthias A. Hediger, Jean-Louis Reymond

Institutions: University of Bern, University Hospital of Bern, Johannes Kepler University of Linz

Language: English

Topic: Ion Channels and Receptors

Subfield: Sensory Systems

Field: Neuroscience

Domain: Life Sciences

Open Access status: green

Funder: Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung

OpenAlex ID: W2964882182

FWCI: 1.563

Cites: 31

Cited by: 21

Related to: 10