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Design, Synthesis and Inhibitory Activity of Photoswitchable RET Kinase Inhibitors.

Journal article
Authors Rubén Ferreira
Jesper Nilsson
Carlos Solano
Joakim Andréasson
Morten Grøtli
Published in Scientific reports
Volume 5
Pages artikel nr 9769
ISSN 2045-2322
Publication year 2015
Published at Department of Chemistry and Molecular Biology
Pages artikel nr 9769
Language en
Links dx.doi.org/10.1038/srep09769
https://gup.ub.gu.se/file/203305
Subject categories Chemical Sciences

Abstract

REarranged during Transfection (RET) is a transmembrane receptor tyrosine kinase required for normal development and maintenance of neurons of the central and peripheral nervous systems. Deregulation of RET and hyperactivity of the RET kinase is intimately connected to several types of human cancers, most notably thyroid cancers, making it an attractive therapeutic target for small-molecule kinase inhibitors. Novel approaches, allowing external control of the activity of RET, would be key additions to the signal transduction toolbox. In this work, photoswitchable RET kinase inhibitors based on azo-functionalized pyrazolopyrimidines were developed, enabling photonic control of RET activity. The most promising compound displays excellent switching properties and stability with good inhibitory effect towards RET in cell-free as well as live-cell assays and a significant difference in inhibitory activity between its two photoisomeric forms. As the first reported photoswitchable small-molecule kinase inhibitor, we consider the herein presented effector to be a significant step forward in the development of tools for kinase signal transduction studies with spatiotemporal control over inhibitor concentration in situ.

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