Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.

Abstract

A structure-activity relationship has been developed around the meridianin scaffold for inhibition of Dyrk1a. The compounds have been focussed on the inhibition of kinase Dyrk1a, as a means to retain the transcription factor NFAT in the nucleus. NFAT is responsible for up-regulation of genes responsible for the induction of a slow, oxidative skeletal muscle… (More)
DOI: 10.1016/j.bmcl.2017.03.037

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Cite this paper

@article{Shaw2017DevelopingDI, title={Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.}, author={Simon J. Shaw and Dane A. Goff and Nan Lin and Rajinder Jit Singh and Wei Li and John R McLaughlin and Kristen A. Baltgalvis and Donald G. Payan and Todd M. Kinsella}, journal={Bioorganic & medicinal chemistry letters}, year={2017}, volume={27 11}, pages={2617-2621} }