Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation

Ines H. Kaltheuner; Kanchan Anand; Jonas Moecking; Robert Düster; Jinhua Wang; Nathanael S. Gray; Matthias Geyer

doi:10.1038/s41467-021-26935-z

Nature Communications (Nov 2021)

Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation

Ines H. Kaltheuner,
Kanchan Anand,
Jonas Moecking,
Robert Düster,
Jinhua Wang,
Nathanael S. Gray,
Matthias Geyer

Affiliations

Ines H. Kaltheuner: Institute of Structural Biology, University of Bonn
Kanchan Anand: Institute of Structural Biology, University of Bonn
Jonas Moecking: Institute of Structural Biology, University of Bonn
Robert Düster: Institute of Structural Biology, University of Bonn
Jinhua Wang: Department of Cancer Biology, Dana-Farber Cancer Institute
Nathanael S. Gray: Department of Chemical and Systems Biology, Chem-H and the Stanford Cancer Institute, Stanford School of Medicine, Stanford University
Matthias Geyer: Institute of Structural Biology, University of Bonn

DOI: https://doi.org/10.1038/s41467-021-26935-z
Journal volume & issue: Vol. 12, no. 1
pp. 1 – 15

Abstract

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Abemaciclib is a third generation CDK-directed drug used in the treatment of HR + /HER2 negative advanced or metastatic breast cancer. Here the authors demonstrate that members of the Homeodomain-interacting protein kinases (HIPKs) HIPK3 and DYRK1A are also targeted by Abemaciclib.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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