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J Med Chem. 2019 Mar 14;62(5):2843-2848. doi: 10.1021/acs.jmedchem.9b00102. Epub 2019 Feb 21.

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.

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Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany.
Drug Discovery Hub Dortmund (DDHD) am Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Institute of Molecular Biotechnology, Austrian Academy of Sciences , Dr. Bohr Gasse 3 , AT-1030 Vienna , Austria.
Lead Discovery Center GmbH , Otto-Hahn-Strasse 15 , 44227 Dortmund , Germany.


The protein kinase MKK7 is linked to neuronal development and the onset of cancer. The field, however, lacks high-quality functional probes that would allow for the dissection of its detailed functions. Against this background, we describe an effective covalent inhibitor of MKK7 based on the pyrazolopyrimidine scaffold.

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