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

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

Patrik Wolle, Julia Hardick, Shane J. F. Cronin, Julian Engel, Matthias Baumann, Jonas Lategahn, Josef M. Penninger, and Daniel Rauh

Journal of Medicinal Chemistry 2019

DOI: 10.1021/acs.jmedchem.9b00102

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.