Strategy for Lead Identification for Understudied Kinases


In our manuscript we outline an approach in which we convert a promiscuous pyrimidine scaffold into narrowly selective, cell-active chemical leads for several understudied kinases, including DRAK1, BMP2K, and MARK4. These chemical tools will allow illumination of the function(s) of these poorly characterized kinases for the first time. Several of the understudied kinases that we inhibit with our pyrimidine-based compounds are also implicated in neurodegenerative disease, pushing the utility of kinase inhibitors outside of the oncology space and offering opportunities for the validation of therapeutic hypotheses attributed to these kinases.


Supplementary material

ChemRxiv pyrimidine SI