Shifting the selectivity of pyridopyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily
M. Rak, R. Tesch, L. M. Berger, E. Shevchenko, M. Raab, A. Tjaden, R. Zhubi, D.-I. Balourdas, A. C. Joerger, A. Poso, A. Kraemer, L. Elson, A. Lucic, T. Kronenberger, T. Hanke, , S. Knapp
This paper develops a selective SIK kinase inhibitor, MR22, by optimizing a pyrido[2,3-d]pyrimidin-7(8H)-one scaffold to eliminate PAK activity, demonstrating its efficacy in ovarian cancer cells.
bioRxiv · Mar 24, 2023Biochemistry