Journal article

In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.

Sean N O'Byrne, John W Scott, Joseph R Pilotte, André da S Santiago, Christopher G Langendorf, Jonathan S Oakhill, Benjamin J Eduful, Rafael M Couñago, Carrow I Wells, William J Zuercher, Timothy M Willson, David H Drewry

Molecules | Published : 2020


The calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) activates CAMK1, CAMK4, AMPK, and AKT, leading to numerous physiological responses. The deregulation of CAMKK2 is linked to several diseases, suggesting the utility of CAMKK2 inhibitors for oncological, metabolic and inflammatory indications. In this work, we demonstrate that STO-609, frequently described as a selective inhibitor for CAMKK2, potently inhibits a significant number of other kinases. Through an analysis of literature and public databases, we have identified other potent CAMKK2 inhibitors and verified their activities in differential scanning fluorimetry and enzyme inhibition assays. These inhibitors are potential..

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