In depth analysis of kinase cross screening data to identify CAMKK2 inhibitory scaffolds
S. O'Byrne, J. W. Scott, J. R. Pilotte, A. d. S. Santiago, C. G. Langendorf, J. S. Oakhill, B. J. Eduful, R. M. Counago, C. I. Wells, W. Zuercher, T. Willson, D. H. Drewry
Abstract
The calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) plays a central role in many cell signaling pathways. CAMKK2 activates CAMK1, CAMK4, AMPK, and AKT leading to numerous physiological responses. Deregulation of CAMKK2 is linked to several diseases, suggesting utility of CAMKK2 inhibitors for oncological, metabolic and inflammatory indications. In this work we review the role of CAMKK2 in biology and disease. Through analysis of literature and public databases we have identified starting points for CAMKK2 inhibitor medicinal chemistry campaigns. These starting points provide an opportunity for the development of selective CAMKK2 inhibitors and will lead to tools that delineate the roles of this kinase in disease biology.
02 /Specification & Classification
Click any tag to browse matching papers- Approach
Reproducibility ledger
Nobody has reported trying to reproduce this paper yet. Did you replicate an experiment or run the code? Your report saves the next lab a week.
Sign in to file a reproducibility report.
Related papers
- Structural and binding studies of human CAMKK2 kinase domain bound to small molecule ligands
Gerson S. Profeta, Caio V. dos Reis, … Rafael M. Couñago·bioRxiv·Feb 1, 2019
- SGC-CAMKK2-1: A chemical probe for CAMKK2
C. I. Wells, Y. Liang, … D. H. Drewry·CellsPeer-reviewed·Jan 11, 2023
- Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors
A. d. S. Santiago, R. M. Counago, … J. Elkins·bioRxiv·Mar 31, 2018
- Unconventional binding of Calmodulin to CHK2 kinase inhibits catalytic activity
Christopher R. Horne, Tingting Wang, … James M. Murphy·Biochemical JournalPeer-reviewed·Sep 26, 2025
- Optimization of pyrazolopyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor
A. Kraemer, C. G. Kurz, … T. Hanke·bioRxiv·Jun 27, 2020
- Simultaneous loss of CAMK2A and CAMK2B reveals endogenous in vivo substrates
Pomme M.F. Rigter, Karel Bezstarosti, … Geeske M. van Woerden·bioRxiv·Nov 17, 2024