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Open AccessArticle

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

Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
St Vincent’s Institute and Department of Medicine, The University of Melbourne, 41 Victoria Parade, Fitzroy 3065, Australia
Mary MacKillop Institute for Health Research, Australian Catholic University, 215 Spring Street, Melbourne 3000, Australia
The Florey Institute of Neuroscience and Mental Health, 30 Royal Parade, Parkville 3052, Australia
Centro de Química Medicinal (CQMED), Centro de Biologia Molecular e Engenharia Genética (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas SP 13083-875, Brazil
Structural Genomics Consortium, Departamento de Genética e Evolução, Instituto de Biologia, UNICAMP, Campinas SP 13083-886, Brazil
Author to whom correspondence should be addressed.
Molecules 2020, 25(2), 325;
Received: 19 December 2019 / Revised: 7 January 2020 / Accepted: 8 January 2020 / Published: 13 January 2020
(This article belongs to the Special Issue Design, Synthesis, and Biological Evaluation of Enzyme Inhibitors)
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 starting points for the development of selective CAMKK2 inhibitors and will lead to tools that delineate the roles of this kinase in disease biology. View Full-Text
Keywords: kinase; CAMKK2; STO-609; chemical probes; oncology; kinase inhibitors kinase; CAMKK2; STO-609; chemical probes; oncology; kinase inhibitors
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O’Byrne, S.N.; Scott, J.W.; Pilotte, J.R.; Santiago, A.S.; Langendorf, C.G.; Oakhill, J.S.; Eduful, B.J.; Couñago, R.M.; Wells, C.I.; Zuercher, W.J.; Willson, T.M.; Drewry, D.H. In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds. Molecules 2020, 25, 325.

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