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Review

Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study

1
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
2
Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge CB2 1GA, UK
*
Author to whom correspondence should be addressed.
Academic Editor: Péter Kele
Molecules 2021, 26(7), 1977; https://doi.org/10.3390/molecules26071977
Received: 25 February 2021 / Revised: 22 March 2021 / Accepted: 25 March 2021 / Published: 31 March 2021
(This article belongs to the Special Issue Chemical Probe Synthesis and Applications in Chemical Biology)
Protein kinases are a large class of enzymes with numerous biological roles and many have been implicated in a vast array of diseases, including cancer and the novel coronavirus infection COVID-19. Thus, the development of chemical probes to selectively target each kinase is of great interest. Inhibition of protein kinases with ATP-competitive inhibitors has historically been the most widely used method. However, due to the highly conserved structures of ATP-sites, the identification of truly selective chemical probes is challenging. In this review, we use the Ser/Thr kinase CK2 as an example to highlight the historical challenges in effective and selective chemical probe development, alongside recent advances in the field and alternative strategies aiming to overcome these problems. The methods utilised for CK2 can be applied to an array of protein kinases to aid in the discovery of chemical probes to further understand each kinase’s biology, with wide-reaching implications for drug development. View Full-Text
Keywords: kinase; CK2; inhibitor; cancer; molecular probe; ATP-site; COVID-19 kinase; CK2; inhibitor; cancer; molecular probe; ATP-site; COVID-19
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MDPI and ACS Style

Atkinson, E.L.; Iegre, J.; Brear, P.D.; Zhabina, E.A.; Hyvönen, M.; Spring, D.R. Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study. Molecules 2021, 26, 1977. https://doi.org/10.3390/molecules26071977

AMA Style

Atkinson EL, Iegre J, Brear PD, Zhabina EA, Hyvönen M, Spring DR. Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study. Molecules. 2021; 26(7):1977. https://doi.org/10.3390/molecules26071977

Chicago/Turabian Style

Atkinson, Eleanor L., Jessica Iegre, Paul D. Brear, Elizabeth A. Zhabina, Marko Hyvönen, and David R. Spring 2021. "Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study" Molecules 26, no. 7: 1977. https://doi.org/10.3390/molecules26071977

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