Novel non-ATP competitive small molecules targeting the CK2 α/β interface

Novel non-ATP competitive small molecules targeting the CK2 α/β interface Bioorganic & Medicinal Chemistry 26 (2018) 3016–3020 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc a b b b b Paul Brear , Andrew North , Jessica Iegre , Kathy Hadje Georgiou , Alexandra Lubin , b b b a b, Laura Carro , William Green , Hannah F. Sore , Marko Hyvönen , David R. Spring Department of Biochemistry, University of Cambridge, Sanger Building, 80 Tennis Court Road, Old Addenbrooke’s Site, Cambridge CB2 1GA, UK Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK ARTIC L E I NF O ABSTRAC T Keywords: Increased CK2 levels are prevalent in many cancers. Combined with the critical role CK2 plays in many cell- CK2 signaling pathways, this makes it a prime target for down regulation to fight tumour growth. Herein, we report a Protein-protein interaction fragment-based approach to inhibiting the interaction between CK2α and CK2β at the α-β interface of the −1 Fragment based drug discovery holoenzyme. A fragment, CAM187, with an IC of 44 μM and a molecular weight of only 257 gmol has been identified as the most promising compound. Importantly, the lead fragment only bound at the interface and was http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Bioorganic & Medicinal Chemistry Elsevier

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Publisher
Elsevier
Copyright
Copyright © 2018 The Authors
ISSN
0968-0896
D.O.I.
10.1016/j.bmc.2018.05.011
Publisher site
See Article on Publisher Site

Abstract

Bioorganic & Medicinal Chemistry 26 (2018) 3016–3020 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc a b b b b Paul Brear , Andrew North , Jessica Iegre , Kathy Hadje Georgiou , Alexandra Lubin , b b b a b, Laura Carro , William Green , Hannah F. Sore , Marko Hyvönen , David R. Spring Department of Biochemistry, University of Cambridge, Sanger Building, 80 Tennis Court Road, Old Addenbrooke’s Site, Cambridge CB2 1GA, UK Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK ARTIC L E I NF O ABSTRAC T Keywords: Increased CK2 levels are prevalent in many cancers. Combined with the critical role CK2 plays in many cell- CK2 signaling pathways, this makes it a prime target for down regulation to fight tumour growth. Herein, we report a Protein-protein interaction fragment-based approach to inhibiting the interaction between CK2α and CK2β at the α-β interface of the −1 Fragment based drug discovery holoenzyme. A fragment, CAM187, with an IC of 44 μM and a molecular weight of only 257 gmol has been identified as the most promising compound. Importantly, the lead fragment only bound at the interface and was

Journal

Bioorganic & Medicinal ChemistryElsevier

Published: Jul 15, 2018

References

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