Development of small cyclic peptides targeting the CK2α/β interface

Eleanor L. Atkinson; Jessica Iegre; Claudio D’Amore; Paul Brear; Mauro Salvi; Marko Hyvönen; David R. Spring

doi:10.1039/D2CC00707J

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Development of small cyclic peptides targeting the CK2α/β interface†

Eleanor L. Atkinson,

^a Jessica Iegre,

^a Claudio D’Amore,^b Paul Brear,

^c Mauro Salvi,

*^b Marko Hyvönen

*^c and David R. Spring

*^a

Author affiliations

* Corresponding authors

^a Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UK
E-mail: spring@ch.cam.ac.uk

^b Department of Biomedical Sciences, University of Padova, Padova, Italy
E-mail: mauro.salvi@unipd.it

^c Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge, UK
E-mail: mh256@cam.ac.uk

Abstract

In this work, an iterative cycle of enzymatic assays, X-ray crystallography, molecular modelling and cellular assays were used to develop a functionalisable chemical probe for the CK2α/β PPI. The lead peptide, P8C9, successfully binds to CK2α at the PPI site, is easily synthesisable and functionalisable, highly stable in serum and small enough to accommodate further optimisation.

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Article information

DOI: https://doi.org/10.1039/D2CC00707J
Article type: Communication
Submitted: 04 Feb 2022
Accepted: 21 Mar 2022
First published: 21 Mar 2022
This article is Open Access

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Chem. Commun., 2022,58, 4791-4794

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Development of small cyclic peptides targeting the CK2α/β interface

E. L. Atkinson, J. Iegre, C. D’Amore, P. Brear, M. Salvi, M. Hyvönen and D. R. Spring, Chem. Commun., 2022, 58, 4791 DOI: 10.1039/D2CC00707J

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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Chemical Communications

Development of small cyclic peptides targeting the CK2α/β interface†

Abstract

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Development of small cyclic peptides targeting the CK2α/β interface

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