Development of small cyclic peptides targeting the CK2α/β interface

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 functionalis...

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Detalles Bibliográficos
Autores principales: Atkinson, Eleanor L., Iegre, Jessica, D’Amore, Claudio, Brear, Paul, Salvi, Mauro, Hyvönen, Marko, Spring, David R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9004346/
https://www.ncbi.nlm.nih.gov/pubmed/35343996
http://dx.doi.org/10.1039/d2cc00707j
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author Atkinson, Eleanor L.
Iegre, Jessica
D’Amore, Claudio
Brear, Paul
Salvi, Mauro
Hyvönen, Marko
Spring, David R.
author_facet Atkinson, Eleanor L.
Iegre, Jessica
D’Amore, Claudio
Brear, Paul
Salvi, Mauro
Hyvönen, Marko
Spring, David R.
author_sort Atkinson, Eleanor L.
collection PubMed
description 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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spelling pubmed-90043462022-05-03 Development of small cyclic peptides targeting the CK2α/β interface Atkinson, Eleanor L. Iegre, Jessica D’Amore, Claudio Brear, Paul Salvi, Mauro Hyvönen, Marko Spring, David R. Chem Commun (Camb) Chemistry 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. The Royal Society of Chemistry 2022-03-21 /pmc/articles/PMC9004346/ /pubmed/35343996 http://dx.doi.org/10.1039/d2cc00707j Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by/3.0/
spellingShingle Chemistry
Atkinson, Eleanor L.
Iegre, Jessica
D’Amore, Claudio
Brear, Paul
Salvi, Mauro
Hyvönen, Marko
Spring, David R.
Development of small cyclic peptides targeting the CK2α/β interface
title Development of small cyclic peptides targeting the CK2α/β interface
title_full Development of small cyclic peptides targeting the CK2α/β interface
title_fullStr Development of small cyclic peptides targeting the CK2α/β interface
title_full_unstemmed Development of small cyclic peptides targeting the CK2α/β interface
title_short Development of small cyclic peptides targeting the CK2α/β interface
title_sort development of small cyclic peptides targeting the ck2α/β interface
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9004346/
https://www.ncbi.nlm.nih.gov/pubmed/35343996
http://dx.doi.org/10.1039/d2cc00707j
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