Mechanism of CK2 Inhibition by a Ruthenium-Based Polyoxometalate.

CK2 SAXS inhibition polyoxometalate substrate competitive

Journal

Frontiers in molecular biosciences
ISSN: 2296-889X
Titre abrégé: Front Mol Biosci
Pays: Switzerland
ID NLM: 101653173

Informations de publication

Date de publication:
2022
Historique:
received: 28 03 2022
accepted: 18 05 2022
entrez: 20 6 2022
pubmed: 21 6 2022
medline: 21 6 2022
Statut: epublish

Résumé

CK2 is a Ser/Thr protein kinase involved in many cellular processes such as gene expression, cell cycle progression, cell growth and differentiation, embryogenesis, and apoptosis. Aberrantly high CK2 activity is widely documented in cancer, but the enzyme is also involved in several other pathologies, such as diabetes, inflammation, neurodegeneration, and viral infections, including COVID-19. Over the last years, a large number of small-molecules able to inhibit the CK2 activity have been reported, mostly acting with an ATP-competitive mechanism. Polyoxometalates (POMs), are metal-oxide polyanionic clusters of various structures and dimensions, with unique chemical and physical properties. POMs were identified as nanomolar CK2 inhibitors, but their mechanism of inhibition and CK2 binding site remained elusive. Here, we present the biochemical and biophysical characterizing of the interaction of CK2α with a ruthenium-based polyoxometalate, [Ru

Identifiants

pubmed: 35720133
doi: 10.3389/fmolb.2022.906390
pii: 906390
pmc: PMC9201508
doi:

Types de publication

Journal Article

Langues

eng

Pagination

906390

Informations de copyright

Copyright © 2022 Fabbian, Giachin, Bellanda, Borgo, Ruzzene, Spuri, Campofelice, Veneziano, Bonchio, Carraro and Battistutta.

Déclaration de conflit d'intérêts

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

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Auteurs

Simone Fabbian (S)

Department of Chemical Sciences, University of Padova, Padova, Italy.

Gabriele Giachin (G)

Department of Chemical Sciences, University of Padova, Padova, Italy.

Massimo Bellanda (M)

Department of Chemical Sciences, University of Padova, Padova, Italy.
CNR Institute of Biomolecular Chemistry, University of Padova, Padova, Italy.

Christian Borgo (C)

Department of Biomedical Sciences, University of Padova, Padova, Italy.

Maria Ruzzene (M)

Department of Biomedical Sciences, University of Padova, Padova, Italy.
CNR Institute of Neurosciences, University of Padova, Padova, Italy.

Giacomo Spuri (G)

Department of Biomedical Sciences, University of Padova, Padova, Italy.

Ambra Campofelice (A)

Department of Chemical Sciences, University of Padova, Padova, Italy.

Laura Veneziano (L)

Department of Chemical Sciences, University of Padova, Padova, Italy.

Marcella Bonchio (M)

Department of Chemical Sciences, University of Padova, Padova, Italy.
Institute on Membrane Technology (ITM)-CNR, University of Padova, Padova, Italy.

Mauro Carraro (M)

Department of Chemical Sciences, University of Padova, Padova, Italy.
Institute on Membrane Technology (ITM)-CNR, University of Padova, Padova, Italy.

Roberto Battistutta (R)

Department of Chemical Sciences, University of Padova, Padova, Italy.
CNR Institute of Biomolecular Chemistry, University of Padova, Padova, Italy.

Classifications MeSH