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Kinases and Phosphatases
Special Issues
Past, Present and Future of Protein Kinase CK2 Research
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Special Issue "Past, Present and Future of Protein Kinase CK2 Research"

A special issue of Kinases and Phosphatases (ISSN 2813-3757).

Deadline for manuscript submissions: 15 February 2024 | Viewed by 3218

Special Issue Editors

Dr. Mauro Salvi

E-Mail Website
Guest Editor
Department of Biomedical Sciences, University of Padova, Padova, Italy
Interests: protein phosphorylation; acidic protein kinases; tyrosine kinases; kinase inhibitors, signal transduction; post-translational modifications; cancer; cystic fibrosis
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Maria Ruzzene

E-Mail Website
Guest Editor
Department of Biomedical Sciences, University of Padova, Padova, Italy
Interests: signal transduction; cell signaling; signaling pathways; protein phosphorylation; protein kinases; protein phosphatases; protein kinase inhibitors; cancer biology; proteins; apoptosis; cell death; cancer research; cancer cell line
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

CK2 (formerly known as casein kinase 2) was the first protein kinase to be discovered in 1954. Since then, a huge number of studies have been published that tried to disclose its biochemical properties and its physiological and pathological roles. It is now established that CK2 is constitutively active, ubiquitously expressed, and involved in many biological processes as well as in the pathogenesis of important human diseases, including cancer, neurodegeneration and inflammation. However, despite much time and scientific effort, CK2 remains an enigmatic enzyme, as we are still far from fully understanding its actual pathophysiological roles, and the mechanisms that might modulate its functions.  Moreover, although it has long been considered a promising pharmacological target for diverse pathologies, and several inhibitors with increasing efficacy and specificity have been developed over the years, the actual value of its targeting in cancer has been recently questioned and deserves further debate. Furthermore, while its therapeutic targeting has been so far considered in terms of inhibition, the recent discovery of genetic diseases related to mutations of CK2 genes prompts the investigation of strategies to stimulate its activity, which has not been available so far.

It is, therefore, time for a Special Issue that on one hand retraces the main discoveries of CK2, and on the other, summarizes recent research and presents updates and new advances in the field.

In this Special Issue, we will, therefore, welcome original, commentary and review contributions in all areas of CK2 research and biological systems, with emphasis on works attempting to answer outstanding questions: how can a constitutive kinase be regulated? How many substrates and molecular partners does it currently count? For which human diseases does it really represent a therapeutic target, and which are the best pharmacological strategies? We look forward to contributions on these crucial issues as well as the many others that will be identified by the numerous scientists who work on CK2 or come across this fundamental enzyme.

Dr. Mauro Salvi
Prof. Dr. Maria Ruzzene
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Kinases and Phosphatases is an international peer-reviewed open access quarterly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • CK2
  • Casein kinase 2
  • CSNK2A1
  • CSNK2A2
  • CSNK2B
  • Protein phosphorylation
  • Human diseases
  • Signal transduction

Published Papers (4 papers)

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Research

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17 pages, 4062 KiB  
Article
Discovery and Exploration of Protein Kinase CK2 Binding Sites Using CK2α′Cys336Ser as an Exquisite Crystallographic Tool
by
Christian Werner
,
Dirk Lindenblatt
,
Kaido Viht
,
Asko Uri
and
Karsten Niefind
Kinases Phosphatases 2023, 1(4), 306-322; https://doi.org/10.3390/kinasesphosphatases1040018 - 25 Nov 2023
Viewed by 279
Abstract
The structural knowledge about protein kinase CK2 is dominated by crystal structures of human CK2α, the catalytic subunit of human CK2, and the product of the CSNK2A1 gene. In contrast, far fewer structures of CK2α′, its paralogous isoform and the product of the [...] Read more.
The structural knowledge about protein kinase CK2 is dominated by crystal structures of human CK2α, the catalytic subunit of human CK2, and the product of the CSNK2A1 gene. In contrast, far fewer structures of CK2α′, its paralogous isoform and the product of the CSNK2A2 gene, have been published. However, according to a PDB survey, CK2α′ is the superior alternative for crystallographic studies because of the inherent potential of the single mutant CK2α′Cys336Ser to provide crystal structures with atomic resolution. In particular, a triclinic crystal form of CK2α′Cys336Ser is a robust tool to determine high-quality enzyme-ligand complex structures via soaking. In this work, further high-resolution CK2α′Cys336Ser structures in complex with selected ligands emphasizing this trend are described. In one of these structures, the “N-terminal segment site”, a small-molecule binding region never found in any eukaryotic protein kinase and holding the potential for the development of highly selective substrate-competitive CK2 inhibitors, was discovered. In order to also address the binding site for the non-catalytic subunit CK2β, which is inaccessible in these triclinic CK2α′Cys336Ser crystals for small molecules, a reliable path to a promising monoclinic crystal form of CK2α′Cys336Ser is presented. In summary, the quality of CK2α′Cys336Ser as an exquisite crystallographic tool is solidified. Full article
(This article belongs to the Special Issue Past, Present and Future of Protein Kinase CK2 Research)
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Review

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18 pages, 2963 KiB  
Review
CK2 Chemical Probes: Past, Present, and Future
by
Han Wee Ong
,
David H. Drewry
and
Alison D. Axtman
Kinases Phosphatases 2023, 1(4), 288-305; https://doi.org/10.3390/kinasesphosphatases1040017 - 01 Nov 2023
Viewed by 881
Abstract
Protein kinase casein kinase 2 (CK2/CSNK2) is a pleiotropic kinase involved in many cellular processes and, accordingly, has been identified as a potential target for therapeutic intervention for multiple indications. Significant research effort has been invested into identifying CK2 inhibitors as potential drug [...] Read more.
Protein kinase casein kinase 2 (CK2/CSNK2) is a pleiotropic kinase involved in many cellular processes and, accordingly, has been identified as a potential target for therapeutic intervention for multiple indications. Significant research effort has been invested into identifying CK2 inhibitors as potential drug candidates and potent and selective CK2 chemical probes to interrogate CK2 function. Here, we review the small molecule inhibitors reported for CK2 and discuss various orthosteric, allosteric, and bivalent inhibitors of CK2. We focus on the pyrazolo[1,5-a]pyrimidines and naphthyridines, two chemotypes that have been extensively explored for chemical probe development. We highlight the uptake and demonstrated utility of the pyrazolo[1,5-a]pyrimidine chemical probe SGC-CK2-1 by the scientific community in cellular studies. Finally, we propose criteria for an ideal in vivo chemical probe for investigating CK2 function in a living organism. While no compound currently meets these metrics, we discuss ongoing and future directions in the development of in vivo chemical probes for CK2. Full article
(This article belongs to the Special Issue Past, Present and Future of Protein Kinase CK2 Research)
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14 pages, 3476 KiB  
Review
Exploring Protein Kinase CK2 Substrate Recognition and the Dynamic Response of Substrate Phosphorylation to Kinase Modulation
by
Luca Cesaro
,
Angelica Maria Zuliani
,
Valentina Bosello Travain
and
Mauro Salvi
Kinases Phosphatases 2023, 1(4), 251-264; https://doi.org/10.3390/kinasesphosphatases1040015 - 07 Oct 2023
Viewed by 477
Abstract
Protein kinase CK2 (formerly known as casein kinase 2 or II), a ubiquitous and constitutively active enzyme, is widely recognized as one of the most pleiotropic serine/threonine kinases. It plays a critical role in numerous signaling pathways, with hundreds of bona fide substrates. [...] Read more.
Protein kinase CK2 (formerly known as casein kinase 2 or II), a ubiquitous and constitutively active enzyme, is widely recognized as one of the most pleiotropic serine/threonine kinases. It plays a critical role in numerous signaling pathways, with hundreds of bona fide substrates. However, despite considerable research efforts, our understanding of the entire CK2 substratome and its functional associations with the majority of these substrates is far from being completely deciphered. In this context, we aim to provide an overview of how CK2 recognizes its substrates. We will discuss the pros and cons of the existing methods to manipulate CK2 activity in cells, as well as exploring the dynamic response of substrate phosphorylation to CK2 modulation. Full article
(This article belongs to the Special Issue Past, Present and Future of Protein Kinase CK2 Research)
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10 pages, 1202 KiB  
Review
Protein Kinase CK2 and SARS-CoV-2: An Expected Interplay Story
by
Camila Paz Quezada Meza
and
Maria Ruzzene
Kinases Phosphatases 2023, 1(2), 141-150; https://doi.org/10.3390/kinasesphosphatases1020009 - 16 Jun 2023
Cited by 3 | Viewed by 1210
Abstract
Protein kinase CK2 is a Ser/Thr protein kinase that phosphorylates hundreds of substrates mainly related to survival and proliferation pathways. It has long been considered an anti-cancer drug target. However, during the recent COVID-19 pandemic, CK2 inhibitors have been repurposed as anti-SARS-CoV-2 drugs. [...] Read more.
Protein kinase CK2 is a Ser/Thr protein kinase that phosphorylates hundreds of substrates mainly related to survival and proliferation pathways. It has long been considered an anti-cancer drug target. However, during the recent COVID-19 pandemic, CK2 inhibitors have been repurposed as anti-SARS-CoV-2 drugs. This was based on the initial finding of CK2 among the proteins of the host cell that interact with the viral proteins and modulate the infection. Since then, several studies have deepened our understanding of the CK2/COVID-19 connection, and we deem it is time to review all the findings. Interestingly, other coronaviruses cross-talk with CK2 as well, with similarities and differences compared to the SARS-CoV-2 case. Therefore, we believe that the analysis of the effects obtained by targeting CK2 in case of coronavirus infections, both at the molecular and phenomenological level, will help in extrapolating information that could be useful not only for COVID-19 (whose pandemic emergency is hopefully turning off) but also for other infections. Full article
(This article belongs to the Special Issue Past, Present and Future of Protein Kinase CK2 Research)
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