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The Emerging Role of Kinase Inhibitors in Cancer
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The Emerging Role of Kinase Inhibitors in Cancer

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pathology, Diagnostics, and Therapeutics".

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 9443

Special Issue Editors

Dr. Giovanna Casili

E-Mail Website
Guest Editor
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno D’Alcontres, 31-98166 Messina, Italy
Interests: neuroinflammation; neurodegeneration; inflammation; oncology; brain tumor
Special Issues, Collections and Topics in MDPI journals
Dr. Irene Paterniti

E-Mail Website
Guest Editor
Dipartimento di Medicina Clinica e Sperimentale, Università degli Studi di Messina, Messina, Italy
Interests: cancer; neuro-oncology; neurodegenerative diseases; pharmacology; inflammation; apoptosis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In the last decade, protein kinase inhibitors have gained great attention in applications relating to the management of various diseases, including cancer. Despite relevant progress made in conventional treatments for cancer therapy, novel therapeutic strategies are needed. Protein kinase inhibitors represent an alternative and safer therapeutic approach for cancer treatment, as they are directed against tumor-specific molecules and signaling pathways; therefore, they should be more selective in their effects than chemotherapy and better tolerated. Thus, this Special Issue will aim to study the role of kinase inhibitors in cancer in depth, highlighting their possible use as therapeutic treatments for cancer.

Dr. Giovanna Casili
Dr. Irene Paterniti
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • cancer
  • protein kinase inhibitor
  • anti-cancer drugs
  • drug targets
  • signal transduction
  • apoptosis

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Published Papers (3 papers)

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Research

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15 pages, 4873 KiB  
Article
The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor
by Alessandro Agnarelli, Andrea Lauer Betrán, Athanasios Papakyriakou, Viviana Vella, Mark Samuels, Panagiotis Papanastasopoulos, Christina Giamas, Erika J. Mancini, Justin Stebbing, John Spencer, Chiara Cilibrasi, Angeliki Ditsiou and Georgios Giamas
Int. J. Mol. Sci. 2023, 24(1), 865; https://doi.org/10.3390/ijms24010865 - 3 Jan 2023
Cited by 4 | Viewed by 4226
Abstract
Recently, the oncogenic role of lemur tyrosine kinase 3 (LMTK3) has been well established in different tumor types, highlighting it as a viable therapeutic target. In the present study, using in vitro and cell-based assays coupled with biophysical analyses, we identify a highly [...] Read more.
Recently, the oncogenic role of lemur tyrosine kinase 3 (LMTK3) has been well established in different tumor types, highlighting it as a viable therapeutic target. In the present study, using in vitro and cell-based assays coupled with biophysical analyses, we identify a highly selective small molecule LMTK3 inhibitor, namely C36. Biochemical/biophysical and cellular studies revealed that C36 displays a high in vitro selectivity profile and provides notable therapeutic effect when tested in the National Cancer Institute (NCI)-60 cancer cell line panel. We also report the binding affinity between LMTK3 and C36 as demonstrated via microscale thermophoresis (MST). In addition, C36 exhibits a mixed-type inhibition against LMTK3, consistent with the inhibitor overlapping with both the adenosine 5′-triphosphate (ATP)- and substrate-binding sites. Treatment of different breast cancer cell lines with C36 led to decreased proliferation and increased apoptosis, further reinforcing the prospective value of LMTK3 inhibitors for cancer therapy. Full article
(This article belongs to the Special Issue The Emerging Role of Kinase Inhibitors in Cancer)
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Review

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10 pages, 1024 KiB  
Review
The Pivotal Role of Protein Phosphatase 2A (PP2A) in Brain Tumors
by Laura Cucinotta, Alessia Filippone, Giovanna Casili, Marika Lanza, Valentina Bova, Anna Paola Capra, Raffaella Giuffrida, Cristina Colarossi, Dorotea Sciacca, Irene Paterniti, Salvatore Cuzzocrea, Michela Campolo and Emanuela Esposito
Int. J. Mol. Sci. 2022, 23(24), 15717; https://doi.org/10.3390/ijms232415717 - 11 Dec 2022
Cited by 3 | Viewed by 2521
Abstract
Protein phosphatase 2A (PP2A) is a highly complex heterotrimeric Ser/Thr phosphatase that regulates many cellular processes. PP2A is dysregulated in several human diseases, including oncological pathology; interestingly, PP2A appears to be essential for controlling cell growth and may be involved in cancer development. [...] Read more.
Protein phosphatase 2A (PP2A) is a highly complex heterotrimeric Ser/Thr phosphatase that regulates many cellular processes. PP2A is dysregulated in several human diseases, including oncological pathology; interestingly, PP2A appears to be essential for controlling cell growth and may be involved in cancer development. The role of PP2A as a tumor suppressor has been extensively studied and reviewed. To leverage the potential clinical utility of combination PP2A inhibition and radiotherapy treatment, it is vital that novel highly specific PP2A inhibitors be developed. In this review, the existing literature on the role of PP2A in brain tumors, especially in gliomas and glioblastoma (GBM), was analyzed. Interestingly, the review focused on the role of PP2A inhibitors, focusing on CIP2A inhibition, as CIP2A participated in tumor cell growth by stimulating cell-renewal survival, cellular proliferation, evasion of senescence and inhibition of apoptosis. This review suggested CIP2A inhibition as a promising strategy in oncology target therapy. Full article
(This article belongs to the Special Issue The Emerging Role of Kinase Inhibitors in Cancer)
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16 pages, 1529 KiB  
Review
Protein Kinase Inhibitors as a New Target for Immune System Modulation and Brain Cancer Management
by Alessia Filippone, Deborah Mannino, Giovanna Casili, Marika Lanza, Irene Paterniti, Salvatore Cuzzocrea, Anna Paola Capra, Lorenzo Colarossi, Dario Giuffrida, Sofia Paola Lombardo and Emanuela Esposito
Int. J. Mol. Sci. 2022, 23(24), 15693; https://doi.org/10.3390/ijms232415693 - 10 Dec 2022
Cited by 1 | Viewed by 1990
Abstract
High-grade brain tumors are malignant tumors with poor survival and remain the most difficult tumors to treat. An important contributing factor to the development and progression of brain tumors is their ability to evade the immune system. Several immunotherapeutic strategies including vaccines and [...] Read more.
High-grade brain tumors are malignant tumors with poor survival and remain the most difficult tumors to treat. An important contributing factor to the development and progression of brain tumors is their ability to evade the immune system. Several immunotherapeutic strategies including vaccines and checkpoint inhibitors have been studied to improve the effectiveness of the immune system in destroying cancer cells. Recent studies have shown that kinase inhibitors, capable of inhibiting signal transduction cascades that affect cell proliferation, migration, and angiogenesis, have additional immunological effects. In this review, we explain the beneficial therapeutic effects of novel small-molecule kinase inhibitors and explore how, through different mechanisms, they increase the protective antitumor immune response in high-grade brain tumors. Full article
(This article belongs to the Special Issue The Emerging Role of Kinase Inhibitors in Cancer)
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