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Special Issue "Activity, Function and Druggability of Cancer-Related Enzymes"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: 30 July 2021.

Special Issue Editors

Dr. Alessio Nocentini
E-Mail Website
Guest Editor
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, 50019 Florence, Italy
Interests: medicinal chemistry; drug design; computational chemistry; carbonic anhydrases; enzymatic evaluation
Dr. Wagdy M. Eldehna
E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Egypt
Interests: drug design; medicinal chemistry; pharmaceutical organic synthesis
Dr. Stanislav Kalinin
E-Mail Website
Guest Editor
Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russia
Interests: medicinal chemistry; drug design; enzyme inhibition; multicomponent reactions

Special Issue Information

Dear colleagues,

Cancer remains a major cause of mortality and morbidity worldwide despite numerous studies have been and are being conducted to improve tumor prevention, early diagnosis and treatment.

Traditionally, several enzymes regulating cell division or involved in DNA replication have been considered valuable anticancer drug targets. Furthermore, alterations of the energy metabolism are among the main hallmarks of cancers making targeting glycolytic pathway enzymes an effective means for treating the disease. Finally, several enzymes have been used as biomarkers for cancer identification and validation being under- or over-expressed in various tumors. As a result, many such enzymes have been also validated as targets for therapeutic intervention. Accordingly, ​several main classes of cancer-related enzymes can be allocated, such as:

  1. Glycolytic enzymes (e.g. lactate dehydrogenase A, glucose-6-phosphate dehydrogenase)
  2. Oncogenic signal transduction enzymes (e.g. kinases, phosphatases)
  3. DNA-related enzymes (e.g. DNA polymerase, topoisomerase, telomerase)
  4. Extracellular enzymes (e.g. carbonic anhydrases, matrix metalloproteases, ecto-5′-nucleotidase)

It is noteworthy that nonglycolytic enzymes such as carbonic anhydrases (CAs) IX and XII play a major role in the metabolic switch of tumor cells. Indeed, the resulting intracellular acidosis, incompatible with basic cellular functions, induces tumor cells to activate complex molecular mechanisms, actively involving CA IX and XII among other proteins, that restore the intracellular pH and acidify the extracellular pH to promote cancer survival and proliferation.

Targeting enzymatic variations of tumor cells shown to be associated with cancer progression offers a huge potential and remains a largely unexplored topic for developing new anti-cancer therapies. This Special Issue is dedicated to all important advances in the field of cancer-related enzymes as biomarkers and therapeutic targets for the diagnosis and treatment of tumors.

Original papers, reviews articles, and perspectives from experts in the field are welcome.

Dr. Alessio Nocentini
Dr. Wagdy M. Eldehna
Dr. Stanislav Kalinin
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 papers will be 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.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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.


  • Enzyme
  • Cancer
  • Glycolysis
  • Metabolic switch
  • Cancer epigenetics
  • Signal transduction
  • Biomarker
  • Therapy

Published Papers (1 paper)

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Open AccessReview
Functional Roles of SPINK1 in Cancers
Int. J. Mol. Sci. 2021, 22(8), 3814; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22083814 - 07 Apr 2021
Viewed by 261
Serine Peptidase Inhibitor Kazal Type 1 (SPINK1) is a secreted protein known as a protease inhibitor of trypsin in the pancreas. However, emerging evidence shows its function in promoting cancer progression in various types of cancer. SPINK1 modulated tumor malignancies and induced the [...] Read more.
Serine Peptidase Inhibitor Kazal Type 1 (SPINK1) is a secreted protein known as a protease inhibitor of trypsin in the pancreas. However, emerging evidence shows its function in promoting cancer progression in various types of cancer. SPINK1 modulated tumor malignancies and induced the activation of the downstream signaling of epidermal growth factor receptor (EGFR) in cancer cells, due to the structural similarity with epidermal growth factor (EGF). The discoverable SPINK1 somatic mutations, expressional signatures, and prognostic significances in various types of cancer have attracted attention as a cancer biomarker in clinical applications. Emerging findings further clarify the direct and indirect biological effects of SPINK1 in regulating cancer proliferation, metastasis, drug resistance, transdifferentiation, and cancer stemness, warranting the exploration of the SPINK1-mediated molecular mechanism to identify a therapeutic strategy. In this review article, we first integrate the transcriptomic data of different types of cancer with clinical information and recent findings of SPINK1-mediated malignant phenotypes. In addition, a comprehensive summary of SPINK1 expression in a pan-cancer panel and individual cell types of specific organs at the single-cell level is presented to indicate the potential sites of tumorigenesis, which has not yet been reported. This review aims to shed light on the roles of SPINK1 in cancer and provide guidance and potential directions for scientists in this field. Full article
(This article belongs to the Special Issue Activity, Function and Druggability of Cancer-Related Enzymes)
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