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Special Issue "Enzyme Inhibitors and Activators in Cancer Research, Therapy and Prevention"

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

Deadline for manuscript submissions: 30 April 2022.

Special Issue Editor

Prof. Dr. Hidayat Hussain
E-Mail Website
Guest Editor
Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, D-06120 Halle (Salle), Germany
Interests: natural product chemistry; medicinal chemistry; cancer biology; bioorganic chemistry; pharmacology; diabetes; synthetic chemistry; biology-oriented synthesis
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Special Issue Information

Dear Colleagues,

Modulating enzyme activity is a proven strategy in drug discovery, as shown by the small-molecule armament of marketed drugs – about half of the total – that is directed against enzymes. Rationales for targeting enzymes are typically based on their pivotal roles in disease states, and the possibility of designing chemical entities capable of docking sensitive ligand-binding sites. In today’s post-genomic era, this area of research can take advantage of, and be expedited by, major advances in target identification and validation, production of natural product and chemical libraries, nutraceutical research, cell-free and cell-based assay methods, high-throughput screening technologies, hyphenated techniques, as well as cheminformatics and bioinformatics resources.

The natural world provided huge number of secondary metabolites with intriguing medical properties known by humankind. Because in recent decade, hundreds of new natural enzyme inhibitors derived from the natural world and these molecules are able to target important biological human proteins or enzymes are identified. Notably, some of these molecules which illustrated activities towards enzymes relevant to cancer, have been included in clinical trials to evaluate their effectiveness.

This Special Issue welcomes original articles, communications and reviews dealing with the isolation and/or the investigation of mechanisms of action of natural products, natural product derivatives and synthetic compounds with potential effects towards cancer-associated enzymes. Finding target-identification (with biological assays together with computational studies), in vivo studies, bioavailability, toxicity, and the design of novel molecules with improved biological effects against cancer-associated enzymes are also welcome. Pharmacological studies should include appropriate positive controls.

Prof. Dr. Hidayat Hussain
Guest Editor

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.


  • cancer
  • natural products
  • natural product derivatives
  • synthetic compounds
  • cancer-associated enzymes
  • (activity-guided) isolation of natural products
  • computational methods
  • in vitro studies
  • in vivo studies
  • mechanism of action
  • bioavailability
  • toxicity

Published Papers (1 paper)

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Progress in the Development of Eukaryotic Elongation Factor 2 Kinase (eEF2K) Natural Product and Synthetic Small Molecule Inhibitors for Cancer Chemotherapy
Int. J. Mol. Sci. 2021, 22(5), 2408; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22052408 - 27 Feb 2021
Cited by 1 | Viewed by 1014
Eukaryotic elongation factor 2 kinase (eEF2K or Ca2+/calmodulin-dependent protein kinase, CAMKIII) is a new member of an atypical α-kinase family different from conventional protein kinases that is now considered as a potential target for the treatment of cancer. This protein regulates [...] Read more.
Eukaryotic elongation factor 2 kinase (eEF2K or Ca2+/calmodulin-dependent protein kinase, CAMKIII) is a new member of an atypical α-kinase family different from conventional protein kinases that is now considered as a potential target for the treatment of cancer. This protein regulates the phosphorylation of eukaryotic elongation factor 2 (eEF2) to restrain activity and inhibit the elongation stage of protein synthesis. Mounting evidence shows that eEF2K regulates the cell cycle, autophagy, apoptosis, angiogenesis, invasion, and metastasis in several types of cancers. The expression of eEF2K promotes survival of cancer cells, and the level of this protein is increased in many cancer cells to adapt them to the microenvironment conditions including hypoxia, nutrient depletion, and acidosis. The physiological function of eEF2K and its role in the development and progression of cancer are here reviewed in detail. In addition, a summary of progress for in vitro eEF2K inhibitors from anti-cancer drug discovery research in recent years, along with their structure–activity relationships (SARs) and synthetic routes or natural sources, is also described. Special attention is given to those inhibitors that have been already validated in vivo, with the overall aim to provide reference context for the further development of new first-in-class anti-cancer drugs that target eEF2K. Full article
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