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Bioactive Compounds and Enzyme Inhibitors in Cancer Therapy
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Bioactive Compounds and Enzyme Inhibitors in Cancer Therapy

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: 20 May 2025 | Viewed by 1323

Special Issue Editor

Prof. Dr. Fabio Altieri

E-Mail Website
Guest Editor
Department of Biochemical Sciences “A. RossiFanelli”, La Sapienza University, 00185 Rome, Italy
Interests: oxidative stress; cellular biochemistry; signal transduction; protein–ligand interaction; bioactive compounds
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is a disease of high mortality, and its prevalence has increased steadily in the last few years. However, during the last decade, the development of modern chemotherapy schemes, new radiotherapy techniques, targeted therapies and immunotherapy has brought new hope in the treatment of cancer. Natural bioactive agents from plants are gaining wide attention for their anticancer activities. The use of natural compounds as cancer therapeutics has several advantages, such as a low toxicity, wide availability, and compatibility with traditional chemotherapeutic agents. Bioactive compounds also play an important role in the inhibition of enzymatic activities associated with human diseases. Furthermore, enzyme inhibitors may be used in cancer treatment to block specific enzymes that play an important role in cell growth. With this, the development of specific inhibitors that control selected enzymes’ activity has a potential research value in cancer therapy.

This Special Issue aims to provide a platform for research on bioactive compounds and enzyme inhibitors, with a special focus on cancer treatment. We welcome your submission of original papers and reviews containing molecular results.

Prof. Dr. Fabio Altieri
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 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.

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.

Keywords

  • bioactive compounds
  • enzyme inhibitors
  • cancer therapy

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Published Papers (1 paper)

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Research

22 pages, 10901 KiB  
Article
Glucosylceramide Synthase Inhibition in Combination with Aripiprazole Sensitizes Hepatocellular Cancer Cells to Sorafenib and Doxorubicin
by Richard Jennemann, Martina Volz, Roberto Carlos Frias-Soler, Almut Schulze, Karsten Richter, Sylvia Kaden and Roger Sandhoff
Int. J. Mol. Sci. 2025, 26(1), 304; https://doi.org/10.3390/ijms26010304 - 31 Dec 2024
Viewed by 1070
Abstract
Hepatocellular carcinoma (HCC) is one of the leading causes of cancer deaths due to its late diagnosis and restricted therapeutic options. Therefore, the search for appropriate alternatives to commonly applied therapies remains an area of high clinical need. Here we investigated [...] Read more.
Hepatocellular carcinoma (HCC) is one of the leading causes of cancer deaths due to its late diagnosis and restricted therapeutic options. Therefore, the search for appropriate alternatives to commonly applied therapies remains an area of high clinical need. Here we investigated the therapeutic potential of the glucosylceramide synthase (GCS) inhibitor Genz-123346 and the cationic amphiphilic drug aripiprazole on the inhibition of Huh7 and Hepa 1-6 hepatocellular cancer cell and tumor microsphere growth. Single and combinatorial treatments with both drugs at 5 µM concentration led to efficient cell cycle arrest, reduced expression of cyclins A and E, increased lipid storage in lysosomal compartments, accompanied by increased uptake of lysotracker, and elevated expression of the autophagy marker Lc3 II. Both drugs affected mitochondrial function, indicated by altered mitotracker uptake and impaired mitochondrial respiration. Aripiprazole in monotherapy, or even more pronounced in combination with Genz, also potentiated the effect of the cytostatic drugs sorafenib and doxorubicin on tumor cell- and tumor spheroid-growth inhibition. Targeting GCS with Genz with the parallel application of cationic amphiphilic drugs such as aripiprazole in combination with cytostatic drugs may thus represent a potent therapeutic approach in the treatment of HCC and potentially other cancer types. Full article
(This article belongs to the Special Issue Bioactive Compounds and Enzyme Inhibitors in Cancer Therapy)
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