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Recent Discovery and Mechanisms of Potential Anticancer Drugs

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

Deadline for manuscript submissions: 20 April 2025 | Viewed by 3951

Special Issue Editors


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Guest Editor
cE3c—Centre for Ecology, Evolution and Environmental Changes, Azorean Biodiversity Group, University of Azores, Rua Mãe de Deus, 9501-801 Ponta Delgada, Portugal
Interests: bioactive natural compounds; secondary metabolites; chromatographic techniques; spectroscopic techniques; natural compounds
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Guest Editor
Institute of Chemical Engineering, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
Interests: natural and synthetic bioactive compounds; mechanisms of anticancer activity; nuclear receptor modulators; nanoparticle-based drug carriers; metronomic anticancer therapy; combination anticancer therapy; high-performance liquid chromatography of bioactive compounds

Special Issue Information

Dear Colleagues,

Despite huge progress in cancer treatment, this disease continues to be a global problem and challenge for scientists to improve the success of the therapy. In addition to the classical cytostatic compounds, a number of new molecules were developed as drugs for precision medicine that targeted selectively cancer cells: antibodies, antibody–drug conjugates, nuclear receptor modulators, cancer protein inhibitors, etc. Nanoparticles, loaded with anticancer antibodies, protein inhibitors or cytostatic compounds, offer alternative approaches to increase the efficiency of bioactive molecules and reduce the toxicity of poorly water-soluble chemotherapeutic compounds. The development of knowledge on the mechanisms of the antiproliferative activity and DNA repair mechanisms is an important step in the treatment of cancer.

This Special Issue is devoted to the discovery of new anticancer drugs along with elucidation of their mechanisms of activity. The identification of new natural or synthetic molecules, including cytostatic compounds, nuclear receptor or oncoprotein modulators, antibodies, etc., with the study of their cancer inhibition mechanisms and drug–protein interactions can contribute to the present Special Issue. Nanotechnology-based new drug delivery systems that target cancer cells are also of interest. Clinical trials are not suitable for this Special Issue; however, preclinical and clinical results with the analysis of the mechanisms of anticancer treatment using biomolecular experiments are also welcome.

Potential topics include, but are not limited to, the following:

  • Mechanisms of activity of new natural or synthetic antiproliferative compounds;
  • Oncoprotein inhibitors and oncogene targeted therapies;
  • Nuclear receptor modulators;
  • Cancer-cell-targeted antibodies, antibody–drug conjugates;
  • Anticancer drug carriers, nanoparticle-based drug delivery systems;
  • DNA repair mechanisms, regulation of gene expression in cancer;
  • Anticancer drug design and drug-protein interactions;
  • Preclinical and clinical results with biomolecular experiments about the mechanisms of activity of anticancer therapy;
  • A new view on conventional anticancer drugs and their mechanisms of activity.

Dr. Ana M. L. Seca
Dr. Diana I. Ivanova
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.

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

  • anticancer drugs
  • drug design
  • drug delivery systems

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Published Papers (2 papers)

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Research

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21 pages, 4772 KiB  
Article
Effect of Diosgenin in Suppressing Viability and Promoting Apoptosis of Human Prostate Cancer Cells: An Interplay with the G Protein-Coupled Oestrogen Receptor?
by Marília I. Figueira, Ricardo Marques, Henrique J. Cardoso, Lara R. S. Fonseca, Ana P. Duarte, Samuel Silvestre and Sílvia Socorro
Int. J. Mol. Sci. 2024, 25(22), 12006; https://doi.org/10.3390/ijms252212006 - 8 Nov 2024
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Abstract
Diosgenin is a phytosteroid sapogenin with reported antitumoral activity. Despite the evidence indicating a lower incidence of prostate cancer (PCa) associated with a higher consumption of phytosteroids and the beneficial role of these compounds, only a few studies have investigated the effects of [...] Read more.
Diosgenin is a phytosteroid sapogenin with reported antitumoral activity. Despite the evidence indicating a lower incidence of prostate cancer (PCa) associated with a higher consumption of phytosteroids and the beneficial role of these compounds, only a few studies have investigated the effects of diosgenin in PCa, and its mechanisms of action remain to be disclosed. The present study investigated the effect of diosgenin in modulating PCa cell fate and glycolytic metabolism and explored its potential interplay with G protein-coupled oestrogen receptor (GPER). Non-neoplastic (PNT1A) and neoplastic (LNCaP, DU145, and PC3) human prostate cell lines were stimulated with diosgenin in the presence or absence of the GPER agonist G1 and upon GPER knockdown. Diosgenin decreased the cell viability, as indicated by the MTT assay results, which also demonstrated that castrate-resistant PCa cells were the most sensitive to treatment (PC3 > DU145 > LNCaP > PNT1A; IC50 values of 14.02, 23.21, 56.12, and 66.10 µM, respectively). Apoptosis was enhanced in diosgenin-treated cells, based on the increased caspase-3-like activity, underpinned by the altered expression of apoptosis regulators evaluated by Western blot analysis, which indicated the activation of the extrinsic pathway. Exposure to diosgenin also altered glucose metabolism. Overall, the effects of diosgenin were potentiated in the presence of G1. Moreover, diosgenin treatment augmented GPER expression, and the knockdown of the GPER gene suppressed the proapoptotic effects of diosgenin in PC3 cells. Our results support the antitumorigenic role of diosgenin and its interest in PCa therapy, alone or in combination with G1, mainly targeting the more aggressive stages of the disease. Full article
(This article belongs to the Special Issue Recent Discovery and Mechanisms of Potential Anticancer Drugs)
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Review

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18 pages, 638 KiB  
Review
Myeloid-Derived Suppressor Cells: Therapeutic Target for Gastrointestinal Cancers
by Junaid Arshad, Amith Rao, Matthew L. Repp, Rohit Rao, Clinton Wu and Juanita L. Merchant
Int. J. Mol. Sci. 2024, 25(5), 2985; https://doi.org/10.3390/ijms25052985 - 4 Mar 2024
Cited by 2 | Viewed by 2442
Abstract
Gastrointestinal cancers represent one of the more challenging cancers to treat. Current strategies to cure and control gastrointestinal (GI) cancers like surgery, radiation, chemotherapy, and immunotherapy have met with limited success, and research has turned towards further characterizing the tumor microenvironment to develop [...] Read more.
Gastrointestinal cancers represent one of the more challenging cancers to treat. Current strategies to cure and control gastrointestinal (GI) cancers like surgery, radiation, chemotherapy, and immunotherapy have met with limited success, and research has turned towards further characterizing the tumor microenvironment to develop novel therapeutics. Myeloid-derived suppressor cells (MDSCs) have emerged as crucial drivers of pathogenesis and progression within the tumor microenvironment in GI malignancies. Many MDSCs clinical targets have been defined in preclinical models, that potentially play an integral role in blocking recruitment and expansion, promoting MDSC differentiation into mature myeloid cells, depleting existing MDSCs, altering MDSC metabolic pathways, and directly inhibiting MDSC function. This review article analyzes the role of MDSCs in GI cancers as viable therapeutic targets for gastrointestinal malignancies and reviews the existing clinical trial landscape of recently completed and ongoing clinical studies testing novel therapeutics in GI cancers. Full article
(This article belongs to the Special Issue Recent Discovery and Mechanisms of Potential Anticancer Drugs)
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