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Pharmaceuticals
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Targeting Apoptosis as a Strategy for Developing New Drugs
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Targeting Apoptosis as a Strategy for Developing New Drugs

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 24 December 2024 | Viewed by 4488

Special Issue Editors

Dr. Magdalena Skonieczna

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Guest Editor
1 Department of Systems Biology and Engineering, Faculty of Automatic Control, Electronics and Computer Science, Silesian University of Technology, 44-100 Gliwice, Poland; 2 Biotechnology Centre, Silesian University of Technology, 44-100 Gliwice, Poland.
Interests: cell biology; cancer cells; cell signaling; oxidative stress; cytotoxicity
Special Issues, Collections and Topics in MDPI journals
Dr. Anna Kasprzycka

E-Mail Website
Guest Editor
1. Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, Poland
2. Biotechnology Centre, Silesian University of Technology, 44-100 Gliwice, Poland
Interests: medicinal chemistry; carbohydrate chemistry; glycoconjugates; organosulfur compounds; anticancer compounds; enzyme inhibitors

Special Issue Information

Dear Colleagues,

Regulated cell death (RCD) plays a significant role in the homeostasis of the body, both in physiological and pathological conditions. Excessive or insufficient RCD can cause diseases. RCD can take many forms, including apoptosis, necroptosis, or ferroptosis. Cells may be sensitive or resistant to different death types, which depends on the cell’s origin and treatment. For a long time, a considerable amount of interest has been paid towards searching for less well-known anticancer agents, especially with proapoptotic activities. They were found to be good targets for drug repurposing because of their proven safety, inexpensiveness, quality, and well-known ways of synthesis. Some of them exhibit a wide range of biological activities, such as anticancer, antiviral, anti-inflammatory, immunosupressive, antibacterial, and reversal of multidrug resistance. A variable type of biologically active molecules, natural or artificially synthesized, were used during the 19th–20th centuries due to their health benefits. However, validated studies of their derivatives, based on different nanoparticles, composed drug delivery systems, encapsulates, etc., with an effect on malignant tumor cells, have only begun within the last few decades. Proapoptotic agents and inducers of cellular death pathways are still the best players in anticancer strategies.

Dr. Magdalena Skonieczna
Dr. Anna Kasprzycka
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. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). 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

  • proapoptotic drugs
  • cellular death
  • death pathways
  • cell signaling
  • apoptosis inductors
  • intracellular death executors
  • crosstalk of signaling pathways
  • regulatory cell death (RCD)
  • regulation of cell death

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Published Papers (3 papers)

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Research

18 pages, 4129 KiB  
Article
In Vitro Studies of Genistein Lipophilic Derivatives as Potential UV Radiation Protectors
by Magdalena Skonieczna, Kinga Plasa, Ewa Borowska, Agata Jakubowska, Wiesław Szeja and Anna Kasprzycka
Pharmaceuticals 2024, 17(9), 1166; https://doi.org/10.3390/ph17091166 - 3 Sep 2024
Viewed by 446
Abstract
The major environmental factor responsible for skin cancer is ultraviolet (UV) radiation, present in sunlight. UV radiation is directly linked to the production of reactive oxygen species (ROS), which accumulate in exposed cells and cause serious damage. The antioxidant systems present in cells [...] Read more.
The major environmental factor responsible for skin cancer is ultraviolet (UV) radiation, present in sunlight. UV radiation is directly linked to the production of reactive oxygen species (ROS), which accumulate in exposed cells and cause serious damage. The antioxidant systems present in cells cannot always sufficiently neutralize the ROS. Therefore, supplementation with exogenous antioxidants has been proposed. The antioxidant properties of some isoflavones, such as genistein, have already been well-proven. Genistein has limited bioavailability. However, its derivatives, with increased lipophilicity, could facilitate its transfer into cells, where they can expose its antioxidative potential. This study aims to investigate three genistein derivatives, with greater lipophilicity than the native compound, regarding their cytotoxicity, antioxidative properties, and effect on the cell cycle in normal human dermal fibroblasts (NHDF) and a melanoma cancer cell line (Me45). Results showed that lipophilic modification of the genistein molecule changes the biological response of NHDF and Me45 cell lines to UV-C radiation, but the lipophilicity cannot be directly linked with the activity of the compounds. A comparison of the effects of the genistein derivatives on healthy and cancerous cells suggests that their mode of action strongly depends on the type of cell involved. Full article
(This article belongs to the Special Issue Targeting Apoptosis as a Strategy for Developing New Drugs)
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15 pages, 4753 KiB  
Article
The Proteasome Inhibitor Marizomib Evokes Endoplasmic Reticulum Stress and Promotes Apoptosis in Human Glioblastoma Cells
by Magdalena Kusaczuk, Natalia Tyszka, Rafał Krętowski and Marzanna Cechowska-Pasko
Pharmaceuticals 2024, 17(8), 1089; https://doi.org/10.3390/ph17081089 - 20 Aug 2024
Viewed by 566
Abstract
Proteasomes play an important role in the physiology of cancer cells, and inhibition of their activity may be used as a promising therapeutic strategy against glioblastoma (GBM). Although certain proteasome inhibitors (PIs) have been approved for the treatment of other malignancies, they have [...] Read more.
Proteasomes play an important role in the physiology of cancer cells, and inhibition of their activity may be used as a promising therapeutic strategy against glioblastoma (GBM). Although certain proteasome inhibitors (PIs) have been approved for the treatment of other malignancies, they have limited effectiveness against GBM due to low brain bioavailability. Marizomib (MZB) is an irreversible, second-generation proteasome inhibitor, which unlike other PIs can penetrate through the blood–brain barrier, making it a promising therapeutic tool in brain malignancies. The antitumor activity of MZB was investigated in LN229 and U118 cells. The MTT test and the ATP-based assay were performed to evaluate cytotoxicity. Flow cytometry analysis was used to determine the apoptotic death of GBM cells. Luminescent assays were used to assess levels of reactive oxygen species (ROS) and the activity of caspase 3/7. RT-qPCR and Western blot analyses were used to determine gene and protein expressions. Marizomib decreased the viability and caused apoptotic death of GBM cells. The proapoptotic effect was accompanied by activation of caspase 3 and overexpression of cl-PARP, Noxa, Cyt C, and DR5. Moreover, treatment with MZB triggered endoplasmic reticulum (ER) stress, as shown by increased expressions of GRP78, IRE1α, p-EIF2α, p-SAPK/JNK, CHOP, ATF6α, and ATF4. On the contrary, overproduction of ROS or increased expressions of ERO1α, LC3 II, Beclin 1, and ATG5 were not detected, suggesting that neither oxidative stress nor autophagy were involved in the process of MZB-induced cell death. Thus, marizomib represents a potentially promising compound for facilitating further progress in brain cancer therapy. Full article
(This article belongs to the Special Issue Targeting Apoptosis as a Strategy for Developing New Drugs)
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14 pages, 2458 KiB  
Article
Researching New Drug Combinations with Senolytic Activity Using Senescent Human Lung Fibroblasts MRC-5 Cell Line
by Maria Carolina Ximenes de Godoy, Juliana Alves Macedo and Alessandra Gambero
Pharmaceuticals 2024, 17(1), 70; https://doi.org/10.3390/ph17010070 - 4 Jan 2024
Cited by 2 | Viewed by 2717
Abstract
Therapeutically targeting senescent cells seems to be an interesting perspective in treating chronic lung diseases, which are often associated with human aging. The combination of the drug dasatinib and the polyphenol quercetin is used in clinical trials as a senolytic, and the first [...] Read more.
Therapeutically targeting senescent cells seems to be an interesting perspective in treating chronic lung diseases, which are often associated with human aging. The combination of the drug dasatinib and the polyphenol quercetin is used in clinical trials as a senolytic, and the first results point to the relief of physical dysfunction in patients with idiopathic pulmonary fibrosis. In this work, we tested new combinations of drugs and polyphenols, looking for senolytic activity using human lung fibroblasts (MRC-5 cell line) with induced senescence. We researched drugs, such as azithromycin, rapamycin, metformin, FK-506, aspirin, and dasatinib combined with nine natural polyphenols, namely caffeic acid, chlorogenic acid, ellagic acid, ferulic acid, gallic acid, epicatechin, hesperidin, quercetin, and resveratrol. We found new effective senolytic combinations with dasatinib and ellagic acid and dasatinib and resveratrol. Both drug combinations increased apoptosis, reduced BCL-2 expression, and increased caspase activity in senescent MRC-5 cells. Ellagic acid senolytic activity was more potent than quercetin, and resveratrol counteracted inflammatory cytokine release during senolysis in vitro. In conclusion, dasatinib and ellagic acid and dasatinib and resveratrol present in vitro senolytic potential like that observed for the combination in clinical trials of dasatinib and quercetin, and maybe they could be future alternatives in the senotherapeutic field. Full article
(This article belongs to the Special Issue Targeting Apoptosis as a Strategy for Developing New Drugs)
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