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Anticancer Drug Development and Cancer Immunotherapy

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

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 14874

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Special Issue Editors

Dr. Dharmendra Kumar Yadav

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Guest Editor

College of Pharmacy, Gachon University of Medicine and Science, Room # 502, Hambakmoeiro 191, Yeonsu-gu, Incheon City 21924, Korea
Interests: cheminformatics; machine learning; bioinformatics; plasma medicine
Special Issues, Collections and Topics in MDPI journals

Dr. Paolo Coghi

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Guest Editor

School of Pharmacy, Macau University of Science and Technology, Macau 999078, China
Interests: infectious disease; malaria; virus; cancer; medicinal chemistry; natural compounds
Special Issues, Collections and Topics in MDPI journals

Dr. Xingxing Fan

E-Mail Website
Guest Editor

Neher's Biophysics Laboratory for Innovative Drug Discovery, Macau University of Science and Technology, Macao, China
Interests: molecular pharmacology; cancer immunotherapy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is a leading cause of death. Around 12.7 million cases and 7.6 million deaths occurred in 2008, and was increased to 19.3 million cases and 10 million deaths (around 13% of all deaths) in 2020. The increase not only reflects an increasing and aging population, but also the remarkable difficulties of curing the disease. It is expected that annual cancer cases will rise to 22 million within the next two decades.

Current regimens are protracted, and the narrow therapeutic index of many agents results in substantial degradation to patient well-being outside of causes due to disease effects in general.

The development of multidrug-resistance to anticancer drugs is the main cause of failure in chemotherapy during the treatment of cancer (e.g., lung, colon, breast). Furthermore, chemotherapy is not broadly effective in eradicating the disease and, on cessation of treatment, the disease may recur, and become more refractory to subsequent treatment. The development of resistance (MDR, multidrug resistance) is a substantial problem in the treatment of cancer.

Cancer immunotherapy is important field of oncology, including monoclonal antibodies, cancer vaccines, and inhibitors checkpoints.

The focus of this Special Issue is on the synthesis, computational studies, and molecular mechanism of action (MOA) analysis of novel antitumor drugs and moreover and on the link between biological reactivity and the chemical structure of the molecules. It also focusses on recent immunotherapy approaches, novel immune therapeutics, and immunology signaling pathways in cancer. This issue will also provide an understanding of the biologic context in which targets are selected for oncology drug discovery.

Experimental papers, review article,s and commentaries are all welcome.

Areas of interest include, but are not limited to:

Anticancer drugs acting via reactive oxygen species
Antitumor drugs targeting tubulin and microtubules
Alkylating agents
Natural compounds anticancer
PARP inhibitors
Drugs targeting mutant p53
Cancer precision medicine
Metabolism-modulating anti-cancer drugs
Conjugate and hybrid drugs
Prodrug-based anticancer agents
PDEPT (polymer-directed enzyme prodrug therapy)
Polymer–protein conjugates
Nuclear receptor antagonists
Cancer immunotherapy (monoclonal antibody, tumor antigen)
Antibody–drug conjugates
Inhibitors of kinases relevant to cancer: tyrosine kinases, serine–threonine kinases
Drugs acting on apoptotic signaling pathways
HSP-90 inhibitors
Photodynamic therapy
Anti-angiogenic therapy
Dual-acting anticancer drugs

Dr. Dharmendra K. Yadav
Dr. Paolo Coghi
Dr. Xingxing Fan
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
cancer drug development
cancer immunotherapy
conjugated drugs

Published Papers (6 papers)

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Research

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15 pages, 3678 KiB

Open AccessArticle

Inhibition of ANO1 by Cis- and Trans-Resveratrol and Their Anticancer Activity in Human Prostate Cancer PC-3 Cells

by Dongkyu Jeon, Minjae Jo, Yechan Lee, So-Hyeon Park, Hong Thi Lam Phan, Joo Hyun Nam and Wan Namkung

Int. J. Mol. Sci. 2023, 24(2), 1186; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24021186 - 07 Jan 2023

Cited by 7 | Viewed by 2083

Abstract

Anoctamin1 (ANO1), a calcium-activated chloride channel, is involved in the proliferation, migration, and invasion of various cancer cells including head and neck squamous cell carcinoma, lung cancer, and prostate cancer. Inhibition of ANO1 activity or downregulation of ANO1 expression in these cancer cells is known to exhibit anticancer effects. Resveratrol, a natural polyphenol abundant in wines, grapes, berries, soybeans, and peanuts, shows a wide variety of biological effects including anti-inflammatory, antioxidant, and anticancer activities. In this study, we investigated the effects of two stereoisomers of resveratrol on ANO1 activity and found that cis- and trans-resveratrol inhibited ANO1 activity with different potencies. Cis- and trans-resveratrol inhibited ANO1 channel activity with IC₅₀ values of 10.6 and 102 μM, respectively, and had no significant effect on intracellular calcium signaling at 10 and 100 μM, respectively. In addition, cis-resveratrol downregulated mRNA and protein expression levels of ANO1 more potently than trans-resveratrol in PC-3 prostate cancer cells. Cis- and trans-resveratrol significantly reduced cell proliferation and cell migration in an ANO1-dependent manner, and both resveratrol isomers strongly increased caspase-3 activity, PARP cleavage, and apoptotic sub-G1 phase ratio in PC-3 cells. These results revealed that cis-resveratrol is a potent inhibitor of ANO1 and exhibits ANO1-dependent anticancer activity against human metastatic prostate cancer PC-3 cells. Full article

(This article belongs to the Special Issue Anticancer Drug Development and Cancer Immunotherapy)

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17 pages, 1791 KiB

Open AccessArticle

Spectrofluorimetric and Computational Investigation of New Phthalimide Derivatives towards Human Neutrophil Elastase Inhibition and Antiproliferative Activity

by Beata Donarska, Marta Świtalska, Joanna Wietrzyk, Wojciech Płaziński and Krzysztof Z. Łączkowski

Int. J. Mol. Sci. 2023, 24(1), 110; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24010110 - 21 Dec 2022

Cited by 2 | Viewed by 1292

Abstract

Herein, nine phthalimide-based thiazoles (4a–4i) were synthesized and investigated as new human neutrophil elastase (HNE) inhibitors using spectrofluorimetric and computational methods. The most active compounds containing 4-trifluoromethyl (4c), 4-naphthyl (4e) and 2,4,6-trichloro (4h) substituents in the phenyl ring exhibited high HNE inhibitory activity with IC₅₀ values of 12.98–16.62 µM. Additionally, compound 4c exhibited mixed mechanism of action. Computational investigation provided a consistent picture of the ligand-receptor pattern of inter-actions, common for the whole considered group of compounds. Moreover, compounds 4b, 4c, 4d and 4f showed high antiproliferative activity against human cancer cells lines MV4-11, and A549 with IC₅₀ values of 8.21 to 25.57 µM. Additionally, compound 4g showed high activity against MDA-MB-231 and UMUC-3 with IC₅₀ values of 9.66 and 19.81 µM, respectively. Spectrophotometric analysis showed that the most active compound 4c demonstrated high stability under physiological conditions. Full article

(This article belongs to the Special Issue Anticancer Drug Development and Cancer Immunotherapy)

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15 pages, 4656 KiB

Open AccessArticle

Capability of Human Dendritic Cells Pulsed with Autologous Induced Pluripotent Stem Cell Lysate to Induce Cytotoxic T Lymphocytes against HLA-A33-Matched Cancer Cells

by Tsutomu Nakazawa, Ryosuke Maeoka, Takayuki Morimoto, Ryosuke Matsuda, Mitsutoshi Nakamura, Fumihiko Nishimura, Shuichi Yamada, Ichiro Nakagawa, Young-Soo Park, Hiroyuki Nakase and Takahiro Tsujimura

Int. J. Mol. Sci. 2022, 23(21), 12992; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232112992 - 27 Oct 2022

Cited by 1 | Viewed by 1780

Abstract

Irradiated murine induced-pluripotent stem cells (iPSCs) elicit the antitumor response in vivo. However, it is unclear whether human iPSCs would elicit antitumor effects. In the present study, we investigated the capability of human iPSC lysate (iPSL)-pulsed dendritic cells (DCs) (iPSL/DCs) to induce cancer-responsive cytotoxic T lymphocytes (CTLs) in vitro. iPSCs and DCs were induced from peripheral blood mononuclear cells isolated from a human leukocyte antigen (HLA)-A33 homozygous donor. The iPSL was pulsed with immature DCs, which were then stimulated to allow full maturation. The activated DCs were co-cultured with autologous CTLs and their responses to SW48 colorectal carcinoma cells (HLA-A32/A33), T47D breast cancer cells (HLA-A33/A33), and T98G glioblastoma cells (HLA-A02/A02) were tested with enzyme-linked immunospot (ELISPOT) assays. Comprehensive gene expression analysis revealed that the established iPSCs shared numerous tumor-associated antigens with the SW48 and T47D cells. Immunofluorescent analysis demonstrated that the fluorescent-labeled iPSL was captured by the immature DCs within 2 h. iPSL/DCs induced sufficient CTL numbers in 3 weeks for ELISPOT assays, which revealed that the induced CTLs responded to SW48 and T47D cells. Human iPSL/DCs induced cancer-responsive CTLs on HLA-A33-matched cancer cells in vitro and could be a promising universal cancer vaccine for treating and preventing cancer. Full article

(This article belongs to the Special Issue Anticancer Drug Development and Cancer Immunotherapy)

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15 pages, 29135 KiB

Open AccessArticle

Developing Bi-Gold Compound BGC2a to Target Mitochondria for the Elimination of Cancer Cells

by Qingbin Cui, Wenwen Ding, Panpan Liu, Bingling Luo, Jing Yang, Wenhua Lu, Yumin Hu, Peng Huang and Shijun Wen

Int. J. Mol. Sci. 2022, 23(20), 12169; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232012169 - 12 Oct 2022

Cited by 3 | Viewed by 1383

Abstract

Reactive oxygen species (ROS) homeostasis and mitochondrial metabolism are critical for the survival of cancer cells, including cancer stem cells (CSCs), which often cause drug resistance and cancer relapse. Auranofin is a mono-gold anti-rheumatic drug, and it has been repurposed as an anticancer agent working by the induction of both ROS increase and mitochondrial dysfunction. Hypothetically, increasing auranofin’s positive charges via incorporating more gold atoms to enhance its mitochondria-targeting capacity could enhance its anti-cancer efficacy. Hence, in this work, both mono-gold and bi-gold compounds were designed and evaluated to test our hypothesis. The results showed that bi-gold compounds generally suppressed cancer cells proliferation better than their mono-gold counterparts. The most potent compound, BGC2a, substantially inhibited the antioxidant enzyme TrxR and increased the cellular ROS. BGC2a induced cell apoptosis, which could not be reversed by the antioxidant agent vitamin C, implying that the ROS induced by TrxR inhibition might not be the decisive cause of cell death. As expected, a significant proportion of BGC2a accumulated within mitochondria, likely contributing to mitochondrial dysfunction, which was further confirmed by measuring oxygen consumption rate, mitochondrial membrane potential, and ATP production. Moreover, BGC2a inhibited colony formation and reduced stem-like side population (SP) cells of A549. Finally, the compound effectively suppressed the tumor growth of both A549 and PANC-1 xenografts. Our study showed that mitochondrial disturbance may be gold-based compounds’ major lethal factor in eradicating cancer cells, providing a new approach to developing potent gold-based anti-cancer drugs by increasing mitochondria-targeting capacity. Full article

(This article belongs to the Special Issue Anticancer Drug Development and Cancer Immunotherapy)

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Review

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11 pages, 935 KiB

Open AccessReview

Evolution of Antiretroviral Drug Rilpivirine and Approach to Oncology

by Mariana Pereira and Nuno Vale

Int. J. Mol. Sci. 2023, 24(3), 2890; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24032890 - 02 Feb 2023

Cited by 1 | Viewed by 2380

Abstract

Rilpivirine is an antiretroviral drug used to treat AIDS worldwide. The drug is a non-nucleoside reverse transcriptase inhibitor that halts the cDNA elongation process and, thus, the capacity of the HIV-1 virus to replicate. With the new wave of drug repurposing in recent years, rilpivirine has been studied in this regard. This drug is useful in Zika virus treatment, with in vivo results indicating regression in neuronal effects often associated with this infection. Several cancer types have also been researched, from breast to leukemia and pancreatic cancer, and rilpivirine has proved to have inhibitory effects in various cell lines with low concentrations, causing cellular death, apoptosis, and cell cycle arrest. The pathways are not yet established, but some works have hypothesized and demonstrated that rilpivirine causes inhibition of Aurora A kinase and has effects on the Janus kinase-signal transducer and activator of transcription (JAK-STAT) signaling pathway and the vascular endothelial growth factors-receptors (VEGFs-VEGFRs) pathway, which are known to be altered in cancer and tumors and can be targeted for cancer treatment. Further testing and clinical trials are needed, but this review demonstrates the potential of rilpivirine’s repurposing for cancer treatment. Full article

(This article belongs to the Special Issue Anticancer Drug Development and Cancer Immunotherapy)

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17 pages, 1695 KiB

Open AccessReview

The Role of Alpha-Fetoprotein (AFP) in Contemporary Oncology: The Path from a Diagnostic Biomarker to an Anticancer Drug

by Joanna Głowska-Ciemny, Marcin Szymański, Agata Kuszerska, Zbyszko Malewski, Constantin von Kaisenberg and Rafał Kocyłowski

Int. J. Mol. Sci. 2023, 24(3), 2539; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24032539 - 28 Jan 2023

Cited by 11 | Viewed by 2893

Abstract

This article presents contemporary opinion on the role of alpha-fetoprotein in oncologic diagnostics and treatment. This role stretches far beyond the already known one—that of the biomarker of hepatocellular carcinoma. The turn of the 20th and 21st centuries saw a significant increase in knowledge about the fundamental role of AFP in the neoplastic processes, and in the induction of features of malignance and drug resistance of hepatocellular carcinoma. The impact of AFP on the creation of an immunosuppressive environment for the developing tumor was identified, giving rise to attempts at immunotherapy. The paper presents current and prospective therapies using AFP and its derivatives and the gene therapy options. We directed our attention to both the benefits and risks associated with the use of AFP in oncologic therapy. Full article

(This article belongs to the Special Issue Anticancer Drug Development and Cancer Immunotherapy)

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