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The Discovery, Synthesis and Development of Cancer Therapeutic Agents

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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: closed (15 September 2023) | Viewed by 8931

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Special Issue Editors

Dr. Po-Lin Liao

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Guest Editor

Institute of Food Safety and Health Risk Assessment, School of Pharmaceutical Sciences, National Yang Ming Chiao Tung University, Taipei 112, Taiwan
Interests: nanomaterials; food toxicology; PAHs; colorectal cancer

Prof. Dr. Tsung-Yun Liu

E-Mail Website
Guest Editor

Institute of Environmental and Occupational Health Sciences, National Yang Ming Chiao Tung University, Taipei 112, Taiwan
Interests: toxicology; metabolomics; betel quid and oral cancer

Special Issue Information

Dear Colleagues,

Cancer accounts for a major public health and economic burden. Despite advances in the diagnostic, medical, and drug discovery fields, cancer remains a leading cause of death worldwide. Carcinogenesis is a multistep process, which allows intervention with natural or synthetic agents to stop or reverse the pathological process. Therefore, researchers are encouraged to focus on discovering novel agents to cancer treatment involving the pathophysiology of the diseases, the discovery of the human genome sequence, and new molecular targets that kill cancer cells. Since most cancer is not curable in an advanced stage, chemopreventive agents are also encouraged. The scope of the Special Issue is to collect any preclinical studies targeting all types of cancer. Therefore, authors are invited to submit original research and review articles which address the progress and current standing of cancer therapeutic agents. Topics of this Special Issue include but are not limited to:

Synthesis and evaluation of new cancer therapeutic agents in vitro and in vivo;
Pre-clinical studies on new cancer therapeutic agents;
Mechanism of action.

Dr. Po-Lin Liao
Prof. Dr. Tsung-Yun Liu
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

alkylating and related agents
antimetabolites
cytotoxic antibiotics
plant derivatives
combination chemotherapy regimens
target therapy agents
other agents being proved to have pharmacological potential targeting cancers

Published Papers (4 papers)

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Research

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16 pages, 2535 KiB

Open AccessArticle

Exploring BenzylethoxyAryl Urea Scaffolds for Multitarget Immunomodulation Therapies

by Raquel Gil-Edo, German Hernández-Ribelles, Santiago Royo, Natasha Thawait, Alan Serrels, Miguel Carda and Eva Falomir

Int. J. Mol. Sci. 2023, 24(10), 8582; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24108582 - 11 May 2023

Cited by 1 | Viewed by 1403

Abstract

Thirteen benzylethoxyaryl ureas have been synthesized and biologically evaluated as multitarget inhibitors of VEGFR-2 and PD-L1 proteins to overcome resistance phenomena offered by cancer. The antiproliferative activity of these molecules on several tumor cell lines (HT-29 and A549), on the endothelial cell line HMEC-1, on immune cells (Jurkat T) and on the non-tumor cell line HEK-293 has been determined. Selective indexes (SI) have been also determined and compounds bearing p-substituted phenyl urea unit together with a diaryl carbamate exhibited high SI values. Further studies on these selected compounds to determine their potential as small molecule immune potentiators (SMIPs) and as antitumor agents have been performed. From these studies, we have concluded that the designed ureas have good tumor antiangiogenic properties, exhibit good inhibition of CD11b expression, and regulate pathways involved in CD8 T-cell activity. These properties suggest that these compounds could be potentially useful in the development of new cancer immune treatments. Full article

(This article belongs to the Special Issue The Discovery, Synthesis and Development of Cancer Therapeutic Agents)

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17 pages, 9565 KiB

Open AccessArticle

Engineering a HER2-CAR-NK Cell Secreting Soluble Programmed Cell Death Protein with Superior Antitumor Efficacy

by Wenjiao Xia, Jiaxin Chen, Wenqing Hou, Junsheng Chen, Ying Xiong, Hongyan Li, Xin Qi, Hui Xu, Zuoquan Xie, Mingfeng Li, Xiaomin Zhang and Jing Li

Int. J. Mol. Sci. 2023, 24(7), 6843; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24076843 - 06 Apr 2023

Cited by 7 | Viewed by 2682

Abstract

A new therapy strategy for relapsing patients who have received trastuzumab treatment urgently needs to be explored. HER2-specific chimeric antigen receptor (CAR)-expressing NK cells are being rapidly developed for solid tumor therapy, as they have many advantages over HER2-CAR-T cells. Endogenous soluble PD-1 (sPD-1) from the PD-1 extracellular domain blocks PD-1/PD-L1 interaction to promote cancer immunology. Herein, we engineered a new HER2-CAR-NK cell that co-expresses sPD-1 (designed as sPD-1-CAR-NK cells) and assessed its cytotoxic activities toward various cancer cells, activation of immunity and sPD-1 release in vitro and in mouse models bearing breast cancer cells with high HER2 expression, with or without trastuzumab resistance. We demonstrated that sPD-1-CAR-NK cells were able to release bioactive sPD-1, thereby enhancing the cytolytic activities of HER2-CAR-NK cells against HER2 and PD-L1 highly expressing target cells accompanied by increases in the secretion of perforin, granzyme B and IFN-γ. In vivo, sPD-1-CAR-NK cells had superior immunological anticancer efficacy compared to HER2-CAR-NK cells, and they had advantages over HER2-CAR-NK cells in the intraperitoneal injection of sPD-1. Moreover, the infiltration and activation of NK and T cells into tumor tissue were increased in mice with sPD-1-CAR-NK cells. There was no significant change in the body temperature, organ tissue and body weight in all groups except for the group with the PD-1 injection. Together, these data indicate that HER2-specific sPD-1-CAR-NK cells can transport sPD-1 into cancer tissues with high HER2 expression, further improving the efficacy of HER-CAR-NK cells without obvious side effects. sPD-1-CAR-NK is a promising cytotherapeutic agent for patients bearing HER2-positive breast cancer, including those with trastuzumab resistance. Full article

(This article belongs to the Special Issue The Discovery, Synthesis and Development of Cancer Therapeutic Agents)

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20 pages, 1717 KiB

Open AccessArticle

Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity

by Goran Poje, Marina Marinović, Kristina Pavić, Marija Mioč, Marijeta Kralj, Lais Pessanha de Carvalho, Jana Held, Ivana Perković and Zrinka Rajić

Int. J. Mol. Sci. 2022, 23(16), 9315; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23169315 - 18 Aug 2022

Cited by 8 | Viewed by 1737

Abstract

Cancer and malaria are both global health threats. Due to the increase in the resistance to the known drugs, research on new active substances is a priority. Here, we present the design, synthesis, and evaluation of the biological activity of harmicens, hybrids composed of covalently bound harmine/β-carboline and ferrocene scaffolds. Structural diversity was achieved by varying the type and length of the linker between the β-carboline ring and ferrocene, as well as its position on the β-carboline ring. Triazole-type harmicens were prepared using Cu(I)-catalyzed azide-alkyne cycloaddition, while the synthesis of amide-type harmicens was carried out by applying a standard coupling reaction. The results of in vitro biological assays showed that the harmicens exerted moderate antiplasmodial activity against the erythrocytic stage of P. falciparum (IC₅₀ in submicromolar and low micromolar range) and significant and selective antiproliferative activity against the MCF-7 and HCT116 cell lines (IC₅₀ in the single-digit micromolar range, SI > 5.9). Cell localization experiments showed different localizations of nonselective harmicene 36 and HCT116-selective compound 28, which clearly entered the nucleus. A cell cycle analysis revealed that selective harmicene 28 had already induced G1 cell cycle arrest after 24 h, followed by G2/M arrest with a concomitant drastic reduction in the percentage of cells in the S phase, whereas the effect of nonselective compound 36 on the cell cycle was much less pronounced, which agreed with their different localizations within the cell. Full article

(This article belongs to the Special Issue The Discovery, Synthesis and Development of Cancer Therapeutic Agents)

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Review

Jump to: Research

17 pages, 1339 KiB

Open AccessReview

Recent Developments in Combination Chemotherapy for Colorectal and Breast Cancers with Topoisomerase Inhibitors

by Jung Yoon Jang, Donghwan Kim and Nam Deuk Kim

Int. J. Mol. Sci. 2023, 24(9), 8457; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24098457 - 08 May 2023

Cited by 8 | Viewed by 2517

Abstract

DNA topoisomerases are important enzymes that stabilize DNA supercoiling and resolve entanglements. There are two main types of topoisomerases in all cells: type I, which causes single-stranded DNA breaks, and type II, which cuts double-stranded DNA. Topoisomerase activity is particularly increased in rapidly dividing cells, such as cancer cells. Topoisomerase inhibitors have been an effective chemotherapeutic option for the treatment of several cancers. In addition, combination cancer therapy with topoisomerase inhibitors may increase therapeutic efficacy and decrease resistance or side effects. Topoisomerase inhibitors are currently being used worldwide, including in the United States, and clinical trials on the combination of topoisomerase inhibitors with other drugs are currently underway. The primary objective of this review was to comprehensively analyze the current clinical landscape concerning the combined application of irinotecan, an extensively investigated type I topoisomerase inhibitor for colorectal cancer, and doxorubicin, an extensively researched type II topoisomerase inhibitor for breast cancer, while presenting a novel approach for cancer therapy. Full article

(This article belongs to the Special Issue The Discovery, Synthesis and Development of Cancer Therapeutic Agents)

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