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Targeted Cancer Therapy: Small Molecules and Immunotherapy

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 August 2024) | Viewed by 3419

Special Issue Editor


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Guest Editor
Instituto de Medicina Molecular João Lobo Antunes, 1649-028 Lisbon, Portugal
Interests: cancer; targeted therapies; cell-surface antigens and proteins; antibodies

Special Issue Information

Dear Colleagues,

Cancer remains the second leading cause of death and morbidity worldwide, with 9.6 million deaths in 2018. Conventional cytotoxic agents have low therapeutic index and frequently display toxicity in cells. The need for innovative chemotypes and the identification of new cancer-relevant targets therefore crucial. In addition to recently developed materials and nanotechnologies, antibody–drug conjugates (ADCs) are still the current vehicles of choice for targeted delivery in Oncology. Over the last couple of years, the use of low-molecular-weight-targeted agents, used as small molecule drug conjugates (SMDCs), has slowly established as a promising alternative to overcome ADCs' limitations.

Exploiting new biomarkers for selective cancer imaging and targeted delivery of therapeutic agents (e.g., cytotoxic agents, small-molecule inhibitors, siRNA, immunomodelators) a pioneering and original means of defying several cancer types.

This Special Issue intentends to publish original and/or review articles covering the state-of-the-art and future viewpoints of targeted therapies in cancer treatment.

Prof. Dr. Marta Coimbra Marques
Guest Editor

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Keywords

  • cancer
  • selective targeted therapy
  • biomarkers
  • antibody–drug conjugates
  • small molecule drug conjugates
  • immunomodelators

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Published Papers (2 papers)

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Research

18 pages, 5379 KiB  
Article
Trastuzumab Potentiates Antitumor Activity of Thiopyrano[2,3-d]Thiazole Derivative in AGS Gastric Cancer Cells
by Piotr Roszczenko, Olga Klaudia Szewczyk-Roszczenko, Agnieszka Gornowicz, Robert Czarnomysy, Andrii Lozynskyi, Krzysztof Bielawski, Roman Lesyk and Anna Bielawska
Molecules 2024, 29(21), 5117; https://doi.org/10.3390/molecules29215117 - 30 Oct 2024
Viewed by 365
Abstract
Gastric cancer remains a significant therapeutic challenge, highlighting the need for new strategies to improve treatment efficacy. This study investigates the potential of combined therapy with the novel Thiopyrano[2,3-d]Thiazole derivative LES-6400 and the anti-HER2 antibody trastuzumab in AGS gastric cancer cells. [...] Read more.
Gastric cancer remains a significant therapeutic challenge, highlighting the need for new strategies to improve treatment efficacy. This study investigates the potential of combined therapy with the novel Thiopyrano[2,3-d]Thiazole derivative LES-6400 and the anti-HER2 antibody trastuzumab in AGS gastric cancer cells. The antitumor effects of the combined therapy were evaluated using various techniques, including the MTT assay for cell viability, [3H]-thymidine incorporation for DNA synthesis, and flow cytometry to assess apoptosis (Annexin V-FITC/PI staining), mitochondrial membrane potential (MMP), and inflammatory cytokine levels. ELISA was employed to measure the levels of IL-6, p53, and cytochrome C. The combination of LES-6400 (1 µM) and trastuzumab (10 µg/mL) demonstrated superior antitumor activity compared to monotherapy with either agent in AGS gastric cancer cells. The combination therapy enhanced apoptosis, presumably by inducing oxidative stress in the cells and disrupting mitochondrial membrane potential. Additionally, a significant increase in p53 protein levels and modulation of interleukin levels, including a marked reduction in IL-6 levels, were observed, suggesting an impact on apoptotic and inflammatory responses. These findings indicate that the combined use of LES-6400 and trastuzumab is a promising therapeutic strategy for gastric cancer, warranting further investigation into the mechanisms of action and potential clinical applications of this combined approach. Full article
(This article belongs to the Special Issue Targeted Cancer Therapy: Small Molecules and Immunotherapy)
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16 pages, 3056 KiB  
Article
A New Flavanone from Chromolaena tacotana (Klatt) R. M. King and H. Rob, Promotes Apoptosis in Human Breast Cancer Cells by Downregulating Antiapoptotic Proteins
by Gina Mendez-Callejas, Ruben Torrenegra, Diego Muñoz, Crispin Celis, Michael Roso, Jojhan Garzon, Ferney Beltran and Andres Cardenas
Molecules 2023, 28(1), 58; https://doi.org/10.3390/molecules28010058 - 21 Dec 2022
Cited by 3 | Viewed by 2227
Abstract
Chromolaena tacotana is a source of flavonoids with antiproliferative properties in human breast cancer cells, the most common neoplasm diagnosed in patients worldwide. Until now, the mechanisms of cell death related to the antiproliferative activity of its flavonoids have not been elucidated. In [...] Read more.
Chromolaena tacotana is a source of flavonoids with antiproliferative properties in human breast cancer cells, the most common neoplasm diagnosed in patients worldwide. Until now, the mechanisms of cell death related to the antiproliferative activity of its flavonoids have not been elucidated. In this study, a novel flavanone (3′,4′-dihydroxy-5,7-dimethoxy-flavanone) was isolated from the plant leaves and identified by nuclear magnetic resonance (NMR) and mass spectrometry (MS). This molecule selectively inhibited cell proliferation of triple-negative human breast cancer cell lines MDA-MB-231 and MCF-7 whit IC50 values of 25.3 μg/mL and 20.8 μg/mL, respectively, determined by MTT assays with a selectivity index greater than 3. Early and late pro-apoptotic characteristics were observed by annexin-V/7-AAD detection, accompanied by a high percentage of the Bcl-2 anti-apoptotic protein inactivated and the activation of effector Caspase-3 and/or 7 in breast cancer cells. It was verified the decreasing of XIAP more than Bcl-2 anti-apoptotic proteins expression, as well as the XIAP/Caspase-7 and Bcl-2/Bax complexes dissociation after flavanone treatment. Docking and molecular modeling analysis between the flavanone and the antiapoptotic protein XIAP suggests that the natural compound inhibits XIAP by binding to the BIR3 domain of XIAP. In this case, we demonstrate that the new flavanone isolated from leaves of Chomolaena tacotana has a promising and selective anti-breast cancer potential that includes the induction of intrinsic apoptosis by downregulation of the anti-apoptotic proteins XIAP and Bcl-2. New studies should deepen these findings to demonstrate its potential as an anticancer agent. Full article
(This article belongs to the Special Issue Targeted Cancer Therapy: Small Molecules and Immunotherapy)
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