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Prof. Dr. Marta Coimbra Marques

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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

Published Papers (1 paper)

Research

16 pages, 3056 KiB

Open AccessArticle

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 2 | Viewed by 1811

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 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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