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Design and Synthesis of Novel Drugs for the Treatment of Cancer

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

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 3244

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Centre of Chemistry (CQUM), Campus de Gualtar, University of Minho, 4710-057 Braga, Portugal
Interests: metal-catalyzed reactions (cross-couplings, C-H activation, and carbonylations); nucleophilic aromatic substitution; heterocycles of N and/or S; antitumoral compounds
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Special Issue Information

Dear colleagues,

Cancer treatment is still a very demanding, important issue in human health, and during the last few years, there has been continuous progress in the development of anticancer drugs.

The overexpression of some proteins of known 3D structures, such as transmembrane receptors with intracellular enzymatic domains and others, makes them special targets in cancer cells, promoting the design and discovery of new drugs, using structure-based drug design (SBDD) that can minimize the effects of toxicity on healthy cells. Multidrug resistance (MDR) in cancer treatment is also an important problem to overcome.

In this Special Issue, researchers can share their experiences and discoveries in this promising field focused on the design and development of new potential anticancer molecules, including the biological studies performed.

Contributions to this issue may cover all aspects of new discovery and development of novel therapeutic agents for cancer.

Prof. Dr. Maria João Queiroz
Guest Editor

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Published Papers (1 paper)

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Research

19 pages, 5831 KiB  
Article
Doxorubicin- and Trastuzumab-Modified Gold Nanoparticles as Potential Multimodal Agents for Targeted Therapy of HER2+ Cancers
by Kinga Żelechowska-Matysiak, Kamil Wawrowicz, Mateusz Wierzbicki, Tadeusz Budlewski, Aleksander Bilewicz and Agnieszka Majkowska-Pilip
Molecules 2023, 28(6), 2451; https://doi.org/10.3390/molecules28062451 - 7 Mar 2023
Cited by 5 | Viewed by 2897
Abstract
Recently, targeted nanoparticles (NPs) have attracted much attention in cancer treatment due to their high potential as carriers for drug delivery. In this article, we present a novel bioconjugate (DOX–AuNPs–Tmab) consisting of gold nanoparticles (AuNPs, 30 nm) attached to chemotherapeutic agent doxorubicin (DOX) [...] Read more.
Recently, targeted nanoparticles (NPs) have attracted much attention in cancer treatment due to their high potential as carriers for drug delivery. In this article, we present a novel bioconjugate (DOX–AuNPs–Tmab) consisting of gold nanoparticles (AuNPs, 30 nm) attached to chemotherapeutic agent doxorubicin (DOX) and a monoclonal antibody, trastuzumab (Tmab), which exhibited specific binding to HER2 receptors. The size and shape of synthesized AuNPs, as well as their surface modification, were analyzed by the TEM (transmission electron microscopy) and DLS (dynamic light scattering) methods. Biological studies were performed on the SKOV-3 cell line (HER2+) and showed high specificity of binding to the receptors and internalization capabilities, whereas MDA-MB-231 cells (HER2−) did not. Cytotoxicity experiments revealed a decrease in the metabolic activity of cancer cells and surface area reduction of spheroids treated with DOX–AuNPs–Tmab. The bioconjugate induced mainly cell cycle G2/M-phase arrest and late apoptosis. Our results suggest that DOX–AuNPs–Tmab has great potential for targeted therapy of HER2-positive tumors. Full article
(This article belongs to the Special Issue Design and Synthesis of Novel Drugs for the Treatment of Cancer)
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