New Small Molecule Inhibitors Used in Cancers

A special issue of Medicina (ISSN 1648-9144). This special issue belongs to the section "Oncology".

Deadline for manuscript submissions: closed (30 April 2024) | Viewed by 1212

Special Issue Editors


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Guest Editor
Institute of Biostructures and Bioimaging, National Research Council, 80145 Naples, Italy
Interests: solid tumors; tyrosine kinase receptors; oncogene drivers; targeted therapies; drug resistance; EMT; cancer stem cell pathways; tumor invasion; molecular imaging in cancer

E-Mail Website
Guest Editor
Institute of Biostructures and Bioimaging, National Research Council, 80145 Naples, Italy
Interests: warburg effect; oncogene-driven tumors; glycolytic and mitochondrial protein kinases; apoptosis; 18F-FDG imaging in cancer; drug resistance; cellular redox homeostasis; DNA damage

Special Issue Information

Dear Colleagues,

Over the past few years, a broad spectrum of small molecules has been developed for anticancer agents and approved for the treatment of several types of tumor. In particular, small-molecule-targeted drugs show advantages in some clinical aspects, such as pharmacokinetic (PK) properties, lower toxicity than chemotherapy, costs, and patient compliance. The targets of such molecules cover large class of receptors, epigenetic regulatory proteins, and DNA damage repair enzymes and proteasomes. The aim of this Special Issue is to present innovative and scientifically robust manuscript to promote advances in personalized cancer therapy, in addition to comprehensive reviews showing the challenges and future perspectives in the field.

Dr. Francesca Iommelli
Dr. Viviana De Rosa
Guest Editors

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Keywords

  • small molecules
  • targeted cancer therapy
  • drug resistance
  • oncogenes

Published Papers (1 paper)

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Research

23 pages, 3739 KiB  
Article
A Preliminary Report Regarding the Morphological Changes of Nano-Enabled Pharmaceutical Formulation on Human Lung Carcinoma Monolayer and 3D Bronchial Microtissue
by Cătălin Prodan-Bărbulescu, Claudia-Geanina Watz, Elena-Alina Moacă, Alexandra-Corina Faur, Cristina-Adriana Dehelean, Flaviu Ionut Faur, Laura Octavia Grigoriţă, Anca Laura Maghiari, Paul Tuţac, Ciprian Duţă, Sorin Bolintineanu and Laura Andreea Ghenciu
Medicina 2024, 60(2), 208; https://doi.org/10.3390/medicina60020208 - 25 Jan 2024
Cited by 2 | Viewed by 1003
Abstract
Background and Objectives: Nowadays, the development of enabled pharmaceutical nanoparticles of solid lipid type is continuously growing, because they have the potential to be used for targeted drug release leading to an increased effect of chemotherapy, being used in lung cancer nano-diagnosis [...] Read more.
Background and Objectives: Nowadays, the development of enabled pharmaceutical nanoparticles of solid lipid type is continuously growing, because they have the potential to be used for targeted drug release leading to an increased effect of chemotherapy, being used in lung cancer nano-diagnosis and nano-therapy. The current study reports the preliminary results obtained regarding the biological effect of a new nano-enabled pharmaceutical formulation in terms of its cytotoxic and biosafety profile. Materials and Methods: The pharmaceutical formulations consist of solid lipid nanoparticles (SLN) obtained via the emulsification–diffusion method by loading green iron oxide nanoparticles (green-IONPs) with a pentacyclic triterpene (oleanolic acid—OA). Further, a complex biological assessment was performed, employing three-dimensional (3D) bronchial microtissues (EpiAirwayTM) to determine the biosafety profile of the SLN samples. The cytotoxic potential of the samples was evaluated on human lung carcinoma, using an in vitro model (A549 human lung carcinoma monolayer). Results: The data revealed that the A549 cell line was strongly affected after treatment with SLN samples, especially those that contained OA-loaded green-IONPs obtained with Ocimum basilicum extract (under 30% viability rates). The biosafety profile investigation of the 3D normal in vitro bronchial model showed that all the SLN samples negatively affected the viability of the bronchial microtissues (below 50%). As regards the morphological changes, all the samples induce major changes such as loss of the surface epithelium integrity, loss of epithelial junctions, loss of cilia, hyperkeratosis, and cell death caused by apoptosis. Conclusions: In summary, the culprit for the negative impact on viability and morphology of 3D normal bronchial microtissues could be the too-high dose (500 µg/mL) of the SLN sample used. Nevertheless, further adjustments in the SLN synthesis process and another complex in vitro evaluation will be considered for future research. Full article
(This article belongs to the Special Issue New Small Molecule Inhibitors Used in Cancers)
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