Free or Nanoformulated Forms of Novel Protease Inhibitors for Cancer Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (20 January 2024) | Viewed by 1759

Special Issue Editor

Department of Scienze, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, Italy
Interests: ER stress; apoptosis; autophagy; proteasome inhibition; liver cancer; cell culture; biochemistry; proteomics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

I recently accepted the invitation to serve as Guest Editor for a new Special Issue of the journal Pharmaceutics on the subject of “Free or Nanoformulated Forms of Novel Protease Inhibitors for Cancer Therapy”. Many studies indicate that intracellular proteases often participate in tumor growth and progression, being involved in important biological processes such as immune and inflammatory responses, angiogenesis, proliferation, epithelial-to-mesenchymal transition (EMT) and many others. Among the anticancer strategies, the antagonization of protease activity with increasingly effective molecules is certainly an encouraging therapeutic approach, especially if formulated in nanoparticle-based delivery systems that can increase bioavailability and circulation time and allow for accumulation—specifically in tumor tissues.

This Special Issue aims to establish a collection of papers to provide cutting-edge insight into all interested in this area of research. We welcome papers in the form of full research papers or focused reviews on some aspects of the theme. If you are interested in contributing or have any questions, please do not hesitate to let us know or contact the Assistant Editor.

I look forward to receiving your contributions.

Dr. Maria Francesca Armentano
Guest Editor

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Keywords

  • human proteases
  • proteases inhibitors
  • cancer treatment
  • ubiquitin–proteasome pathway inhibitors
  • apoptosis
  • nanoscale drug-delivery systems
  • lipidic nanoparticles
  • targeting approaches

Published Papers (1 paper)

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Research

18 pages, 4635 KiB  
Article
Targeting Lactate Dehydrogenase-B as a Strategy to Fight Cancer: Identification of Potential Inhibitors by In Silico Analysis and In Vitro Screening
by Manos Vlasiou, Vicky Nicolaidou and Christos Papaneophytou
Pharmaceutics 2023, 15(10), 2411; https://doi.org/10.3390/pharmaceutics15102411 - 01 Oct 2023
Viewed by 1341
Abstract
Lactate dehydrogenase (LDH) is an enzyme that catalyzes the reversible conversion of lactate to pyruvate while reducing NAD+ to NADH (or oxidizing NADH to NAD+). Due to its central role in the Warburg effect, LDH-A isoform has been considered a [...] Read more.
Lactate dehydrogenase (LDH) is an enzyme that catalyzes the reversible conversion of lactate to pyruvate while reducing NAD+ to NADH (or oxidizing NADH to NAD+). Due to its central role in the Warburg effect, LDH-A isoform has been considered a promising target for treating several types of cancer. However, research on inhibitors targeting LDH-B isoform is still limited, despite the enzyme’s implication in the development of specific cancer types such as breast and lung cancer. This study aimed to identify small-molecule compounds that specifically inhibit LDH-B. Our in silico analysis identified eight commercially available compounds that may affect LDH-B activity. The best five candidates, namely tucatinib, capmatinib, moxidectin, rifampicin, and acetyldigoxin, were evaluated further in vitro. Our results revealed that two compounds, viz., tucatinib and capmatinib, currently used for treating breast and lung cancer, respectively, could also act as inhibitors of LDH-B. Both compounds inhibited LDH-B activity through an uncompetitive mechanism, as observed in in vitro experiments. Molecular dynamics studies further support these findings. Together, our results suggest that two known drugs currently being used to treat specific cancer types may have a dual effect and target more than one enzyme that facilitates the development of these types of cancers. Furthermore, the results of this study could be used as a new starting point for identifying more potent and specific LDH-B inhibitors. Full article
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