Drug Discovery for Infectious Diseases—Second Edition

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Drug Discovery, Development and Delivery".

Deadline for manuscript submissions: closed (31 October 2024) | Viewed by 1744

Special Issue Editors


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Guest Editor
1. Department of Pharmacology and Toxicology, University of Veterinary Medicine, István utca 2, H-1078 Budapest, Hungary
2. National Laboratory of Infectious Animal Diseases, Antimicrobial Resistance, Veterinary Public Health and Food Chain Safety, University of Veterinary Medicine, István utca 2, H-1078 Budapest, Hungary
Interests: pharmacology; drug repositioning; pharmacokinetics; antimicrobial resistance
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Pharmacology and Toxicology, University of Veterinary Medicine Budapest, Budapest, Hungary
Interests: veterinary usage of antibiotics; antimicrobial resistance; antibiotic sensitivity testing; antibiotic alternatives
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Infectious diseases encompass a wide range of diseases caused by viruses, bacteria, fungi and parasites, all of which have serious consequences for human health. The rapid emergence of new viral and parasitic diseases, as well as the spread of antimicrobial resistance, is also putting drug research at a disadvantage, posing a challenge to the biomedical research field to develop new drugs and drug innovation strategies to keep pace with these new needs. Recent pandemics in particular highlight the need for novel antiviral drugs in several areas of human and animal health.

This Special Issue welcomes reviews and papers describing host-entry and reproduction of the pathogen and pathomechanism of diseases at the molecular level, as well as those reporting on the discovery of new drug candidates that affect these processes. New mechanisms of drug action and new drug targets are esecially promising approaches, which, besides their significance, may have potential applications in other areas. Approaches based on the ‘One Health’ principle are also encouraged. Innovative drug discovery strategies, including repositioning stategies from other pharmacological areas, drug combinations or multiple-targeting ligands, as well as new drug formulations for improved ADME, also represent suitable subjects of submitted papers.

Dr. Ákos Jerzsele
Dr. Dóra Kovács
Guest Editors

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Keywords

  • human drug discovery
  • antiviral, antibacterial, antifungal, antiparasitic
  • infectious pathomechanisms
  • drug discovery strategy
  • one health principle

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Published Papers (1 paper)

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Research

17 pages, 3341 KiB  
Article
In Vitro Evaluation of Antipseudomonal Activity and Safety Profile of Peptidomimetic Furin Inhibitors
by Sara Maluck, Rivka Bobrovsky, Miklós Poór, Roman W. Lange, Torsten Steinmetzer, Ákos Jerzsele, András Adorján, Dávid Bajusz, Anita Rácz and Erzsébet Pászti-Gere
Biomedicines 2024, 12(9), 2075; https://doi.org/10.3390/biomedicines12092075 - 11 Sep 2024
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Abstract
Inhibitors of the serine protease furin have been widely studied as antimicrobial agents due to their ability to block the cleavage and activation of certain viral surface proteins and bacterial toxins. In this study, the antipseudomonal effects and safety profiles of the furin [...] Read more.
Inhibitors of the serine protease furin have been widely studied as antimicrobial agents due to their ability to block the cleavage and activation of certain viral surface proteins and bacterial toxins. In this study, the antipseudomonal effects and safety profiles of the furin inhibitors MI-1851 and MI-2415 were assessed. Fluorescence quenching studies suggested no relevant binding of the compounds to human serum albumin and α1-acid glycoprotein. Both inhibitors demonstrated significant antipseudomonal activity in Madin–Darby canine kidney cells, especially compound MI-1851 at very low concentrations (0.5 µM). Using non-tumorigenic porcine IPEC-J2 cells, neither of the two furin inhibitors induced cytotoxicity (CCK-8 assay) or altered significantly the intracellular (Amplex Red assay) or extracellular (DCFH-DA assay) redox status even at a concentration of 100 µM. The same assays with MI-2415 conducted on primary human hepatocytes also resulted in no changes in cell viability and oxidative stress at up to 100 µM. Microsomal and hepatocyte-based CYP3A4 activity assays showed that both inhibitors exhibited a concentration-dependent inhibition of the isoenzyme at high concentrations. In conclusion, this study indicates a good safety profile of the furin inhibitors MI-1851 and MI-2415, suggesting their applicability as antimicrobials for further in vivo investigations, despite some inhibitory effects on CYP3A4. Full article
(This article belongs to the Special Issue Drug Discovery for Infectious Diseases—Second Edition)
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