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Antibiotics
Special Issues
New Approaches in Antimicrobial Drug Discovery and Design
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New Approaches in Antimicrobial Drug Discovery and Design

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: 31 August 2024 | Viewed by 2062

Special Issue Editor

Prof. Dr. Robert Penchovsky

E-Mail Website
Guest Editor
Department of Genetics, Faculty of Biology, Sofia University St. Kliment Ohridski, 8 Dragan Tzankov Blvd, 1164 Sofia, Bulgaria
Interests: ribozymes; riboswitches; bioinformatics; biosensors; microfluidics; DNA/RNA computing; RNA synthetic biology; rational drug design

Special Issue Information

Dear Colleagues,

The rise of multi-drug-resistant human pathogenic bacteria found in many infectious diseases worldwide is a global problem recognized by the World Health Organization. To confront this global health threat, we must develop novel strategies for improved antibacterial drug development that are prompt, accurate, and consequently more efficient. Such approaches can be based on genome-wide bioinformatics analyses and systems biology for the in silico evaluation of new targets for antibacterial drug development. In addition, various synthetic biology tools can be employed to rationalize new antibacterial drug agents. Therefore, the main subject of this Special Issue includes novel approaches for antibacterial drug development based on novel drug targets, mechanisms of action, rational drug design, in silico drug target evaluation using bioinformatics and AI-based methods, etc. 

Prof. Dr. Robert Penchovsky
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Antibiotics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • rational drug design
  • multi-drug resistant human pathogenic bacteria
  • new antibiotics
  • antibacterial drugs
  • antibacterial drug targets
  • in silico drug target evaluation

Published Papers (1 paper)

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Review

25 pages, 1701 KiB  
Review
Targeting FMN, TPP, SAM-I, and glmS Riboswitches with Chimeric Antisense Oligonucleotides for Completely Rational Antibacterial Drug Development
by Nikolet Pavlova, Martina Traykovska and Robert Penchovsky
Antibiotics 2023, 12(11), 1607; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics12111607 - 8 Nov 2023
Cited by 2 | Viewed by 1544
Abstract
Antimicrobial drug resistance has emerged as a significant challenge in contemporary medicine due to the proliferation of numerous bacterial strains resistant to all existing antibiotics. Meanwhile, riboswitches have emerged as promising targets for discovering antibacterial drugs. Riboswitches are regulatory elements in certain bacterial [...] Read more.
Antimicrobial drug resistance has emerged as a significant challenge in contemporary medicine due to the proliferation of numerous bacterial strains resistant to all existing antibiotics. Meanwhile, riboswitches have emerged as promising targets for discovering antibacterial drugs. Riboswitches are regulatory elements in certain bacterial mRNAs that can bind to specific molecules and control gene expression via transcriptional termination, prevention of translation, or mRNA destabilization. By targeting riboswitches, we aim to develop innovative strategies to combat antibiotic-resistant bacteria and enhance the efficacy of antibacterial treatments. This convergence of challenges and opportunities underscores the ongoing quest to revolutionize medical approaches against evolving bacterial threats. For the first time, this innovative review describes the rational design and applications of chimeric antisense oligonucleotides as antibacterial agents targeting four riboswitches selected based on genome-wide bioinformatic analyses. The antisense oligonucleotides are coupled with the cell-penetrating oligopeptide pVEC, which penetrates Gram-positive and Gram-negative bacteria and specifically targets glmS, FMN, TPP, and SAM-I riboswitches in Staphylococcus aureus, Listeria monocytogenes, and Escherichia coli. The average antibiotic dosage of antisense oligonucleotides that inhibits 80% of bacterial growth is around 700 nM (4.5 μg/mL). Antisense oligonucleotides do not exhibit toxicity in human cell lines at this concentration. The results demonstrate that these riboswitches are suitable targets for antibacterial drug development using antisense oligonucleotide technology. The approach is fully rational because selecting suitable riboswitch targets and designing ASOs that target them are based on predefined criteria. The approach can be used to develop narrow or broad-spectrum antibiotics against multidrug-resistant bacterial strains for a short time. The approach is easily adaptive to new resistance using targeting NGS technology. Full article
(This article belongs to the Special Issue New Approaches in Antimicrobial Drug Discovery and Design)
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