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Antibiotics
Special Issues
New Antibiotic Compounds: Discovery and Strategies
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New Antibiotic Compounds: Discovery and Strategies

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

Deadline for manuscript submissions: closed (31 May 2023) | Viewed by 3822

Special Issue Editors

Dr. Florie Desriac

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Guest Editor
CBSA, Bacterial Communication and Antimicrobial Strategies, University of Caen Normandie, Caen, France
Interests: antibiotics discovery; natural products; antibiofilm; non-traditional antibacterials
Dr. Yannick Fleury

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Guest Editor
LBCM, Laboratoire de Biotechnologie et Chimie Marines Université de Brest, Quimper, France
Interests: antibiotics from marine microbiota; antibiofilm; gram negative pathogens; antimicrobial peptides
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antimicrobial resistance (AMR) is now recognized as one of the world’s biggest economic and security threats and requires a global solution that tackles the issue from different angles. Because bacteria constantly evolve to resist antibiotics they come into contact with, new antibacterial drugs or strategies are bound to renew themselves continuously, turning the antibiotic discovery field into one of the three key aspects of a global solution to tackle AMR. According to the WHO and the Pew Charitable Trusts, only 292 compounds are in the preclinical stages, and 43 antibiotics are currently in clinical trials (2021). In light of this dire need for new drugs and treatments, rethinking of the process of anti-infective discovery is needed.

This Special Issue welcomes all submissions related to antibacterial discovery. Perspectives (opinion letters) and submissions focusing on requirements to improve/accelerate antibacterial screening and hit to lead translation are encouraged.

Potential topics include but are not limited to the following:

  • Natural or synthetic antibacterial compounds;
  • Antibiotic potentiators, efflux pumps inhibitors;
  • Antivirulence, antibiofilm, and/or quorum quenchers;
  • Microbial genome mining for antibiotic discovery;
  • New strategies to enhance high throughput screening (from natural or synthetic libraries);
  • Natural products dereplication strategies;
  • Antibiotic discovery platforms.

Dr. Florie Desriac
Dr. Yannick Fleury
Guest Editors

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

  • antibiotic
  • antimicrobial
  • discovery
  • high-throughput
  • screen
  • molecule-based strategies

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Published Papers (1 paper)

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Research

15 pages, 2146 KiB  
Article
An Optimized Workflow for the Discovery of New Antimicrobial Compounds Targeting Bacterial RNA Polymerase Complex Formation
by Alessia Caputo, Sara Sartini, Elisabetta Levati, Ilaria Minato, Gian Marco Elisi, Adriana Di Stasi, Catherine Guillou, Peter G. Goekjian, Pierre Garcia, David Gueyrard, Stéphane Bach, Arnaud Comte, Simone Ottonello, Silvia Rivara and Barbara Montanini
Antibiotics 2022, 11(10), 1449; https://doi.org/10.3390/antibiotics11101449 - 21 Oct 2022
Cited by 4 | Viewed by 2958
Abstract
Bacterial resistance represents a major health problem worldwide and there is an urgent need to develop first-in-class compounds directed against new therapeutic targets. We previously developed a drug-discovery platform to identify new antimicrobials able to disrupt the protein–protein interaction between the β’ subunit [...] Read more.
Bacterial resistance represents a major health problem worldwide and there is an urgent need to develop first-in-class compounds directed against new therapeutic targets. We previously developed a drug-discovery platform to identify new antimicrobials able to disrupt the protein–protein interaction between the β’ subunit and the σ70 initiation factor of bacterial RNA polymerase, which is essential for transcription. As a follow-up to such work, we have improved the discovery strategy to make it less time-consuming and more cost-effective. This involves three sequential assays, easily scalable to a high-throughput format, and a subsequent in-depth characterization only limited to hits that passed the three tests. This optimized workflow, applied to the screening of 5360 small molecules from three synthetic and natural compound libraries, led to the identification of six compounds interfering with the β’–σ70 interaction, and thus was capable of inhibiting promoter-specific RNA transcription and bacterial growth. Upon supplementation with a permeability adjuvant, the two most potent transcription-inhibiting compounds displayed a strong antibacterial activity against Escherichia coli with minimum inhibitory concentration (MIC) values among the lowest (0.87–1.56 μM) thus far reported for β’–σ PPI inhibitors. The newly identified hit compounds share structural feature similarities with those of a pharmacophore model previously developed from known inhibitors. Full article
(This article belongs to the Special Issue New Antibiotic Compounds: Discovery and Strategies)
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