Issue 2, 2021

Modulators of protein–protein interactions as antimicrobial agents


Protein–Protein interactions (PPIs) are involved in a myriad of cellular processes in all living organisms and the modulation of PPIs is already under investigation for the development of new drugs targeting cancers, autoimmune diseases and viruses. PPIs are also involved in the regulation of vital functions in bacteria and, therefore, targeting bacterial PPIs offers an attractive strategy for the development of antibiotics with novel modes of action. The latter are urgently needed to tackle multidrug-resistant and multidrug-tolerant bacteria. In this review, we describe recent developments in the modulation of PPIs in pathogenic bacteria for antibiotic development, including advanced small molecule and peptide inhibitors acting on bacterial PPIs involved in division, replication and transcription, outer membrane protein biogenesis, with an additional focus on toxin–antitoxin systems as upcoming drug targets.

Graphical abstract: Modulators of protein–protein interactions as antimicrobial agents

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Article information

Article type
Review Article
12 Nov 2020
27 Jan 2021
First published
03 Feb 2021
This article is Open Access
Creative Commons BY license

RSC Chem. Biol., 2021,2, 387-409

Modulators of protein–protein interactions as antimicrobial agents

R. Kahan, D. J. Worm, G. V. de Castro, S. Ng and A. Barnard, RSC Chem. Biol., 2021, 2, 387 DOI: 10.1039/D0CB00205D

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