A New and Simple Screening Tool for Antibacterial Drug Discovery

Lead Research Organisation: King's College London
Department Name: Pharmaceutical Sciences

Abstract

During a certain time period in the 70s and 80s, infections had perhaps been regarded as a medical ?problem solved?, at least in the developed world. However, many bacterial pathogens are now back with a vengeance ? and our lines of defence are weak. Despite the emergence of multidrug-resistant, bacterial pathogens like MRSA (methicillin-resistant S. aureus) and the resurgence of killers such as tuberculosis, only 13 new antibiotics have entered the market in the past decade. And there isn?t much else in the pipeline either.
In this project, we are developing tools to explore a new strategy for throwing a ?spanner? in the bacterial works. We are looking at a large class of bacterial enzymes ? part of the machinery bacteria use to cover themselves with a protective coat ? which has not previously been explored for antibacterial drug development. We are developing tools to explore a new strategy for punching holes in the protective coat of bacteria, which may ultimately lead to the development of novel antibacterial agents.

Technical Summary

The emergence of multidrug-resistant, bacterial pathogens like MRSA (methicillin-resistant S. aureus), the resurgence of infectious diseases such as tuberculosis, which had been close to eradication only a few decades ago, and the growing threat from bioterrorism have created an urgent need for the development of novel antibacterial therapeutics. In this project, a simple inhibitor screening assay will be developed and validated, to explore the potential of glycosyltransferases involved in the biosynthesis of the gram-negative cell wall as novel targets for antibacterial drug discovery.

Publications

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