What is it about?
The small molecule ES24 shows antibacterial activity that is equivalent to and, against certain clinically relevant bacterial strains, better than that of the known antibiotic nitrofurantoin. We show that, following its activation in vivo, ES24 exerts its antibacterial activity by inhibiting the synthesis of bacterial proteins via the SecYEG translocon.
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Why is it important?
Increasing resistance to antibiotics is a public health concern. Here we demonstrate that ES24 shows enhanced antibacterial activity towards the antibiotic-resistant 'superbugs' MRSA (methicillin-resistant Staphylococcus aureus) and VRE (vancomycin-resistant enterococcus) when compared to the clinically approved antibiotic nitrofurantoin. Thus, ES24 is a promising candidate for a broad-acting, effective and much needed new antibiotic.
Perspectives
It is increasingly clear that the 'Golden Age' of antibiotics has come to an end; a feat exacerbated by the fact that research into new antibiotics has not matched the evolution of the bacteria themselves. I hope that our recent work with ES24 paves the way for its future development as an antibiotic.
Dr Sarah O'Keefe
University of Manchester
Read the Original
This page is a summary of: Eeyarestatin 24 impairs SecYEG‐dependent protein trafficking and inhibits growth of clinically relevant pathogens, Molecular Microbiology, September 2020, Wiley,
DOI: 10.1111/mmi.14589.
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