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Image of new antibiotic in action opens up new opportunities to combat antibacterial resistance
Date:8/4/2010

Detailed pictures published today reveal how a new type of experimental antibiotic can kill bacteria that are already resistant to existing treatments [1]. The findings could ultimately help scientists to develop new antibiotics to tackle the bacteria responsible for many hospital and community-acquired infections.

Using an imaging technique called x-ray crystallography, a team of researchers from GlaxoSmithKline (GSK) captured a snapshot of the new compound latched on to the enzyme topoisomerase. This enzyme is part of the bacteria's internal machinery and helps the bacteria produce proteins and replicate. Stopping this enzyme prevents the bacteria from reproducing. Medicines, known as the quinolones, that target the enzyme have been used successfully as antibiotics since 1962, however bacteria are increasingly developing resistance to this class of drugs.

By looking at x-ray images, the team have demonstrated that the new investigational medicine attaches to the enzyme in a different place to the quinolones, enabling it to stop the same bacteria that are resistant to these older treatments. The research is published today in the journal Nature, and is the result of two unique collaborations between GSK and the Wellcome Trust's Seeding Drug Discovery initiative and the U.S. Defense Threat Reduction Agency (DTRA).

"We already knew that targeting this enzyme was clinically proven to stop bacteria in their tracks, we just needed to be a bit more inventive in how we attacked it," said Michael Gwynn, from GSK's Infectious Diseases research group. "These images and the data showing the efficacy of this compound against a range of bacteria validate our approach, demonstrating that the enzyme can still be blocked even in bacteria already resistant to other antibiotics that work against this same enzyme."

The study also reports the potency of the new compound, called GSK 299423, against antibiotic-resistant strains of bacte
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Contact: Jen Middleton
j.middleton@wellcome.ac.uk
44-207-611-7262
Wellcome Trust
Source:Eurekalert

Page: 1 2

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