News

Antibiotic breakthrough

Amy Schofield 07 November 2017

Scientists working to develop a ‘game-changing’ new antibiotic have made a significant advance towards creating commercially viable drug treatments by producing two simplified synthetic versions of the substance, teixobactin, which are just as potent at killing superbugs like MRSA as its natural form.

The breakthrough, by researchers at the University of Lincoln, marks an important step towards realising the potential of teixobactin in aiding the global fight against antibiotic-resistant pathogens. Teixobactin is a recently discovered natural antibiotic which many in the international scientific community believe could lead to creation of the first commercially viable new antibiotic drug in 30 years.

The Lincoln team successfully synthesised new simplified versions of teixobactin which harness the same powerful antibiotic effects in a way that could be produced on a commercial scale.

Until now, scientists attempting to synthesise teixobactin believed they needed to use cationic (or positively charged) amino acids which bind to the bacterial target using a ‘side chain’. This meant they had to use either the very rare amino acid found naturally in teixobactin, called enduracididine, or alternative ones which had lower potency against superbugs.

The Lincoln team successfully replaced enduracididine with two alternative amino acids which are not positively charged. These amino acids lack the ‘binding’ part, overturning the prior understanding that enduracididine is essential for to so-called ‘target binding’ to be highly potent against superbugs.
 
With this new knowledge, synthesised versions of teixobactin can be more easily developed.

Research lead Dr Ishwar Singh, a specialist in novel drug design and development from the University of Lincoln’s School of Pharmacy, said: “We have discovered that we can in fact use amino acids which are structurally different, and are commercially-available. They are also 16 times more potent than a clinically-used antibiotic in killing the superbug MRSA, and they were also highly potent against other antibiotic-resistant infections, such as vancomycin resistant enterococci, and tuberculosis.”

Dr Singh is working with colleagues from the School of Life Sciences and the School of Chemistry at the University of Lincoln to develop teixobactins into a viable drug.

 

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