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22nd of November 2017

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Chemists Synthesize Two Simplified Forms of Superbug-Killing Antibiotic Teixobactin | Chemistry, Medicine | Sci-News.com

An international team of researchers led by the University of Lincoln, UK, has produced two simplified versions of teixobactin, a powerful natural antibiotic which many in the scientific community believe could lead to creation of the first commercially viable new antibiotic drug in three decades.

Teixobactin eliminates MRSA, Mycobacterium tuberculosis, Streptococcus pneumoniae, Bacillus anthracis and other dangerous pathogens without encountering any detectable resistance. This digitally-colorized, scanning electron microscopic image depicts green-colored, spheroid-shaped MRSA bacteria, as they were in the process of being enveloped by a much larger, human white blood cell. Image credit: National Institute of Allergy and Infectious Diseases.

Teixobactin eliminates MRSA, Mycobacterium tuberculosis, Streptococcus pneumoniae, Bacillus anthracis and other dangerous pathogens without encountering any detectable resistance. This digitally-colorized, scanning electron microscopic image depicts green-colored, spheroid-shaped MRSA bacteria, as they were in the process of being enveloped by a much larger, human white blood cell. Image credit: National Institute of Allergy and Infectious Diseases.

“When teixobactin was discovered it was ground breaking in itself as a new antibiotic which kills bacteria without detectable resistance including superbugs such as methicillin-resistant Staphylococcus aureus (MRSA),” said lead author Dr. Ishwar Singh, from the University of Lincoln’s School of Pharmacy.

“We have been investigating a way to simplify the design while retaining the high potency against resistant bacteria.”

Until now, chemists attempting to synthesize 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.

Each amino acid sits at a specific place in teixobactin’s structure, and Dr. Singh and co-authors have now successfully replaced enduracididine with two alternative amino acids which are not positively charged.

These amino acids lack the ‘binding’ part, over-turning the prior understanding that enduracididine is essential for to so-called ‘target binding’ to be highly potent against superbugs.

With this new knowledge, synthesized versions of teixobactin can be more easily developed, taking the process from up to 30 hours to just 10 minutes for a single coupling step — a significant step towards turning teixobactin into a viable new drug.

Importantly, the two new simplified forms of teixobactin have also proven to have identical potency against superbugs as the natural form of teixobactin.

“This simplified design and more efficient synthesize will enable work to be carried out at a commercial level,” Dr. Singh said.

“Enduracididine was severely limiting our ability to do this because of its scarcity, a complex multistep synthesis, and long and repetitive steps of between 16 and 30 hours with high failure rate and very low yields.”

“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 MRSA, and they were also highly potent against other antibiotic-resistant infections, such as vancomycin resistant enterococci, and tuberculosis.”

The results are published in the journal Chemical Science.

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Anish Parmar et al. Teixobactin analogues reveal enduracididine to be non-essential for highly potent antibacterial activity and lipid II binding. Chemical Science, published online October 5, 2017; doi: 10.1039/C7SC03241B

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