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Top journal recognises MWC anti-TB research

7 March 2018

Maurice Wilkins Centre researchers and colleagues who synthesised a potent anti-tubercular (TB) compound have had their long hours in the lab recognised in leading chemistry journal Angewandte Chemie.

Distinguished Professor Margaret Brimble and PhD student Shengping Zhang, together with Maurice Wilkins Centre investigators Dr Paul Harris and Professor Greg Cook, and colleagues, completed the first ever synthesis of callyaerin A, a naturally occurring product with strong potential as an agent for combatting TB.

Importantly, their achievement in the lab resulted in Angewandte Chemie selecting their research manuscript for very important paper (VIP) status and a cover page for the printed version. The results were evaluated as ‘highly important’ or ‘very important’ by the referees, and less than 10% of Angewandte Chemie manuscripts receive such a positive review.

 

 

TB is a highly contagious airborne disease caused by the bacterium Mycobacterium tuberculosis and is a leading cause of death globally.

Callyaerin A has been shown to have high levels of potency against M. tuberculosis and is a cyclic peptide with a unique structure, including a rare (Z)-2,3-diaminoacrylamide motif.

Distinguished Professor Brimble praised the team’s work.

“It's the first synthesis of a naturally occurring peptide active against TB containing that particularly challenging structural feature. So that in itself was a significant chemistry feat,” she said.

The team used an in vitro system to show that the synthetic peptide had potent anti-TB activity and that the (Z)-2,3-diaminoacrylamide motif was critical for this activity.

Reference

"Total Synthesis and Conformational Study of Callyaerin A: Anti-Tubercular Cyclic Peptide Bearing a Rare Rigidifying (Z)-2,3- Diaminoacrylamide Moiety" S. Zhang, L. M. De Leon Rodriguez, I. K. H. Leung, G. M. Cook, P. W. R. Harris, M. A. Brimble, Angewandte Chemie International Edition, 2018, doi:10.1002/anie.201712792