4 years ago

Investigation of the N-Terminus Amino Function of Arg10-Teixobactin.

Ramchuran, Noki, Albericio, Monaim, Torre, El-Faham
Teixobactin is a recently described antimicrobial peptide that shows high activity against gram-positive bacteria as well as mycobacterium tuberculosis. Due to both its structure as a head-to-side chain cyclodepsipeptide and its activity, it has attracted the attention of several research groups. In this regard, a large number of analogs with substitutions in both the cycle and the tail has been described. Here, we report the contribution of the N-terminus residue, N-Me-d-Phe, to the activity of Arg10-teixobactin. On the basis of our findings, we conclude that the N-terminus accepts minimum changes but not the presence of long alkyl chains. The presence of a positive charge is a requirement for the activity of the peptide. Furthermore, acylation of the N-terminus leads to total loss of activity.

Publisher URL: http://doi.org/10.3390/molecules22101632

DOI: 10.3390/molecules22101632

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