RECENT PUBLICATION: A 17-mer Membrane-Active MSI-78 Derivative with Improved Selectivity toward Bacterial Cells

INEB researchers recently published an article in the Molecular Pharmaceutics, accepted in June 11, 2015. The article is entitled "A 17-mer Membrane-Active MSI-78 Derivative with Improved Selectivity toward Bacterial Cells." and is authored by Claudia Monteiro, Marina Pinheiro, Mariana Fernandes, Sílvia Maia, Catarina L. Seabra, Frederico Ferreira-da-Silva, Salette Reis, Paula Gomes, and M. Cristina L. Martins.

Antimicrobial peptides are widely recognized as an excellent
alternative to conventional antibiotics. MSI-78, a highly effective and broad
spectrum AMP, is one of the most promising AMPs for clinical application.
In this study, we have designed 17-mer derivatives of MSI-78 with the aim of
improving selectivity while maintaining antimicrobial activity.

Despite the truncations made, we found a
17-mer peptide, MSI-78(4−20) (KFLKKAKKFGKAFVKIL), which 
demonstrated to be as effective as MSI-78 against the Gram-positive
Staphylococcus strains tested and the Gram-negative Pseudomonas aeruginosa.
This shorter derivative is more selective toward bacterial cells, representing an improved version of
the lead peptide. Biophysical studies support a mechanism of action for
MSI-78(4−20) based on the loss of membrane integrity.