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.