L’article « Lysine analogue of Polymyxin B as a significant opportunity for photodynamic antimicrobial chemotherapy. », écrit par Florent LE GUERN, , Tan Sothéa OUK, Yves CHAMPAVIER, Emilie PINAULT et Vincent SOL du Laboratoire PEIRENE, en collaboration avec Régis VANDERESSE du LRGP ENSIC de Nancy (Université de Lorraine), Catherine OUK de la plate-forme BISCEm  (Université de Limoges) a été mis à l’honneur en illustrant la couverture du mois de janvier 2018 de ACS Medicinal Chemistry Letters  https://doi.org/10.1021/acsmedchemlett.7b00360.

Résumé de l’article :

This paper reports the highlight the potential of PACT in case of infections by antibiotic resistant-strains, a new antimicrobial peptide conjugate has been synthesized, consisting of a derivative of polymyxin B and a cationic porphyrin covalently attached together to a spacer. A polymyxin-derived moiety was subjected to a primary structural modification consisting in the replacement of 4 diaminobutyrate residues with lysine ones. This modification was done in order to strongly reduce bactericidal activity, with the aim to eliminate the potential rise of polymyxin-resistant strains. Despite this modification, this new conjugate displayed a strong photobactericidal activity against Gram-positive as well as Gram-negative bacteria. It was further shown that this conjugate was able to strongly stick to the cell walls of either kind of strains, thus helping to inactivate bacteria through the production of ROS under light irradiation.

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