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Evènements I2BC

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  • Lundi 13 novembre 11:00-12:00 - Pr Brice Felden - U1230 Inserm, Pharmaceutical Biochemistry, Rennes University, Rennes, France.

    ESKAPE active antibiotics avoiding resistance development

    Résumé : Antibiotic resistance is one of the greatest threats to human health. Infections caused by bacteria with developed resistance to nearly all antibiotic classes are critically spreading. They represent a major cause of mortality and morbidity worldwide, and urgently require new compounds into clinical practice. We previously reported that a Staphylococcus aureus peptide toxin could act as a powerful antimicrobial peptide, and therefore be an attractive starting point for antibacterial drug development1. We present novel cyclic pseudomimetic antibiotics bactericidal against ESKAPE ( E nterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter spp) human multi-resistant clinical isolates, and stable in human sera. Modified, unnatural amino acids are required for stability and antibacterial activity on infected mice. These antibiotics trigger bacterial deformity, induce cell wall dissolution and alter membrane permeability. Two are active against methicillin- and vancomycin resistant Staphylococcus aureus on a mice sepsis model. Upon prolonged exposure to the antibiotics in vitro and also in infected mice, multi-resistant S. aureus did not develop resistance. The three-dimensional structure of the most active compound was solved by NMR and compared to an inactive molecule lacking modified amino acids. These novel antibiotics are currently in preclinical studies.
    1 Solecki et al. Converting a Staphylococcus aureus toxin into effective cyclic pseudopeptide antibiotics. Chem Biol. 2015, 22(3):329-35.

    Lieu : Auditorium - Bâtiment 21, campus de gif

  • Jeudi 23 novembre 11:00-12:00 - Professor Sir Tom Blundell - Department of Biochemistry , University of Cambridge, Cambridge , UK

    Multiprotein Systems, Structural Biology and Drug Discovery : Understanding Selectivity and Targeting DNA Damage Response and Repair

    Lieu : Auditorium - Bâtiment 21, Campus de Gif

  • Vendredi 8 décembre 09:00-17:00 -

    YOUR-Carreer day

    Lieu : Auditorium - Bâtiment 21, campus de Gif

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