Academic Journal
Semisynthetic guanidino lipoglycopeptides with potent in vitro and in vivo antibacterial activity
| العنوان: | Semisynthetic guanidino lipoglycopeptides with potent in vitro and in vivo antibacterial activity |
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| المؤلفون: | Groesen, E. van, Mons, E., Kotsogianni, I., Arts, M., Tehrani, K.H.M.E., Wade, N., Lysenko, V., Stel, F.M., Zwerus, J.T., Benedetti, S. de, Bakker, A., Chakraborty, P., Stelt, M. van der, Scheffers, D.J., Gooskens, J., Smits, W.K., Holden, K., Gilmour, P.S., Willemse, J., Hitchcock, C.A., Hasselt, J.G.C. van, Schneider, T., Martin, N.I. |
| المصدر: | Science Translational Medicine |
| سنة النشر: | 2024 |
| المجموعة: | Leiden Repository (Leiden University) |
| الوصف: | Vancomycin and its second-generation lipoglycopeptide derivatives work mainly by binding the peptidoglycan precursor lipid II to inhibit cell wall synthesis in Gram-positive bacteria. However, antibiotic resistance and safety concerns remain, and improved antibiotics are still needed. Van Groesen et al . report the optimization of a series of vancomycin-derived antibiotic compounds: lipoglycopeptides that bear a guanidino lipid group. This modification promoted stronger binding to the cell wall precursor lipid II, resulting in potent antibacterial activity while also showing less toxicity to mammalian cells than second-generation vancomycin derivatives. The lead candidate compound outperformed vancomycin in improving therapeutic outcome in mouse models of S. aureus thigh infection and sepsis, suggesting that guanidino lipoglycopeptides may benefit from further development. ; Molecular basis of bacterial pathogenesis, virulence factors and antibiotic resistance |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| Relation: | https://hdl.handle.net/1887/4107290 |
| DOI: | 10.1126/scitranslmed.abo4736 |
| الاتاحة: | https://hdl.handle.net/1887/4107290 https://doi.org/10.1126/scitranslmed.abo4736 |
| رقم الانضمام: | edsbas.9A9525DC |
| قاعدة البيانات: | BASE |
| DOI: | 10.1126/scitranslmed.abo4736 |
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