“CLipP”ing on lipids to generate antibacterial lipopeptides

We herein report the synthesis and biological and computational evaluation of 12 linear analogues of the cyclic lipopeptide battacin, enabled by Cysteine Lipidation on a Peptide or Amino Acid (CLipPA) technology. Several of the novel “CLipP”ed lipopeptides exhibited low micromolar MICs and MBCs agai...

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Detalles Bibliográficos
Autores principales: Yim, Victor, Kavianinia, Iman, Knottenbelt, Melanie K., Ferguson, Scott A., Cook, Gregory M., Swift, Simon, Chakraborty, Aparajita, Allison, Jane R., Cameron, Alan J., Harris, Paul W. R., Brimble, Margaret A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2020
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8159387/
https://www.ncbi.nlm.nih.gov/pubmed/34094080
http://dx.doi.org/10.1039/d0sc01814g
Descripción
Sumario:We herein report the synthesis and biological and computational evaluation of 12 linear analogues of the cyclic lipopeptide battacin, enabled by Cysteine Lipidation on a Peptide or Amino Acid (CLipPA) technology. Several of the novel “CLipP”ed lipopeptides exhibited low micromolar MICs and MBCs against both Gram-negative and Gram-positive bacteria. The mechanism of action was then simulated with the MIC data using computational methods.

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