Teixobactin analogues reveal enduracididine to be non-essential for highly potent antibacterial activity and lipid II binding† †Electronic supplementary information (ESI) available: Peptide synthesis, HPLC, LC-MS analysis, NMR spectra, microbiological data (MIC, MBC, time kill kinetics), lipid II and geranyl pyrophosphate binding, cytotoxicity assay. See DOI: 10.1039/c7sc03241b

Autor: Parmar, Anish, Iyer, Abhishek, Prior, Stephen H., Lloyd, Daniel G., Leng Goh, Eunice Tze, Vincent, Charlotte S., Palmai-Pallag, Timea, Bachrati, Csanad Z., Breukink, Eefjan, Madder, Annemieke, Lakshminarayanan, Rajamani, Taylor, Edward J., Singh, Ishwar

Publikováno v: Chemical Science

Leu10-teixobactin and Ile10-teixobactin have shown comparable activity to natural teixobactin.
Teixobactin is a highly promising antibacterial depsipeptide consisting of four d-amino acids and a rare l-allo-enduracididine amino acid. l-allo-Endu

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http://europepmc.org/articles/PMC5855875

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Defining the molecular structure of teixobactin analogues and understanding their role in antibacterial activities.

Autor: Parmar A; School of Pharmacy, JBL Building, University of Lincoln, Beevor St., Lincoln LN6 7DL, UK. isingh@lincoln.ac.uk., Prior SH; School of Chemistry, University of Lincoln, Beevor St., Lincoln LN6 7DL, UK., Iyer A; School of Pharmacy, JBL Building, University of Lincoln, Beevor St., Lincoln LN6 7DL, UK. isingh@lincoln.ac.uk and Organic and Biomimetic Chemistry Research Group, Department of Organic Chemistry, Ghent University, Krijgslaan 281 (S4), B-9000 Ghent, Belgium., Vincent CS; School of Life Sciences, Joseph Bank Laboratories, University of Lincoln, Green Lane, Lincoln LN6 7DL, UK. etaylor@lincoln.ac.uk., Van Lysebetten D; Organic and Biomimetic Chemistry Research Group, Department of Organic Chemistry, Ghent University, Krijgslaan 281 (S4), B-9000 Ghent, Belgium., Breukink E; Department of Membrane Biochemistry and Biophysics, Institute of Biomembranes, Utrecht University, Padualaan 8, 3584 CH Utrecht, The Netherlands., Madder A; Organic and Biomimetic Chemistry Research Group, Department of Organic Chemistry, Ghent University, Krijgslaan 281 (S4), B-9000 Ghent, Belgium., Taylor EJ; School of Life Sciences, Joseph Bank Laboratories, University of Lincoln, Green Lane, Lincoln LN6 7DL, UK. etaylor@lincoln.ac.uk., Singh I; School of Pharmacy, JBL Building, University of Lincoln, Beevor St., Lincoln LN6 7DL, UK. isingh@lincoln.ac.uk.

Publikováno v: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2017 Feb 07; Vol. 53 (12), pp. 2016-2019.