A Fluorescent Teixobactin Analogue.

ABSTRACT: This report describes the first synthesis and application of a fluorescent teixobactin analogue that exhibits antibiotic activity and binds to the cell walls of Gram-positive bacteria. The teixobactin analogue, Lys(Rhod)₉,Arg₁₀-teixobactin, has a fluorescent tag at position 9 and an arginine in place of the natural allo-enduracididine residue at position 10. The fluorescent teixobactin analogue retains partial antibiotic activity, with minimum inhibitory concentrations of 4-8 μg/mL across a panel of Gram-positive bacteria, as compared to 1-4 μg/mL for the unlabeled Arg₁₀-teixobactin analogue. Lys(Rhod)₉,Arg₁₀-teixobactin is prepared by a regioselective labeling strategy that labels Lys₉ with an amine-reactive rhodamin

SUBMITTER: Morris MA 

PROVIDER: S-EPMC7814985 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature