Inhibits bacterial protein biosynthesis by binding to ribosomes. Specifically, binds to the complex of 23S rRNA and ribosomal protein L11 (RPLK) in the 50S ribosomal subunit. While allowing a weak binding of elongation factor G (EF-G) to the ribosome and subsequent GTP-hydrolysis, probably impairs conformational changes in both the ribosome and EF-G which are necessary for translocation. In vitro, inhibits Gram-positive bacteria S.aureus strain 209P (MIC=0.0009 ?g,ml), S.aureus strain 133 (MIC=0.0019 ?g,ml), S.aureus strain B3 (MIC=0.003 ?g,ml), S.aureus strain Hb (MIC=0.003 ?g,ml), M.citreus strain ATCC 8411 (MIC=0.0038 ?g,ml), M.lysodeikticus strain ATCC 4698 (MIC=0.003 ?g,ml), S.lutea strain ATCC 9341 (MIC=0.0011 ?g,ml), S.faecalis strain ATCC 9790 (MIC=0.0007 ?g,ml), S.viridans (MIC=0.0065 ?g,ml), S.pyogenes hemolyticus strain Dig7 (MIC=0.00028 ?g,ml), D.pneumoniae strain Til (MIC=0.00015 ?g,ml), N.catrrhalis (MIC=0.0017 ?g,ml), L.casei strain ATCC 6633 (MIC=0.003 ?g,ml), B.cereus strain ATCC 6630 (MIC=0.0071 ?g,ml) and various isolates of L.monocytogenes. In vitro, inhibits Gram-negative bacterium P.multocida strain A125 (MIC=0.0024 ?g,ml) but not M.smegmatis strain ATCC 6630, S.typhimurium, A.aerogenes strain ATCC 8308, P.vulgaris, K.pneumoniae strain ATCC 10031, S.marcescens strain A476, P.aeruginosa strain Bass or B.bronchiseptica strain CN387. Does not inhibit Gram-negative bacterium E.coli strain ATCC 9637 but does inhibit purified ribosomes from E.coli. In vivo, has no systemic effect in mice infected with staphylococci or streptococci when applied orally or subcutaneously. Has a local effect in mice infected subcutaneously or intraperitoneally with staphylococci when applied immediately afterwards. Is not toxic to mice.
"Mapping the binding site of thiopeptide antibiotics by proximity-induced covalent capture."Baumann S., Schoof S., Harkal S.D., Arndt H.D.
J. Am. Chem. Soc. 130:5664-5666(2008)
Research Topic:Others
