Thiostrepton is a bactericidal macrocyclic thiopeptide antibiotic that is produced by Streptomyces azureus and was originally detailed by Donovick et al. in 1955. Thiostrepton shows broad activity against both gram-positive and gram-negative bacteria, as well as anti-plasmodial effects.
Thiostrepton inhibits prokaryotic translation by inhibiting ribosome turnover after the elongation step in protein synthesis by inhibiting both the dissociation of elongation factor G (EF-G) from the ribosome and the release of inorganic phosphate from EF-G following GTP hydrolysis. Thiostrepton has also been shown to inhibit the binding of elongation factor 4 (EF4) to the 70S ribosome.
Thiostrepton has been shown to inhibit the oncogenic transcription factor FoxM1 and is cytotoxic to malignant mesothelioma cells in a dose dependent fashion.
Thiostrepton conforms to United States Pharmacopeia specifications.
