thiostrepton

Thiostrepton is a natural cyclic oligopeptide antibiotic of the thiopeptide (thiopeptide antibiotic) class, originally derived from several strains of Streptomyces, including Streptomyces azureus and Streptomyces laurentii[1][2][8]. It is primarily used as a veterinary topical antimicrobial agent for mastitis and dermatologic disorders caused by gram-negative organisms, but it also exhibits activity against gram-positive bacteria[4][8]. Thiostrepton acts as an irreversible inhibitor of the bacterial ribosome by binding to nucleotides A1065 and A1095 on helices 43 and 44 of 23S rRNA, as well as proline residues within the N-terminal domain of ribosomal protein uL11. This disrupts elongation factor G (EF-G) function after GTP hydrolysis during protein synthesis, inhibiting tRNA translocation and factor dissociation from the ribosome[3][6][8]. In addition to its antibacterial effects, thiostrepton has demonstrated anti-cancer properties in vitro by targeting transcription factors such as FOXM1 in breast cancer cells and inducing apoptosis via proteasome inhibition. It has also shown potential in reversing insulin resistance ex vivo and inhibiting osteoclast precursor cells in animal models[5][8].

Other names

TST