Suramin, a drug widely used as therapeutic agent and in research, inhibits translation in eukaryotic cell-free systems from rabbit reticulocyte lysate (IC50=142-241 microM). Suramin affects both initiation (block of 43 S pre-initiation complex formation) and elongation (impairment of poly(U) translation). The drug induces an increase in the pools of ribosomal subunits and the formation of high molecular weight ribosomal complexes, thus causing the disappearance of polysomes. Ribosomes isolated from suramin-treated translating mixtures are inactivated. [3H]Suramin binds to ribosomes and to isolated 60 S and 40 S ribosomal subunits (116, 106 and 3 binding sites, respectively) showing higher affinity for the small subunit (Kd=2 microM).
M. Brigotti, Alfieri R.R., Petronini P.G., Carnicelli D. (2006). Inhibition by suramin of protein synthesis in vitro. Ribosomes as the target of the drug. BIOCHIMIE, 88, 497-503 [10.1016/j.biochi.2005.10.009].
Inhibition by suramin of protein synthesis in vitro. Ribosomes as the target of the drug
BRIGOTTI, MAURIZIO;CARNICELLI, DOMENICA
2006
Abstract
Suramin, a drug widely used as therapeutic agent and in research, inhibits translation in eukaryotic cell-free systems from rabbit reticulocyte lysate (IC50=142-241 microM). Suramin affects both initiation (block of 43 S pre-initiation complex formation) and elongation (impairment of poly(U) translation). The drug induces an increase in the pools of ribosomal subunits and the formation of high molecular weight ribosomal complexes, thus causing the disappearance of polysomes. Ribosomes isolated from suramin-treated translating mixtures are inactivated. [3H]Suramin binds to ribosomes and to isolated 60 S and 40 S ribosomal subunits (116, 106 and 3 binding sites, respectively) showing higher affinity for the small subunit (Kd=2 microM).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
