Structure-based design of agents targeting the bacterial ribosome.
作者： Justin Bower , Martin Drysdale , Richard Hebdon , Allan Jordan , Georg Lentzen
DOI: 10.1016/S0960-894X(03)00495-5
关键词: Translation (biology) 、 Chemistry 、 Ribosomal protein 、 Protein synthesis inhibitor 、 Biochemistry 、 Thiostrepton 、 Ribosome 、 Protein biosynthesis 、 Binding domain 、 Antibacterial agent
摘要: Rational structure-based drug design has been applied to the antibiotic thiostrepton, in an attempt overcome some of its' limitations. The identification a proposed binding fragment allowed construction number key fragments, which were derivatised generate library potential antibiotics. These then evaluated determine their ability bind L11 domain prokaryotic ribosome and inhibit bacterial protein translation.
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