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ID: ALA1145726

Journal: Bioorg Med Chem Lett

Title: Structure-based design of agents targeting the bacterial ribosome.

Authors: Bower J, Drysdale M, Hebdon R, Jordan A, Lentzen G, Matassova N, Murchie A, Powles J, Roughley S.

Abstract: Rational structure-based drug design has been applied to the antibiotic thiostrepton, in an attempt to overcome some of its' limitations. The identification of a proposed binding fragment allowed construction of a number of key fragments, which were derivatised to generate a library of potential antibiotics. These were then evaluated to determine their ability to bind to the L11 binding domain of the prokaryotic ribosome and inhibit bacterial protein translation.

CiteXplore: 12852942

DOI: 10.1016/s0960-894x(03)00495-5