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Bioorg Med Chem Lett. 2003 Aug 4;13(15):2455-8.
Structure-based design of agents targeting the bacterial ribosome.

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

Department of Medicinal Chemistry, RiboTargets Ltd., Granta Park, Abington, Cambridge CB1 6GB, UK.

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.

online pharmacy ref. source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12852942&dopt=Abstract [PubMed - in process]

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