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Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine
Binto Simon1, Claire Walmsley1, Victoria J Jackson1
1Manchester Institute of Biotechnology and School of Chemistry, The University of Manchester, Manchester M1 7DN, UK.
Abstract:
Synthetic neamine mimetics have been evaluated for binding to the HIV-1 Rev response element. Modified neamine derivatives, obtained from reductive amination of neamine, led to identification of new 6-amino modified neamine-type ligands with HIV-1 RRE binding affinity up to 20× that of neamine and up to 6× that of the more complex neomycin itself. This provides a noteworthy structure-activity increase and a useful lead to simplified, chemically accessible mimetics.
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