Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues.

Affiliation

Manchester Institute of Biotechnology and School of Chemistry, The University of Manchester, Manchester M1 7DN, UK. Electronic address: [Email]

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.

Keywords

Aminoglycosides,HIV-1,Neamine,Neomycin,RNA RRE,