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Tripeptides from synthetic amino acids block the Tat-TAR association and slow down HIV spread in cell cultures.

TitleTripeptides from synthetic amino acids block the Tat-TAR association and slow down HIV spread in cell cultures.
Publication TypeJournal Article
Year of Publication2007
AuthorsLudwig V, Krebs A, Stoll M, Dietrich U, Ferner J, Schwalbe H, Scheffer U, Dürner G, Göbel MW
JournalChembiochem
Volume8
Pagination1850–1856
Date PublishedOct
Accession Number147
Abstract

Non-natural amino acids with aromatic or heteroaromatic side chains were incorporated into tripeptides of the general structure Arg-X-Arg and tested as ligands of the HIV RNA element TAR. Some of these compounds could compete efficiently with the association of TAR and Tat and downregulated a TAR-controlled reporter gene in HeLa cells. Peptide 7, which contains a 2-pyrimidinyl-alkyl chain, also inhibited the spread of HIV-1 in cell cultures. NMR studies of 7 bound to HIV-2-TAR gave evidence for contacts in the bulge region.

URLhttp://dx.doi.org/10.1002/cbic.200700232
DOI10.1002/cbic.200700232