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- Title
Design and Synthesis of Guanidinoglycosides Directed against the TAR RNA of HIV-1.
- Authors
Min Wang; Peng-Fei Tu; Zhi-Dong Xu; Xiao-Lin Yu; Ming Yang
- Abstract
Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of the Tat protein with the transactivation responsive region (TAR) RNA. Tat-TAR RNA Interaction is mediated by a short arginine-rich domain of the protein. Disruption of this interaction could, in theory, create a state of complete viral latency. Here, four novel 6-amino-6-deoxytrehalose guanidinoglycoside derivatives (10 and 1315) as target molecules have been designed to bind to TAR RNA for blocking the interaction of Tat-TAR RNA. They were obtained by coupling 6-amino-6-deoxy-α,α-trehalose (6) with the protected amino acids, deprotection by catalytic hydrogenation, followed by guanidinylated with S-methylisothiourea sulfate. Their abilities to inhibit Tat-TAR RNA interaction were determined by a Tat-dependent HIV-1 long terminal repeats (LTR)-driven chloramphenicol acetyltransferase (CAT) assays.
- Subjects
HIV; RNA; PROTEINS
- Publication
Helvetica Chimica Acta, 2003, Vol 86, Issue 7, p2637
- ISSN
0018-019X
- Publication type
Article