644965-01-5Relevant academic research and scientific papers
Design and synthesis of guanidinoglycosides directed against the TAR RNA of HIV-1
Wang, Min,Tu, Peng-Fei,Xu, Zhi-Dong,Yu, Xiao-Lin,Yang, Ming
, p. 2637 - 2644 (2007/10/03)
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 13-15) 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.
