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学科主题: 药学
题名:
Design and synthesis of guanidinoglycosides directed against the TAR RNA of HIV-1
作者: Wang, M; Tu, PF; Xu, ZD; Yu, XL; Yang, M
刊名: HELVETICA CHIMICA ACTA
发表日期: 2003
卷: 86, 期:7, 页:2637-2644
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary
研究领域[WOS]: Chemistry
关键词[WOS]: HUMAN-IMMUNODEFICIENCY-VIRUS ; TYPE-1 GENE-EXPRESSION ; BINDING ; TRANSACTIVATION
英文摘要:

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-alpha,alpha-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.

语种: 英语
WOS记录号: WOS:000184797400029
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60706
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Natl Res Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Wang, M,Tu, PF,Xu, ZD,et al. Design and synthesis of guanidinoglycosides directed against the TAR RNA of HIV-1[J]. HELVETICA CHIMICA ACTA,2003,86(7):2637-2644.
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