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杨铭

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期刊论文

a, a-Trehalose derivatives bearing guanidino groups as inhibitors to HIV-1 Tat-TAR RNA interaction in human cells

杨铭Min Wangab Zhidong Xub Pengfei Tua Xiaolin Yua Sulong Xiao a and Ming Yang a*

Bioorganic & Medicinal Chemistry Letters 14 (2004) 2585-2588,-0001,():

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摘要/描述

Replication of HIV-1 requires specific interactions of Tat protein with TAR RNA. Disruption of Tat-TAR RNA interaction could inhibit HIV-1 replication. Here four target compounds were designed and synthesized to bind to TAR RNA for blocking the interaction of Tat-TAR RNA. The core molecule 6,60-diamino-6,60-dideoxy-a,a-trehalose was obtained from selective bromination of, a,a-trehalose at C-6,60, followed by acetylation, azide displacement, deacetylation, and reduction. Coupling of the core molecule with the protected amino acid, then deprotection and guanidinylation generated the novel a,a-trehalose derivatives. Their abilities to inhibit Tat-TAR RNA interaction in human cells were determined by a Tat-dependent HIV-1 LTR-driven CAT assays.

版权说明:以下全部内容由杨铭上传于   2005年06月16日 22时46分09秒,版权归本人所有。

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