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Short cyclic peptides derived from the C-terminal sequence of alpha 1-antitrypsin exhibit significant anti-HIV-1 activity

  作者 Jia, QY; Jiang, XF; Yu, F; Qiu, JY; Kang, XY; Cai, LF; Li, L; Shi, WG; Liu, SW; Jiang, SB; Liu, KL  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-7;  页码  2393-2395  
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[摘要]Serpin A1 (alpha 1-AT), the largest subgroup of serpins, presents in human plasma at high concentration and plays important regulatory roles in physiological and pathological processes. Accumulated evidence suggests that alpha 1-AT may play a role in controlling HIV-1 infection. In this study, we designed and synthesized a set of short linear peptides derived from the C-terminal sequence of alpha 1-AT. Since none of them showed significant anti-HIV-1activity, we proceeded to synthesize four short cyclic peptides having 7 amino acids, and we found that three of them exhibited significant anti-HIV-1 activity. One of these cyclic peptides, designated CPM, inhibited HIV-1 entry and infection at low mu M level, indicating that these short cyclic peptides could serve as leads for the development of novel anti-HIV-1 therapeutics. (C) 2012 Elsevier Ltd. All rights reserved.

 
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