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Synthesis and thrombolytic activity of carboline-3-carboxylic acid modified metabolites of Ala-Arg-Pro-Ala-Lys
Zhao, M; Wang, C; Wu, YF; Zhou, KX; Peng, SQ
关键词P6a Metabolites Modification Thrombolytic Activity
刊名PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY
2004
DOI10.1081/PB-120027113
34期:1页:57-76
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Biochemistry & Molecular Biology ; Biotechnology & Applied Microbiology
研究领域[WOS]Biochemistry & Molecular Biology ; Biotechnology & Applied Microbiology
关键词[WOS]FIBRINOGEN
英文摘要

From the metabolism of H-Ala-Arg-Pro-Ala-Lys-OH, four metabolites, H-Pro-Ala-Lys-OH, H-Arg-Pro-Ala-Lys-OH, H-Ala-Arg-Pro-OH, and H-Ala-Arg-Pro-Ala-OH were identified. In order to find a new lead compound of thrombolytic peptide, 3S-1,2,3,4-tetrahydro-beta-carboline3-carboxylic acid was introduced to the N- and C-terminal of the metabolites by use of the common coupling strategy. Under this condition, the pseudopeptides (5a-d and 7a-d) were obtained with a good yield. The thrombolytic activities of 3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid containing oligopeptides were evaluated in vitro and in vivo. The result indicated that the thrombolytic activity of the pseudopeptide depended on the sequence and the modification pattern of the metabolites, and only when 3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid was introduced into the C-terminal of H-Pro-Aal-Lys-OH or H-Arg-Pro-AlaLys-OH, the desirable thrombolytic activity was retained and enhanced significantly.

语种英语
WOS记录号WOS:000220079000005
引用统计
被引频次:6[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/56846
专题北京大学药学院
作者单位1.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
2.Guangzhou Baiyunshan Pharmaceut Co Ltd, Guangzhou, Peoples R China
推荐引用方式
GB/T 7714
Zhao, M,Wang, C,Wu, YF,et al. Synthesis and thrombolytic activity of carboline-3-carboxylic acid modified metabolites of Ala-Arg-Pro-Ala-Lys[J]. PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY,2004,34(1):57-76.
APA Zhao, M,Wang, C,Wu, YF,Zhou, KX,&Peng, SQ.(2004).Synthesis and thrombolytic activity of carboline-3-carboxylic acid modified metabolites of Ala-Arg-Pro-Ala-Lys.PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY,34(1),57-76.
MLA Zhao, M,et al."Synthesis and thrombolytic activity of carboline-3-carboxylic acid modified metabolites of Ala-Arg-Pro-Ala-Lys".PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY 34.1(2004):57-76.
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