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学科主题: 药学
题名:
PAK: an essential motif for forming beta-turn structures and exhibiting the thrombolytic effect of P6A and its analogs
作者: Zhao, Ming2; Jia, Xin3; Wang, Chao3; Li, Qin3; Zhou, Kexiang2; Wang, Lili1; Liu, Hu1; Peng, Shiqi2
关键词: thrombolysis ; fibrinolysis ; peptide 6A ; NMR structure ; beta-turn ; plasminogen
刊名: BIOCHEMISTRY AND CELL BIOLOGY-BIOCHIMIE ET BIOLOGIE CELLULAIRE
发表日期: 2007-12-01
DOI: 10.1139/O07-143
卷: 85, 期:6, 页:730-740
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Cell Biology
研究领域[WOS]: Biochemistry & Molecular Biology ; Cell Biology
关键词[WOS]: DEGRADATION PRODUCT PEPTIDE-6A ; ANGIOTENSIN CONVERTING ENZYME ; PLASMINOGEN-ACTIVATOR ; VASOACTIVE PEPTIDES ; GLOBULAR-PROTEINS ; CRYSTAL-STRUCTURE ; BLOOD-FLOW ; FIBRINOGEN FRAGMENT ; HYDROPHOBIC BASIS ; ESCHERICHIA-COLI
英文摘要:

Ala-Arg-Pro-Ala-Lys (ARPAK; also known as P6A) and 19 of its analogs were synthesized, and their thrombolytic activities were assessed in vitro and in vivo. The solution structures of 12 of the P6A analogs were determined using nuclear magnetic resonance (NMR) spectroscopy. The thrombolytic activity and conformational structure relationship was analyzed. We found that the Pro-Ala-Lys (PAK) sequence was essential for thrombolytic activity and was also responsible for the beta-turn structure found in the P6A analogs studied. The well defined beta turn may act as a binding head with the protruding lysine side-chain (positively charged) found at the target site for target recognition. Additionally, the N-terminal residue may be critical for thrombolytic activity, which for PAK-containing peptides, is likely achieved via a plasminogen-dependent pathway.

语种: 英语
WOS记录号: WOS:000252316300008
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/50118
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Mem Univ Newfoundland, Sch Pharm, St John, NF A1B 3V6, Canada
2.Capital Med Univ, Coll Chem Biol & Pharmaceut Sci, Beijing 100069, Peoples R China
3.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Zhao, Ming,Jia, Xin,Wang, Chao,et al. PAK: an essential motif for forming beta-turn structures and exhibiting the thrombolytic effect of P6A and its analogs[J]. BIOCHEMISTRY AND CELL BIOLOGY-BIOCHIMIE ET BIOLOGIE CELLULAIRE,2007,85(6):730-740.
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