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Synthesis and evaluation of ferrocenoyl pentapeptide (Fc-KLVFF) as an inhibitor of Alzheimer’s Aβ1–42 fibril formation in vitro

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成果类型:
期刊论文
作者:
Wei, Chuan-Wan;Peng, Yong;Zhang, Lin;Huang, Qiyu;Cheng, Ming;...
通讯作者:
Liu, You-Nian
作者机构:
[Cheng, Ming; Wei, Chuan-Wan; Huang, Qiyu; Peng, Yong; Liu, You-Nian; Li, Juan; Zhang, Lin] Cent S Univ, Coll Chem & Chem Engn, Changsha 410083, Hunan, Peoples R China.
[Wei, Chuan-Wan] Univ S China, Coll Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[Liu, You-Nian] C
Cent S Univ, Coll Chem & Chem Engn, Changsha 410083, Hunan, Peoples R China.
语种:
英文
关键词:
beta-amyloid aggregation;Inhibitor;Ferrocene;KLVFF
期刊:
Bioorganic & Medicinal Chemistry Letters
ISSN:
0960-894X
年:
2011
卷:
21
期:
19
页码:
5818-5821
基金类别:
We thank Dr. Feimeng Zhou (California State University, Los Angeles) for helpful discussions in electrochemistry. We are grateful to the National Natural Science Foundation of China (Nos. 20876179, 20904066 and 21076232) for financial support.
机构署名:
本校为其他机构
院系归属:
化学化工学院
摘要:
Aggregation and fibril formation of β-amyloid peptides (Aβ) is the key event in the pathogenesis of Alzheimer's disease. Many efforts have been made on the development of effective inhibitors to prevent Aβ fibril formation or disassemble the preformed Aβ fibrils. Peptide inhibitors with sequences homologous to the hydrophobic segments of Aβ can alter the aggregation pathway of Aβ, together with decrease of the cell toxicity. In this study, the conjugate of ferrocenoyl (Fc) with pentapeptide KLVFF (Fc-KLVFF), was synthesized by HBTU/HOBt p...

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