A novel peptide from alpha5 helix of Asterina pectinifera cyclin B conjugated to HIV-Tat(49-57) with cytotoxic and apoptotic effects against human cancer cells

A series of novel peptides from various motifs of Asterina pectinifera cyclin B and their derivatives conjugated to HIV-Tat(49-57) were designed and synthesized. Their bioactivities on two human cancer cell lines were determined. Among them, Tat-a5 (KAQIRAMECNILGRKKRRQRRR) exhibited significant cyto...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2008-08, Vol.18 (16), p.4633-4637
Main Authors: Lou, Huiping, Gao, Yanfeng, Zhai, Mingxia, Qi, Yuanming, Chen, Lixiang, Lv, Hong, Yu, Jibing, Li, Yongxin
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Animals
Antineoplastic Agents - pharmacology
Apoptosis
Asterina - metabolism
Cell Cycle - drug effects
Cell Line, Tumor
Chemistry, Pharmaceutical - methods
Cyclin B - chemistry
Dose-Response Relationship, Drug
Drug Design
Humans
Molecular Sequence Data
Peptide Fragments - chemistry
Peptides - chemistry
tat Gene Products, Human Immunodeficiency Virus - chemistry
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Summary:A series of novel peptides from various motifs of Asterina pectinifera cyclin B and their derivatives conjugated to HIV-Tat(49-57) were designed and synthesized. Their bioactivities on two human cancer cell lines were determined. Among them, Tat-a5 (KAQIRAMECNILGRKKRRQRRR) exhibited significant cytotoxic effects on cancer cell lines EC-9706 and HCT-116. Tat-a5 could arrest cancer cells at G(2)/M phase and make them apoptotic. Our results suggested that Tat-a5 could be a novel leading peptide with anticancer activity.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2008.07.017