Biological evaluation of tubulysin A:: a potential anticancer and antiangiogenic natural product

被引：108
|
作者：
Kaur, Gurmeet
Hollingshead, Melinda
Holbeck, Susan
Schauer-Vukasinovic, Vesna
Camalier, Richard F.
Doemling, Alexander
Agarwal, Seema
机构：
[1] NCI, DCTD, Dev Therapeut Program, Bethesda, MD 20892 USA
[2] Morphochem Inc, Monmouth Jct, NJ 08852 USA
[3] Morphochem AG, D-81379 Munich, Germany
来源：
BIOCHEMICAL JOURNAL | 2006年 / 396卷
关键词：
antiangiogenesis; anticancer agent; cytochrome P450; microtubule; tubulin; tubulysin A;
D O I：
10.1042/BJ20051735
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Tubulysin A (tubA) is a natural product isolated from a strain of myxobacteria that has been shown to depolymerize microtubules and induce mitotic arrest. The potential of tubA as an anticancer and antiangiogenic agent is explored in the present study. tubA shows potent antiproliferative activity in a panel of human cancer cell lines irrespective of their multidrug resistance properties. It induces apoptosis in cancer cells but not in normal cells and shows significant potential antiangiogenic properties in several in vitro assays. It is efficacious in initial animal studies using a hollow fibre assay with 12 different human tumour cell lines. This study suggests that both in vitro and preclinical profiles of tubA may translate into clinically useful anticancer properties.
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收藏
页码：235 / 242
页数：8
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