Chemistry and biology of tubulysins: antimitotic tetrapeptides with activity against drug resistant cancers

被引：59
|
作者：
Murray, Bryan C. [1 ]
Peterson, Michael T. [1 ]
Fecik, Robert A. [1 ]
机构：
[1] Univ Minnesota, Med Chem, Minneapolis, MN 55455 USA
来源：
NATURAL PRODUCT REPORTS | 2015年 / 32卷 / 05期
关键词：
POTENTIAL ANTICANCER; NATURAL TUBULYSINS; ANALOGS; DESIGN; CYTOTOXICITY; INHIBITORS; PEPTIDES;
D O I：
10.1039/c4np00036f
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：
Since their first report in 2000, tubulysins have sparked great interest for development as anti-cancer agents due to their exceptionally potent antiproliferative activity. Progress in the discovery and development of tubulysins, especially tubulysin conjugates, has quickly advanced despite limitations in their availability from Nature. In this Highlight, the key research on the isolation and structure determination, biosynthesis, bioactivity, structure-activity relationships (SAR), synthesis, and conjugates of tubulysins is presented.
引用
收藏
页码：654 / 662
页数：9
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