HR22C16: A potent small-molecule probe for the dynamics of cell division

被引:134
作者
Hotha, S
Yarrow, JC
Yang, JG
Garrett, S
Renduchintala, KV
Mayer, TU
Kapoor, TM
机构
[1] Rockefeller Univ, Lab Chem & Cell Biol, New York, NY 10021 USA
[2] Harvard Univ, Sch Med, Dept Cell Biol, Boston, MA 02115 USA
[3] Max Planck Inst Biochem, D-82152 Martinsried, Germany
关键词
antimitotics; inhibitors; molecular motors; photolysis; solid-phase synthesis;
D O I
10.1002/anie.200351173
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A high-throughput, microscopy-based chemical-genetic screen identified HR22C16, which causes a monoastral mitotic block, as a small-molecule probe for cell division (see picture). By using a diastereoselective, traceless solid-phase synthesis and biological assays, a more potent HR22C16 analogue was then identified. A photocaging strategy for HR22C16 was also developed to allow fast temporal control over the function of the target protein Eg5.
引用
收藏
页码:2379 / 2382
页数:4
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