Covalent modification as a strategy to block protein-protein interactions with small-molecule drugs

被引:39
|
作者
Way, JC [1 ]
机构
[1] Inst Mol Sci, Berkeley, CA 94704 USA
关键词
D O I
10.1016/S1367-5931(99)00049-6
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
It is generally difficult to block protein-protein interactions with small-molecule drugs. A novel pharmaceutical development strategy to block protein interactions is emerging: targeted covalent modification to sterically block interactions. By this approach, compounds first interact non-covalently with a specific target protein. This interaction juxtaposes a weakly reactive group of the drug with a target amino acid sidechain, which then react by virtue of their high local concentration.
引用
收藏
页码:40 / 46
页数:7
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