The structural requirements for inhibition of proteasome function by the lactacystin-derived β-lactone and synthetic analogs

The structural requirements for inhibition of proteasome function by the lactacystin-derived β-lactone and synthetic analogs
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DOI:
10.1016/s0040-4020(98)01142-9
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发表时间:
1999-03-12
期刊:
影响因子:
2.1
通讯作者:
Fenteany, G
Fenteany, G
中科院分区:
化学3区
文献类型:
--
作者:
Corey, EJ;Li, WDZ;Fenteany, G

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其中C(5)、C(7)和C(9)处的取代基系统地变化的乳胱氨酸衍生的β-内酯(2)的类似物的合成导致了对于哺乳动物20 S蛋白酶体的高度选择性抑制的明确定义的结构-活性相关性。(C)1999爱思唯尔科技有限公司。保留所有权利。
The synthesis of analogs of the lactacystin-derived beta-lactone (2) in which the substituents at C(5), C(7) and C(9) were systematically varied has led to a well defined structure-activity correlation for the highly selective inhibition of the mammalian 20 S proteasome. (C) 1999 Elsevier Science Ltd. All rights reserved.