Solid-phase synthesis of succinylhydroxamate peptides: Functionalized matrix metalloproteinase inhibitors
Solid-phase synthesis of succinylhydroxamate peptides: Functionalized matrix metalloproteinase inhibitors
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DOI：
10.1021/ol060409e
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发表时间：
2006-04-13
期刊：
影响因子：
5.2
通讯作者：
Overkleeft, HS
中科院分区：
文献类型：
--
作者：
Leeuwenburgh, MA;Geurink, PP;Overkleeft, HS
一种新的固相合成策略对琥珀酰异羟肟酸肽，使用适当保护的异羟肟酸积木，描述。获得了对胺官能化肽的快速和有效的访问，其可以用例如荧光标记来修饰。此外，我们证明了一个树脂合成的生物素化的光活化异羟肟酸肽，它可以用作基于活性的探针基质金属蛋白酶和亚当斯。
A novel solid-phase synthesis strategy toward succinylhydroxamate peptides, using an appropriately protected hydroxamate building block, is described. Rapid and efficient access is gained to amine-functionalized peptides, which can be decorated with, for instance, a fluorescent label. In addition, we demonstrate an on-resin synthesis of a biotinylated photoactivatable hydroxamate peptide, which can be used as an activity-based probe for matrix metalloproteinases and ADAMs.