Synthetic inhibitors of the multicatalytic proteinase complex (proteasome).
Synthetic inhibitors of the multicatalytic proteinase complex (proteasome).
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多催化蛋白酶复合物（蛋白酶体）的合成抑制剂。
DOI：
10.1159/000468688
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发表时间：
1993
期刊：
影响因子：
--
通讯作者：
Figueiredo-Pereira,ME
中科院分区：
文献类型：
--
作者：
Wilk,S;Figueiredo-Pereira,ME
多催化酶复合体(蛋白酶体)的合成抑制剂可以为揭示这种大分子的功能意义和催化机制提供手段。虽然缓蚀剂的开发仍处于早期阶段，但已经制备了一些有用的化合物。到目前为止，在所研究的各种类型的抑制剂中，肽醛是最有效的。由于肽醛同时抑制丝氨酸和半胱氨酸蛋白酶，缺乏特异性是它们的主要限制。本文详细介绍了一种有效的Suc-LLVY-MCA水解酶抑制剂N-苄氧羰基-IE(OT-Bu)A-亮氨酸的性质。
Synthetic inhibitors of the multicatalytic proteinase complex(proteasome) can provide the means to uncover the functional significance and catalytic mechanism of this macromolecule. Although inhibitor development is still in its early stages,some useful compounds have already been prepared. Of the various types of inhibitors thus far studied, peptidyl aldehydes have been the most effective. Since peptidyl aldehydes inhibit both serine and cysteine proteinases, lack of specificity is their major limitation. The properties of one such compound N-benzyloxycarbonyl-IE(Ot-Bu)A-Leucinal, a potent inhibitor of suc-LLVY-MCA hydrolysis, are described in detail.