Aminoalkylphosphonofluoridate derivatives: rapid and potentially selective inactivators of serine peptidases.
Aminoalkylphosphonofluoridate derivatives: rapid and potentially selective inactivators of serine peptidases.
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氨基烷基氟膦酸衍生物：丝氨酸肽酶的快速且潜在选择性灭活剂。
DOI：
10.1016/0006-291x(83)91729-1
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发表时间：
1983
影响因子：
3.1
通讯作者：
Bartlett,PA
中科院分区：
文献类型：
--
作者：
Lamden,LA;Bartlett,PA
n - cbz -丙氨酸和n - cbz -苯丙氨酸的膦酸类似物已被转化为酯类和酰胺类氟化物，并被评价为弹性酶（EC 3.4.21.11）和凝乳胰蛋白酶（EC 3.4.21.1）的灭活剂。这些抑制剂，模拟天然肽底物，是目前报道的弹性蛋白酶和凝乳胰蛋白酶最有效的失活剂，显示出适度的选择性，这与两种酶的底物特异性相关。
Phosphonic acid analogs of N-Cbz-alanine and N-Cbz-phenylalanine have been converted to the ester and amide fluoridates and evaluated as inactivators of elastase (EC 3.4.21.11) and chymotrypsin (EC 3.4.21.1). These inhibitors, which mimic the natural peptide substrates, are the most potent inactivators of elastase and chymotrypsin yet reported, showing a modest selectivity which correlates with the substrate specificity of the two enzymes.