人白细胞弹性蛋白酶的对映选择性抑制
Enantioselective inhibition of human leukocyte elastase.
作者信息
Groutas W C, Brubaker M J, Venkataraman R, Stanga M A
机构信息
Department of Chemistry, Wichita State University, Kansas 67208.
出版信息
Arch Biochem Biophys. 1992 Aug 15;297(1):144-6. doi: 10.1016/0003-9861(92)90652-d.
PMID:1637176
Abstract
(RS)-Diethyl-2-benzyl-succinate was resolved using alpha-chymotrypsin. The two enantiomers were then elaborated to yield (S)-(+) and (R)-(-)-3-benzyl-N-[(methyl-sulfonyl)oxy]succinimide and the inhibitory activity of the two enantiomers toward human leukocyte elastase was subsequently determined. The k2/KI values for the R and S isomers were found to be 330 and 1500 M-1 s-1, respectively.
摘要
使用α-胰凝乳蛋白酶拆分（RS）-二乙基-2-苄基琥珀酸酯。然后将两种对映体进行衍生化，得到（S）-（+）和（R）-（-）-3-苄基-N-[(甲基磺酰基)氧基]琥珀酰亚胺，随后测定了这两种对映体对人白细胞弹性蛋白酶的抑制活性。发现R和S异构体的k2/KI值分别为330和1500 M-1 s-1。
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