Fricker L D, Plummer T H, Snyder S H
Biochem Biophys Res Commun. 1983 Mar 29;111(3):994-1000. doi: 10.1016/0006-291x(83)91398-0.
Biproduct analogs of lysine and arginine are potent inhibitors of enkephalin convertase, a carboxypeptidase B-like enzyme which appears to be physiologically associated with enkephalin biosynthesis. The most effective derivatives are guanidinoethylmercaptosuccinic acid and guanidinopropylsuccinic acid with respective Ki's of 8.8 and 7.5 nM. These dicarboxylic acid analogs of arginine are several hundred fold more potent towards enkephalin convertase than towards carboxypeptidase B or N. Kinetic analysis indicates the pure competitive nature of the inhibition. Bromoacetyl-D-arginine, an irreversible inhibitor of carboxypeptidase B and N, is also an efficient irreversible inhibitor of enkephalin convertase.
赖氨酸和精氨酸的双产物类似物是脑啡肽转化酶的有效抑制剂，脑啡肽转化酶是一种类似于羧肽酶B的酶，似乎在生理上与脑啡肽生物合成相关。最有效的衍生物是胍基乙基巯基琥珀酸和胍基丙基琥珀酸，其各自的抑制常数（Ki）分别为8.8和7.5纳摩尔。这些精氨酸的二羧酸类似物对脑啡肽转化酶的效力比对羧肽酶B或N的效力强数百倍。动力学分析表明抑制作用具有纯粹的竞争性。溴乙酰-D-精氨酸是羧肽酶B和N的不可逆抑制剂，也是脑啡肽转化酶的有效不可逆抑制剂。
