肾脏中性内肽酶以及突触膜对脑啡肽的水解作用对抑制剂表现出相似的敏感性。
Kidney neutral endopeptidase and the hydrolysis of enkephalin by synaptic membranes show similar sensitivity to inhibitors.
作者信息
Fulcher I S, Matsas R, Turner A J, Kenny A J
出版信息
Biochem J. 1982 May 1;203(2):519-22. doi: 10.1042/bj2030519.
Abstract
Neutral endopeptidase (EC 3.4.24.11) from pig kidney hydrolyses [125I]iodo-insulin B-chain and leucine-enkephalin. Both activities were equally sensitive to inhibition by phosphoramidon [N-(alpha-L-rhamnopyranosyloxyhydroxyphosphinyl)-L-leucyl-L-tryptophan] and thiorphan [N-(DL-2-benzyl-3-mercaptopropionyl)glycine]. Thermolysin hydrolysis of insulin B-chain was also sensitive to both inhibitors. The hydrolysis of the Gly3-Phe4 bond of Leu-enkephalin by synaptic membranes prepared from pig brain was partially inhibited by phosphoramidon and thiorphan. Synaptic membranes appear to contain another endopeptidase activity that is insensitive to these reagents. These observations suggest that enzymes similar to the kidney endopeptidase may play a general role in neuropeptide metabolism.
摘要
猪肾来源的中性内肽酶（EC 3.4.24.11）可水解[125I]碘胰岛素B链和亮氨酸脑啡肽。两种活性对磷酰胺脒[N-(α-L-鼠李糖吡喃糖氧基羟基膦酰基)-L-亮氨酰-L-色氨酸]和硫磷酰胺[N-(DL-2-苄基-3-巯基丙酰基)甘氨酸]的抑制作用同样敏感。胰岛素B链的嗜热菌蛋白酶水解也对这两种抑制剂敏感。猪脑制备的突触膜对亮氨酸脑啡肽Gly3-Phe4键的水解被磷酰胺脒和硫磷酰胺部分抑制。突触膜似乎含有另一种对这些试剂不敏感的内肽酶活性。这些观察结果表明，类似于肾内肽酶的酶可能在神经肽代谢中起普遍作用。
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