Walter R
Biochim Biophys Acta. 1976 Jan 23;422(1):138-58. doi: 10.1016/0005-2744(76)90015-2.
The inactivation of the neurohypophyseal hormones arginine vasopressin and oxytocin, both 14C-labelled in the C-terminal glycine residue, by enzymes present in kidney homogenates of various species has been investigated, and some of the enzymes responsible have been partially purified and characterized. The Leu-Gly peptide bond of oxytocin is generally most effectively cleaved by kidney homogenates, although with certain species enzymic activity hydrolyzing the Pro-Leu bond is significant. Degradation of arginine vasopressin is slower than oxytocin in all species studied, and appears to occur by a different overall mechanism since cleavage of the Pro-Arg bond is more significant than hydrolysis of the Arg-Gly bond. The enzyme releasing glycinamide from oxytocin and the "Post-Proline Cleaving Enzyme", which releases C-terminal dipeptide from oxytocin and arginine vasopressin, were partially purified from lamb kidney by ammonium sulfate fractionation and column chromatography. The two enzymes are shown to be separate entities with different pH profiles. The prolyl peptidase activity released the C-terminal dipeptides from oxytocin and arginine vasopressin at similar rates and was inhibited by p-chloromercuriphenylsulfonic acid, 1,10-phenanthroline, L-1-tosylamido-2-phenylethylchloromethyl ketone, Co2+, Ca2+, and Zn2+, but significantly enhanced by dithiothreitol. The prolyl peptidase preparation cleaves proline-containing peptide substrates at the Pro-X bond. The rate of cleavage is dependent on the nature of residue X and with the conditions used there is no cleavage when X equals Pro; however, cleavage occurs when X is a D isomer: [Mpr1, D-Arg8] vasopressin is inactivated at a rate similar to [Mpr1, Arg8]- and [Mpr1, Lys8] vasopressin, suggesting that the known prolonged biological action of [Mpr1, D-Arg8] vasopressin is not due to resistance to the prolyl peptidase. In all characteristics tested the lamb kidney prolyl peptidase was identical to the post-proline cleaving enzyme isolated earlier from human uterus. In vivo experiments in the cat suggested that both the glycinamide-releasing enzyme and post-proline cleaving enzyme are present and effective in inactivating neurohypophyseal hormones in the intact animal.
研究了各种物种肾脏匀浆中存在的酶对神经垂体激素精氨酸加压素和催产素(二者在C末端甘氨酸残基处均用¹⁴C标记)的失活作用,并对一些相关酶进行了部分纯化和特性鉴定。催产素的亮氨酸 - 甘氨酸肽键通常最易被肾脏匀浆裂解,不过某些物种中水解脯氨酸 - 亮氨酸键的酶活性也很显著。在所有研究的物种中,精氨酸加压素的降解都比催产素慢,而且其整体降解机制似乎不同,因为脯氨酸 - 精氨酸键的裂解比精氨酸 - 甘氨酸键的水解更显著。通过硫酸铵分级分离和柱色谱法从羊肾中部分纯化了从催产素释放甘氨酰胺的酶以及从催产素和精氨酸加压素释放C末端二肽的“脯氨酸后裂解酶”。结果表明这两种酶是具有不同pH谱的独立实体。脯氨酰肽酶活性以相似的速率从催产素和精氨酸加压素释放C末端二肽,并受到对氯汞苯磺酸、1,10 - 菲咯啉、L - 1 - 甲苯磺酰氨基 - 2 - 苯乙基氯甲基酮、Co²⁺、Ca²⁺和Zn²⁺的抑制,但二硫苏糖醇可显著增强其活性。脯氨酰肽酶制剂在脯氨酸 - X键处裂解含脯氨酸的肽底物。裂解速率取决于残基X的性质,在所使用的条件下,当X等于脯氨酸时不发生裂解;然而,当X是D异构体时会发生裂解:[Mpr1, D - Arg8]加压素的失活速率与[Mpr1, Arg8] - 和[Mpr1, Lys8]加压素相似,这表明[Mpr1, D - Arg8]加压素已知的延长生物作用并非由于对脯氨酰肽酶有抗性。在所有测试的特性方面,羊肾脯氨酰肽酶与先前从人子宫中分离出的脯氨酸后裂解酶相同。在猫身上进行的体内实验表明,释放甘氨酰胺的酶和脯氨酸后裂解酶在完整动物体内均存在且能有效使神经垂体激素失活。