Griffiths E C, Hooper K C, Hopkinson C R
Acta Endocrinol (Copenh). 1975 May;79(1):7-15. doi: 10.1530/acta.0.0790007.
Luteinizing hormone-releasing hormone (LH-RH) is known to be inactivated by peptidases in the rat hypothalamus with consequent loss of LH-releasing ability. To make a further study of the peptidases' action on the decapeptide, synthetic LH-RH and its [1-9NH2] analogue were incubated with the supernatant hypothalamic fraction containing the enzyme activity. Using an assay system measuring gonadotrophin release in ovariectomized/steroid-primed rats, both LH-RH and the [1-9NH2] analogue were found to be inactivated to different extents after incubation with the fraction, the analogue completely losing both LH- and FSH-releasing activity, and the releasing hormone almost completely losing its LH- and totally losing its FSH-releasing activity. The findings extend the initial studies by showing that the peptidases can remove both the decapeptide's intrinsic LH- and FSH-releasing activity and that these enzymes act on LH-RH at a site other than the C-terminal glycinamide, since they are able to inactivate the [1-9NH2] analogue lacking this residue.
已知促黄体生成素释放激素(LH-RH)在大鼠下丘脑被肽酶灭活,从而导致促黄体生成素释放能力丧失。为了进一步研究肽酶对十肽的作用,将合成的LH-RH及其[1-9NH2]类似物与含有酶活性的下丘脑上清液部分一起孵育。使用一种测定去卵巢/类固醇预处理大鼠中促性腺激素释放的测定系统,发现LH-RH和[1-9NH2]类似物在与该部分孵育后均被不同程度地灭活,该类似物完全丧失了促黄体生成素和促卵泡激素释放活性,而释放激素几乎完全丧失了其促黄体生成素释放活性并完全丧失了其促卵泡激素释放活性。这些发现扩展了最初的研究,表明肽酶可以去除十肽固有的促黄体生成素和促卵泡激素释放活性,并且这些酶作用于促黄体生成素释放激素的位点不是C末端甘氨酰胺,因为它们能够使缺乏该残基的[1-9NH2]类似物失活。