McDermott J R, Smith A I, Dodd P R, Hardy J A, Edwardson J A
Peptides. 1983 Jan-Feb;4(1):25-30. doi: 10.1016/0196-9781(83)90160-2.
The products of degradation of LH-RH and neurotensin by synaptosomes isolated from rat hypothalamus and cortex have been identified. LH-RH is cleaved at Tyr5-Gly6 and Pro9-Gly10 giving rise to LH-RH (1-5), LH-RH (6-10) and LH-RH (1-9). Neurotensin is cleaved at Arg8-Arg9, Pro10-Tyr11 and Ile12-Leu13, giving neurotensin (1-8), neurotensin (1-10), neurotensin (1-12) and neurotensin (9-13) as major products. While most of the peptidase activity is localized in the cytoplasmic fraction, a small but significant proportion is membrane bound. For LH-RH, the specificity of the membrane-bound activity is similar to that in the cytosol fraction; for neurotensin, the membrane fraction preferentially gives rise to the (1-10) and (1-11) peptides. The most potent inhibitors of the LH-RH and neurotensin degrading enzymes in synaptosomes are heavy metal ions (mercury and copper), p-chloromercuribenzoate and 1,10 phenanthroline.
已鉴定出从大鼠下丘脑和皮层分离的突触体对促黄体生成素释放激素（LH - RH）和神经降压素的降解产物。LH - RH在Tyr5 - Gly6和Pro9 - Gly10处裂解，产生LH - RH（1 - 5）、LH - RH（6 - 10）和LH - RH（1 - 9）。神经降压素在Arg8 - Arg9、Pro10 - Tyr11和Ile12 - Leu13处裂解，产生神经降压素（1 - 8）、神经降压素（1 - 10）、神经降压素（1 - 12）和神经降压素（9 - 13）作为主要产物。虽然大多数肽酶活性定位于细胞质部分，但有一小部分但显著比例是与膜结合的。对于LH - RH，膜结合活性的特异性与胞质溶胶部分相似；对于神经降压素，膜部分优先产生（1 - 10）和（1 - 11）肽。突触体中LH - RH和神经降压素降解酶的最有效抑制剂是重金属离子（汞和铜）、对氯汞苯甲酸和1,10 - 菲咯啉。
