Pentapeptide (Pepstatin) Inhibition of Brain Acid Proteinase
Pentapeptide (Pepstatin) Inhibition of Brain Acid Proteinase
复制标题
五肽（胃酶抑素）抑制脑酸性蛋白酶
作者：
N. Marks;A. Grynbaum;A. Lajtha
从放线菌培养液中获得的五肽胃酶抑素在极低浓度下完全抑制脑酸性蛋白酶（组织蛋白酶D）。在测试的脑酶中，该效应对酸性蛋白酶具有特异性，因为添加1000倍高浓度对中性蛋白酶、氨肽酶和芳基酰胺酶没有影响。胃蛋白酶抑制素也抑制胃蛋白酶，如用血红蛋白或用N-乙酰苯丙氨酰-L-二碘酪氨酸作为底物所测试的。胃蛋白酶抑制素是迄今为止发现的抑制脑细胞内酸性蛋白水解酶活性最强的药物。
The pentapeptide pepstatin obtained from culture filtrates of actinomycetes completely inhibited brain acid proteinase (cathepsin D) at exceedingly low concentrations. Among the brain enzymes tested, the effect is specific for acid proteinase because addition of 1000-fold higher concentrations was without effect on neutral proteinase, aminopeptidase, and arylamidases. Pepstatin also inhibits pepsin as tested with hemoglobin or with N-acetylphenylalanyl-L-diiodotyrosine as substrate. Pepstatin must be regarded as the most powerful agent yet described that inhibits intracellular acidic proteolytic enzyme in brain.