胃蛋白酶抑制剂对大鼠心肌酸性蛋白酶的抑制作用
Pepstatin inhibition of rat myocardial acid protease.
作者信息
Hokins B E, Smith T W
出版信息
Recent Adv Stud Cardiac Struct Metab. 1976;12:439-43.
PMID:1031998
Abstract
The protease inhibitor, pepstatin, inhibited acid protease in rat heart homogenates with a Ki of 7 x 10(-11) M by a noncompetitive mechanism, but it had no effect on myocardial acid protease activity when given in high doses to intact animals. Exposure of heart slices to 10(-7) M pepstatin for two hours also failed to produce demonstrable acid protease inhibition, suggesting that myocardial acid protease activity is unaffected by this potent inhibitor unless the integrity of the cell is disturbed.
摘要
蛋白酶抑制剂胃蛋白酶抑素通过非竞争性机制抑制大鼠心脏匀浆中的酸性蛋白酶，其抑制常数Ki为7×10⁻¹¹M，但给完整动物大剂量给药时对心肌酸性蛋白酶活性无影响。将心脏切片暴露于10⁻⁷M胃蛋白酶抑素两小时也未能产生可证实的酸性蛋白酶抑制作用，这表明除非细胞完整性受到干扰，心肌酸性蛋白酶活性不受这种强效抑制剂的影响。
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