合成类丝氨酸蛋白酶抑制剂的研究进展  

Advances of synthetic serine protease inhibitors

作　　者：刘宝玉[1] 孟昭力[1] 

机构地区：[1]山东大学药学院药物化学研究室,济南250012

出　　处：《中国新药杂志》2006年第5期334-336,共3页Chinese Journal of New Drugs

摘　　要：合成类丝氨酸蛋白酶抑制剂是人工合成的非肽类小分子化合物,具有广谱抑制性,无抗原性,相对分子质量小,可以自由进入血管及胰腺组织,能直接作用于胰腺细胞上,抑制胰酶(trypsin)、血纤维蛋白溶酶(plas- min)、血浆激肽释放酶(plasma kellilrein)、凝血酶(throbin)及补体酯酶C_1和_(?)目前已获准上市的药物有加贝酯、奈莫司他、卡莫司他和司匹司他,临床主要用于急、慢性胰腺炎和弥散性血管内凝血的治疗。Synthetic serine protease inhibitors are a group of proteins that inhibit peptidase. Serine proteases are defined by the presence of a serine residue in their active domain. The serine protease inhibitors feature broad-spectrum, non-antigenicity and small molecular weight. Although the function of the serine protease inhibitors varies widely, they share a number of structural details, and are found free in blood vessel and pancreatic tissue. One of the examples is effect of the synthetic serine protease inhibitors on proliferation and collagen synthesis of human pancreatic ceils. Moreover, they could inhibit trypsin-like serine proteases such as trypsin, chymotrypsin, chymase, plasmin, plasma kellilrein, thrombin, C1 and C1r.

关 键 词：丝氨酸蛋白酶抑制剂 加贝酯 奈莫司他 卡莫司他 司匹司他 

分 类 号：R914.5[医药卫生—药物化学]