水蛭素融合蛋白研究进展  

Research Progress in Hirudin Fusion Protein——Review

作　　者：张传领[1] 于爱平[1] 靳继德[1] 吴祖泽[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《中国实验血液学杂志》2007年第1期215-218,共4页Journal of Experimental Hematology

摘　　要：水蛭素是一种高效特异的凝血酶抑制剂,临床上用于血栓病的预防和治疗,但它半衰期短、出血副作用强和功能单一。近年来,通过把水蛭素与某些功能蛋白融合表达来解决这些问题,得到的融合蛋白或在体内延长水蛭素的半衰期,或降低其出血副作用,或带来新的功能,如:溶栓、抑制血小板凝集、特异寻靶等。本文对近年来国内外水蛭素融合蛋白研究状况进行综述。Natural hirudin extracted from the secretion of medical leech salivary gland is a single-chain pepfide containing 65 aminoacid residues with molecular weight of 7000 D, and exists in three isomers of HV1, HV2 and HV3. Hirudin possesses three disulfide bridges forming the structure of core cyclic peptides, which binds to the catalytic site of thrombin so as to inhibit the catalysis of thrombin. Its c-terminus rich in acidic aminoacid residues possesses hydrophilicity, and is free on the molecular surface, and can bind with fibrin recognition site of hirudin. The minimal segment of 12 - 16 C-terminal acidic residues keeps the minimal activity of anti-thrombosis. Thus, hirudin, as a potent and specific inhibitor of thrombin, can be used to protect from and to treat clinically thrombosis. As it has some disadvantages such as short half-life, bleeding side-effect and mono-function, and so on, hirudin has been fused with some other functional proteins in recent years. The obtained fusion proteins can prolong the half life of hirudin, or relieve it bleeding side effect, or bring new functions, such as thrombolysis, inhibiting the platelet aggregation, targething specifically. The research progress in hirudin fusion protein was summarized in this review.

关 键 词：水蛭素 融合蛋白 抗凝 血栓形成 

分 类 号：R973.2[医药卫生—药品]