靶向寡肽溶栓剂  

Targeting Thrombolytic Oligopeptide

作　　者：赵逸松[1] 赵明[1] 

机构地区：[1]首都医科大学化学生物学与药学院实验中心

出　　处：《首都医科大学学报》2008年第1期103-105,共3页Journal of Capital Medical University

摘　　要：对靶向寡肽溶栓剂P6A(ARPAK)及其衍生物、RGD肽及含有自由基伪肽的靶向溶栓作用进行综述。P6A是纤溶酶原的降解产物之一,具有增加血管通透性和溶栓作用。P6A的衍生物及P6A代谢产物具有更强的溶栓作用。血栓形成中,RGD序列是纤维蛋白原与血小板结合的关键序列。将RGD序列与溶栓寡肽结合,构成了具有靶向溶栓作用的杂交寡肽。在溶栓治疗中,血流再灌注生成的大量自由基会对组织造成损伤,将自由基清除剂与溶栓寡肽结合可得到具有溶栓和自由基清除双向功能的溶栓伪肽。因为溶栓处是产生大量自由基的部位,所以含自由基清除剂的溶栓伪肽可将自由基清除剂带到自由基堆积部位,体现了靶向内涵。The targeting thrombolytic effects of P6A （ARPAK） and its derivatives, RGD peptides, nitronyl nitroxide containing peptides are reviewed. P6A, one of the degradation products from fibrinogen, is known to increase microvascular permeability and have thrombolytic effects. Its derivatives and degradation products also have potent thrombolytic effects. RGD is the key sequence in the binding of fibrinogen to platelet. The binding leads to thrombosis. Coupling RGD sequence to thrombolytic oligopeptide gives targeting thrombolytic oligopeptide. Sometimes the ischemia/reperfusion injury by free radicals is beyond thrombus itself. Binding free radical scavenger with thrombolytic oligopeptide gives peptide with two fold effects.

关 键 词：靶向溶栓寡肽 P6A PGD序列 自由基 

分 类 号：R962[医药卫生—药理学]