多肽N端修饰方法研究进展

Research Progress in N-Terminal Modification of Polypeptides

多肽是源于生物体内的一类重要的生物活性物质,但由于稳定性差等原因,大大限制了其应用。通过对多肽进行结构修饰,可以改变其理化性质,进而提高其稳定性及生物活性。综述了近年来多肽N端修饰方法的研究进展,包括乙酰化、PEG(聚乙二醇)修饰、荧光试剂修饰、多肽N端亲水性基团修饰、NCL及EPL连接反应等,介绍了2-氨基辛酸、丁烯酶1、N-脒基-焦谷氨酰苯丙氨酸、N-terminal caps等多肽N端修饰实例。

Polypeptides is a kind of important bioactive substance derived from organism,however,due to their poor stability,the application of polypeptides is greatly limited.The physicochemical properties of polypeptides can be changed by modifying the structure,furthermore the stability and biological activity can be improved.We review the recent advances in N-terminal modification of polypeptides,including acetylation,PEG(polyethylene glycol)modification,fluorescent reagent modification,N-terminal hydrophilic group modification of polypeptides,and ligation reactions of NCL(national chemical ligation)and EPL(expressed protein ligation),and introduce the examples of N-terminal modification of 2-aminooctanoic acid,butelase 1,N-amidino-pyroglutamyl-phenylalanine,and N-terminal caps.