重组人粒细胞集落刺激因子的N端氨基定点PEG化修饰_英文_.pdfVIP

ISSN 1007-7626 20095 CN 11-3870PQ Chinese Journal of Biochemistry and olecular Biology 25(5):421~ 428 N-Terminal Site-specific Mono-PEGylation of Recombinant Human Granulocyte Colony-Stimulating Factor 1) 1) * 1) 1) NIEYong-Jun , CHEN Jun-Hui , WANG Xin-Chang , TAN Xiao-Jun , 1) 2) 2) WANG Wen-Li , ZHU Hao-Wen , RONG Zh-i Gang 1) ( State Key Laboratory of Pharmaceutical Biotechnology , School of Lfi e sciences , N anj ing 2) University , Nanj ing 210093, China ; Biop harmaceutical Institute of Jiangsu Wu hong , Su hou 215000, China) Abstract Despite of all its therapeutic values for human beings, the use of recombinant human granulocyte colony-stimulating factor (rhG-CSF) has a primary limitation because of its short half-life in the peripheral blood. In order to solvethis problem, theN-terminus of rhG-CSFwas PEGylated in a site-specificmanner by methoxy poly-ethyleneglycol (mPEG) propionaldehydeswith an average molecularweight of either 5 kD or 20 4 kD, respectively. With a statistical L9(3 ) orthogonal test, theoptimal conditions of thesite-specific reaction were achieved. The results indicated that PEG-rhG-CSF had higher stability than unmodified rhG-CSF while incubatedwith protease orhuman serumorplaced in an extreme environment such as at an extr