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B27K—去B链C端三肽胰岛素的制备、生物活力与自聚合性质
引用本文:丁金国,崔大敷,张友尚. B27K—去B链C端三肽胰岛素的制备、生物活力与自聚合性质[J]. Acta biochimica et biophysica Sinica, 2003, 35(3): 215-218
作者姓名:丁金国  崔大敷  张友尚
作者单位:中国科学院上海生命科学研究院生物化学与细胞生物学研究所 上海200031(丁金国,崔大敷),中国科学院上海生命科学研究院生物化学与细胞生物学研究所 上海200031(张友尚)
摘    要:液相合成五肽Gly Phe Phe Tyr Lys(Boc)Obut,与B链C端去八肽胰岛素酶促缩合得到B2 7K 去B链C端三肽胰岛素(B2 7K DTrI,B2 7K destripeptideinsulin)。用小鼠惊厥法和小鼠降血糖法测得B2 7K DTrI的整体生物活力为标准胰岛素的 80 % ,B2 7K DTrI与人胎盘细胞膜胰岛素受体结合能力为标准胰岛素的 ( 12 5± 13 ) %。用凝胶过滤法证明B2 7K DTrI自聚合性质降低 ,具有与去B链C端五肽胰岛素相同的单体性质。在B2 7K DtrI结构中 ,B2 7T被K取代 ,其优点是在酵母中表达其前体后 ,可以很方便地通过胰蛋白酶水解获得

关 键 词:B27K-去B链C端三肽胰岛素  生物活力  单体胰岛素

Monomeric B27 Lys Destripeptide Insulin: Semisynthesis, Characterization and Biological Activity
DING Jin-Guo,CUI Da-Fu,ZHANG You-Shang. Monomeric B27 Lys Destripeptide Insulin: Semisynthesis, Characterization and Biological Activity[J]. Acta biochimica et biophysica Sinica, 2003, 35(3): 215-218
Authors:DING Jin-Guo  CUI Da-Fu  ZHANG You-Shang
Affiliation:DING Jin-Guo,CUI Da-Fu,ZHANG You-Shang *
Abstract:In this paper, we report the semisynthesis of B27 Lys destripeptide insulin (B27 Lys DTrI), i.e. destetrapeptide insulin with an additional Lys residue at the C-terminus of B-chain. B27 Lys DTrI is also monomeric as shown by gel filtration. Its in vivo biological activity is 80% in comparison with that of native insulin. The addition of a Lys residue at the C-terminus of B-chain makes it possible to obtain monomeric B27 Lys DTrI from a precursor expressed in Saccharomyces cerevesiae by tryptic hydrolysis instead of the less efficient tryptic transpeptidation.
Keywords:B27 Lys destripeptide insulin  biological activity  monomeric insulin
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