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| Protease-catalyzed Synthesis of Bz-Arg-Gly-Asp-OMe in Full Aqueous Medium | |
| 作者单位： | HOU Rui-zhen1，2，LI Hong-mei3，LIU Yun-jia1，ZHANG Long2，XU Li1 and ZHANG Xue-zhong11.Key Laboratory for Molecular Enzymology and Engineering of Ministry of Education，Jilin University，Changchun 130021，P.R.China;2.College of Chemical Engineering，Changchun University of Technology，Changchun 130012，P.R.China;3.College of Food Engineering，Jilin Agricultural University，Changchun 130018，P.R.China |
| 基金项目： | Supported by the Scientific Research Foundation for the Returned Overseas Chinese Scholars of Ministry of Education, China. |
| 摘 要： | Synthesis of N-benzoyl-argininylglycylasparagine methyl ester(Bz-Arg-Gly-Asp-OMe),a precursor tripeptide of Arg-Gly-Asp)was catalyzed by papain under kinetic control,at alkaline pH,in a full aqueous medium.The substrates were N-benzoyl-argininylglycine ethyl ester and asparagine dimethyl ester.An aqueous solution of 0.1 mol/L KCl/NaOH containing 8 mmol/L EDTA and 2 mmol/L DTT was selected as the reaction medium.The synthesized hydrophilic tripeptide was soluble in the reaction medium during the reaction process,however,the secondary hydro-lysis of the tripeptide product was not considerable.The effects of different factors,including water content,temperature,reaction time,and molar ratio of the substrates,on the yield of Bz-Arg-Gly-Asp-OMe were examined.The optimal reaction conditions were 0.05 mol/L Bz-Arg-Gly-OEt and 0.15 mol/L Asp(-OMe)2·HCl in 0.1 mol/L KCl/NaOH solution(pH 8.5),at 40 ℃,and a reaction time of 60 min,with a maximum conversion yield of 62.4%. |
| 关 键 词： | 蛋白酶催化合成 木瓜蛋白酶 缩氨酸 反应动力学控制 |
| 文章编号： | 1005-9040（2007）-06-693-04 |
| 收稿时间： | 2007-03-12 |
Protease-catalyzed Synthesis of Bz-Arg-Gly-Asp-OMe in Full Aqueous Medium |
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| Authors: | Rui-zhen HOU Hong-mei LI Yun-jia LIU Long ZHANG Li XU Xue-zhong ZHANG |
| Institution: | aKey Laboratory for Molecular Enzymology and Engineering of Ministry of Education, Jilin University, Changchun 130021, P. R. China bCollege of Chemical Engineering, Changchun University of Technology, Changchun 130012, P. R. China cCollege of Food Engineering, Jilin Agricultural University, Changchun 130018, P. R. China |
| Abstract: | Synthesis of N-benzoyl-argininylglycylasparagine methyl ester(Bz-Arg-Gly-Asp-OMe), a precursor tripeptide of Arg-Gly-Asp) was catalyzed by papain under kinetic control, at alkaline pH, in a full aqueous medium. The substrates were N-benzoyl-argininylglycine ethyl ester and asparagine dimethyl ester. An aqueous solution of 0. 1 mol/L KCl/NaOH containing 8 mmol/L EDTA and 2 mmol/L DTT was selected as the reaction medium. The synthesized hydrophilic tripeptide was soluble in the reaction medium during the reaction process, however, the secondary hydrolysis of the tripeptide product was not considerable. The effects of different factors, including water content, temperature, reaction time, and molar ratio of the substrates, on the yield of Bz-Arg-Gly-Asp-OMe were examined. The optimal reaction conditions were 0.05 mol/L Bz-Arg-Gly-OEt and 0.15 mol/L Asp(-OMe)2 · HCl in 0.1 mol/L KCl/NaOH solution(pH 8.5), at 40 ℃, and a reaction time of 60 min, with a maximum conversion yield of 62.4%. |
| Keywords: | RGD Peptide synthesis Papain Kinetic control |
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