Synthesis of tripeptide RGD amide by a combination of chemical and enzymatic methods |
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Authors: | Rui-Zhen Hou Na Zhang Gang Li Yi-Bing Huang Hua Wang Yu-Peng Xiao Yun-Jia Liu Yan Yang Lang Zhao Xue-Zhong Zhang |
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Affiliation: | aKey Laboratory for Molecular Enzymology and Engineering of Ministry of Education, Jilin University, Changchun 130023, China bJilin Province Product Quality Supervision Testing Institute, Changchun 130022, China |
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Abstract: | The tripeptide Bz-Arg-Gly-Asp(NH2)OH was synthesized by a combination of chemical and enzymatic methods in this study. Firstly, Gly-Asp-(NH2)2 was synthesized by a novel chemical method in three steps including chloroacetylation of l-aspartic acid, esterification of chloroacetyl l-aspartic acid and ammonolysis of chloroacetyl l-aspartic acid diethyl ester. Secondly, the linkage of the third amino acid (Bz-Arg-OEt) to Gly-Asp-(NH2)2 was completed by enzymatic method under kinetic control condition. An industrial alkaline protease alcalase was used in water–organic cosolvents systems. The synthesis reaction conditions were optimized by examining the effects of several factors including water content, temperature, pH and reaction time on the yield of the synthesis product Bz-Arg-Gly-Asp(NH2)OH. The optimum conditions are pH 8.0, 35 °C, in ethanol/Tris–HCl buffer system (85:15, v/v), 8 h with the tripeptide yield of 73.6%. |
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Keywords: | RGD Peptide synthesis Alcalase Organic solvents Enzyme |
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