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| Chemoenzymatic Synthesis of Cellular Adhesion Tripeptide RGD Precursor in Organic Media | |
| 作者姓名： | WANG Hua ZHAO Mi-feng PU Li-mei DING Wei HUANG Yi-bing HOU Rui-zhen ZENG Hong-bin XU Li ZHANG Xue-zhong |
| 作者单位： | WANG Hua~ 1，2，ZHAO Mi-feng~ 1，PU Li-mei~ 3，DING Wei~ 3，HUANG Yi-bing~ 1，HOU Rui-zhen~ 1，ZENG Hong-bin~ 1，XU Li~ 1 and ZHANG Xue-zhong~ 1** 1. Key Laboratory of Molecular Enzymology and Engineering，Jilin University，Changchun 130021，P. R. China; 2. China-Japan Union Hospital，Jilin University，Changchun 130033，P. R. China; 3. First Hospital，Jilin University，Changchun 130021，P. R. China |
| 基金项目： | Supported by the Special Research Grant from State Administration of Traditional Chinese Medicine of China （No. 2004ZDZX003 ）. |
| 摘 要： | IntroductionA characteristic tripeptide sequence Arg-Gly-Asp(RGD) that is found within fibronectin and other rela-ted adhesion molecules in extracellular matrices(ECM)has received considerable attention from researcherssince it was proved to be a recognit… |
| 关 键 词： | RGD 合成 胰岛素 有机溶剂 化合酶 |
| 文章编号： | 1005-9040（2006）-06-721-06 |
| 收稿时间： | 2005-12-26 |
Chemoenzymatic Synthesis of Cellular Adhesion Tripeptide RGD Precursor in Organic Media |
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| WANG Hua ZHAO Mi-feng PU Li-mei DING Wei HUANG Yi-bing HOU Rui-zhen ZENG Hong-bin XU Li ZHANG Xue-zhong.Chemoenzymatic Synthesis of Cellular Adhesion Tripeptide RGD Precursor in Organic Media[J].Chemical Research in Chinese University,2006,22(6):721-726. | |
| Authors: | Hua WANG Mi-feng ZHAO Li-mei PU Wei DING Yi-bing HUANG Rui-zhen HOU Hong-bin ZENG Li XU Xue-zhong ZHANG |
| Institution: | aKey Laboratory of Molecular Enzymology and Engineering, Jilin University, Changchun 130021, P. R. China bChina-Japan Union Hospital, Jilin University, Changchun 130033, P. R. China cFirst Hospital, Jilin University, Changchun 130021, P. R. China |
| Abstract: | Chemoenzymatic synthesis of tripeptide Bz-RGD-(OEt)2 was conducted in this study. First, the free dipeptide Gly-Asp was synthesized via a novel chemical method, wherein only L-aspartic acid was used and was followed by the esterification of Gly-Asp. The formation of the linkage between the third amino acid Bz-Arg-OEt and Gly-Asp-(OEt)2 was completed by using the enzymatic method in organic media. The effects of several factors such as pH, the water content, triethylamine(TEA), the molar ratio of the substrates, and the reaction time on the yield of Bz-RGD-(OEt)2 were examined. It was obtained that the optimum conditions for Bz-RGD-(OEt)2 synthesis in an ethanol/Tris-HCl buffer system(volume ratio 93:7) were as follows; pH=8.0; temperature, 30 ℃; reaction time, 7 h. The tripeptide yield was 75.2%. |
| Keywords: | RGD Synthesis Trypsin Organic solvent |
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