化学学报 ›› 2003, Vol. 61 ›› Issue (3): 406-410. 上一篇    下一篇

研究论文

固定化酶催化合成CCK-8C-端三肽衍生物

郭丽;张凌之;吕子敏;徐正   

  1. 四川大学华西药学院;四川大学化学工程学院;华中科技大学同济医学院药学 院
  • 发布日期:2003-03-15

Synthesis of a CCK-8 C-Terminal Tripeptide Derivative Catalyzed by Immobilized Enzyme

Guo Li;Zhang Lingzhi;Lu Zimin;Xu Zheng   

  1. West China Shool of Pharmacy,Sichuan University;College of Chemical Engineering,Sichuan University;School of Pharmacy,Tongji Medical College,Huazhong University of Science and Technology
  • Published:2003-03-15

报道胆囊收缩素(CCK-8)C-末端片段三肽衍生物外Hpac-Met_Asp(Cam为起始 原料,采用三种固定化酶--α-糜蛋白酶/Celite-545、木瓜蛋白酶/VA-Epoxy、 步酶促反应得到目标三肽化合物.对酶的专一性、酶的固定化、溶剂选择和合成条 件等进行了研究,比较了自由酶法与固定化酶法的结果.

关键词: 多肽, 固定化酶, 蛋白酶, 合成

Synthesis of tripeptide derivative Phac-Met-Asp(OMe)-Phe-NH_2 catalyzed by immobilized enzyme is reported. This tripeptide is a fragment of cholecystokinin C-terminal octapeptide CCK-8. Starting with Phac-Met-OCam, the target tripeptide derivative was successfully synthesized with three immobilized enzymes, a-chymotrypsin/ Celite-545, papain/VA-Epoxy and thermolysin/Celite-545 by three reaction steps in reasonable yields. The choice of appropriate enzymes, solvents and immobilization was studied. By a comparative study of free and immobilized enzymatic synthesis, the results also show some advantages of the use of immobilized enzymes.

Key words: POLYPEPTIDE, POLYPEPTIDE, PROTEASE, SYNTHESIS

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