作者:Rajendra Joshi、Liping Meng、Heiner Eckstein
DOI:10.1002/hlca.200890128
日期:2008.6
The Bz-Arg group was used as an N-terminal protecting group in the synthesis of the tripeptide fragment. The protected CCK-8 was treated with trypsin to remove the Bz-Arg group successfully. Free or immobilized enzymes were used as catalysts. The effect of the acyl donor ester structure, the C(α) protecting group of the nucleophile, reaction media, enzyme, and the carrier of the enzymes on the outcome
报道了胆囊收缩素八肽(CCK-8)的酶促合成。靶八肽CCK-8是具有与天然胆囊收缩素相同的生物学活性的最小活性序列,并且是控制胃肠功能的潜在治疗剂,并且是治疗癫痫和肥胖症的候选药物。通过将Bz-Arg-Asp(OEt)-Tyr-Met-OAl和Gly-Trp-Met-Asp(OMe)-Phe-NH 2与固定的α一起孵育获得受保护的CCK-8-胰凝乳蛋白酶。在三肽片段的合成中,Bz-Arg基团被用作N端保护基。用胰蛋白酶处理受保护的CCK-8,以成功去除Bz-Arg基团。游离的或固定的酶用作催化剂。研究了酰基给体酯结构,亲核试剂的C(α)保护基,反应介质,酶和酶载体对偶联反应结果的影响。