化学-酶法合成RGD三肽  

Synthesis of RGD tripeptide by the combination of chemical and enzymatic method

作　　者：宋明媚[1] 鞠培培[1] 曹建军[1] 沈树宝[1] 

机构地区：[1]南京工业大学制药与生命科学学院,江苏南京210009

出　　处：《南京工业大学学报（自然科学版）》2004年第5期17-19,36,共4页Journal of Nanjing Tech University(Natural Science Edition)

基　　金：国家自然科学基金(No 29976019;No 20176018;No 20376034);江苏省自然科学基金(No BK99123;No BK200201)

摘　　要：采用化学法和酶法相结合的合成策略,合成具有高生物活性肽RGD。先采用DCC合成GD二肽(HCl·Gly Asp(oBzl)2),然后利用胰蛋白酶(trypsin)催化合成RGD三肽(Z Arg GlyAsp(oBzl)2)。实验结果表明,其中GD二肽在反应10h,两底物G与D的摩尔比为1 5∶1时,得率为77 7%;RGD三肽在微水-1,4-丁二醇反应体系中得率为41 9%。The method of synthesizing the active peptide RGD was adopted with the combinational strategies of chemistry and enzyme. DCC was used to produce GD dipeptide (HCl·Gly-Asp(oBzl)_2) , and then RGD tripeptide (Z-Arg-Gly-Asp(oBzl)_2) was enzymatically synthesized by trypsin. The results showed that the yield of GD dipeptide is 77.7% after 10 hours with the mole ratio of G and D is 1.5∶1, and under the low-water 1,4-butanediol solvents condition the yield of RGD is 41.9%.

关 键 词：酶法合成 摩尔比 催化合成 丁二醇 得率 反应体系 化学法 RGD 二肽 DCC 

分 类 号：R581[医药卫生—内分泌]