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内吗啡肽-2的人工合成及其酶促降解
引用本文:李俊,陈钧辉,聂永军,王新昌.内吗啡肽-2的人工合成及其酶促降解[J].中国生物化学与分子生物学报,2004,20(2):270-274.
作者姓名:李俊  陈钧辉  聂永军  王新昌
作者单位:南京大学生物化学系医药生物枝术国家重点实验室,南京,210093
摘    要:内吗啡肽-2(endomorphin-2)是Zadina等人1]于1997年发现的一种具有镇痛作用的四肽,它存在于动物和人的中枢神经系统内2].它是内源性μ阿片受体的激动剂,具有高亲合性(K1=690pmol,L)和选择性(δ/μ=13400、K/μ=7600).

收稿时间:2004-04-20
修稿时间:2003年4月8日

Synthesis and Proteolysis of Endomorphin-2
LI Jun,CHEN Jun hui,NIE Yong jun,WANG Xin chang.Synthesis and Proteolysis of Endomorphin-2[J].Chinese Journal of Biochemistry and Molecular Biology,2004,20(2):270-274.
Authors:LI Jun  CHEN Jun hui  NIE Yong jun  WANG Xin chang
Affiliation:(Pharmaceutic Biotechnology Key Laboratory;Department of Biochemistry,Nanjing University,Nanjing 210093,China
Abstract:The recently discovered native endomorphin 2 plays an important role in opioid analgesia, but its metabolic fate in the organism remains relatively little known. The successful synthesis of endomorphin 2 was carried out by solution method. The C teminal dipeptide and the N terminal dipeptide have been synthesized, respectively, and then coupled successfully. High performance liquid chromatography and electrospray ionization mass spectrometry were used to identify the degradation products from the incubation of endomorphin 2 with brain synaptic membrane. The patterns of peptide metabolites indicated that brain synaptic membrane associated peptidases hydrolyzed first at the N terminal, and then split the peptide at the Phe Phe bond.
Keywords:endomorphin 2  solution phase synthesis  proteolysis  brain synaptic membrane
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