高等学校化学学报

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含有络合功能基的非天然氨基酸的设计、合成及在生物活性肽中的应用

周宁1, 付慧君1, 荣嫡2, 程卯生2, 刘克良1   

    1. 军事医学科学院毒物药物研究所, 北京 100850;
    2. 沈阳药科大学制药工程学院, 沈阳110016
  • 收稿日期:2006-05-16 修回日期:1900-01-01 出版日期:2007-04-10 发布日期:2007-04-10
  • 通讯作者: 刘克良

Design, Synthesis of Unnatural Amino Acids with Chelating Functional Groups and Their Application in Bio-active Peptide

ZHOU Ning1, FU Hui-Jun1, RONG Di2, CHENG Mao-Sheng2, LIU Ke-Liang1*   

    1. Beijing Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China;
    2. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
  • Received:2006-05-16 Revised:1900-01-01 Online:2007-04-10 Published:2007-04-10
  • Contact: LIU Ke-Liang

摘要: 设计合成了一类侧链带有络合基团的非天然氨基酸, 即侧链带有N,N-二羧甲基氨甲基、N,N-二酰胺甲基氨甲基和N,N-二羟乙基氨甲基的苯丙氨酸衍生物, 并将这类非天然氨基酸用于促性腺激素释放激素(LHRH)类似物的固相合成. 高效液相色谱分析结果表明, 粗肽的纯度较好, 易于纯化; 用电喷雾质谱测定了多肽的分子量. 这些非天然氨基酸可作为其它肽类药物合成的构建单元.

关键词: 络合功能基, 非天然氨基酸, 生物活性肽

Abstract: In order to synthesize long acting bio-active peptides, some novel unnatural amino acid with chelating functional group were designed and synthesized, and were used in the solid phase synthesis of LHRH analogues. The purity of peptide was analyzed by HPLC and the structure of peptide was confirmed by ESI-MS. The experiment result shows that these unnatural amino acids could be successfully used in the solid phase synthesis of peptides as novel monomers. LHRH antagonists with functional groups show a longer duration of action and half-lives than that of model peptide in vivo and in vitro respectively.

Key words: Chelating functional group, Unnatural amino acid, Bio-active peptide

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