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.
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.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2007年第4期668-671,共4页
Chemical Journal of Chinese Universities
基金
国家自然科学基金(批准号:30500629)
北京市科委基础专项(批准号:Z0005187040531)
中国博士后基金(批准号:2004036043)资助.
关键词
络合功能基
非天然氨基酸
生物活性肽
Chelating functional group
Unnatural amino acid
Bio-active peptide
