化学学报 ›› 2001, Vol. 59 ›› Issue (10): 1745-1750. 上一篇    下一篇

研究论文

生物素衍生化环孢素A的合成及其与人亲环素A的相互作用 研究

江辉;麻锦彪;朱向明;惠永正;吴厚铭;陈海宝   

  1. 中国科学院上海有机化学研究所.上海(200032);中国科学院生命有机化学国家 重点实验室
  • 发布日期:2001-10-15

Synthesis of biotinylated cyclosporin A and studies on its interaction with human cyclophilin A

Jiang Hui;Ma Jinbiao;Zhu Xiangming;Hui Yongzheng;Wu Houming;Chen Haibao   

  1. Shanghai Inst Organ Chem., CAS.Shanghai(200032)
  • Published:2001-10-15

通过∈-氨基已酸二聚体的乙酯与生物素缩合将其羧端延伸14个原子,然后与氨基衍生化的环孢素A缩合合成了生物素衍生化的环孢素A。经过药物免疫印迹和表面等离子体共振(SurfacePlasmonResonance)测定表明生物素衍生化的环孢素A还保留了与人亲环素A结合的活力。

关键词: 生物素, 环孢素A, 相互作用, 药物免疫印迹, 表面等离子体共振

Biotinylated cyclosporin A was synthesized by condensing the amino- derivative of cyclosporin A with ethyl N-(N-biotinlyl-∈ - aminocapronyl) -∈-aminocaproate, which was preformed from coupling biothin and the ethyl ester of dimeric ∈-aminocaproic acid to extent the carboxyl group of biotin for 14 atoms. Both of drug wastern blot and surface plasmon resonance (SPR) proved that the biotinylated cyclosporin A remained the capacity of binding human cyclophilin A.

Key words: BIOTIN, INTERACTIONS

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