Landry D W, Zhao K, Yang G X, Glickman M, Georgiadis T M
Department of Medicine, Columbia University College of Physicians and Surgeons, New York, NY 10032.
Science. 1993 Mar 26;259(5103):1899-901. doi: 10.1126/science.8456315.
Immunization with a phosphonate monoester transition-state analog of cocaine provided monoclonal antibodies capable of catalyzing the hydrolysis of the cocaine benzoyl ester group. An assay for the degradation of radiolabeled cocaine identified active enzymes. Benzoyl esterolysis yields ecgonine methyl ester and benzoic acid, fragments devoid of cocaine's stimulant activity. Passive immunization with such an artificial enzyme could provide a treatment for dependence by blunting reinforcement.
用可卡因的膦酸单酯过渡态类似物进行免疫接种可产生能够催化可卡因苯甲酰酯基团水解的单克隆抗体。一项针对放射性标记可卡因降解的检测鉴定出了活性酶。苯甲酰酯水解产生芽子碱甲酯和苯甲酸，这些片段没有可卡因的刺激活性。用这种人工酶进行被动免疫接种可以通过减弱强化作用来治疗成瘾。
