IMPROVE HAPTEN DESIGN FOR ANTICOCAINE CATALYTIC ANTIBODY

描述(申请人摘要)： 降解可卡因的催化抗体具有抗成瘾的潜力 治疗剂。此前已经发现了九种这样的催化剂， 被克隆并被诱变以提高催化活性。 然而，过渡态类似物的合成是第一个，也是关键的 在创造催化抗体方面迈出了一步，两种新的策略已经 最近有报道称，产生的抗体具有特别高的 催化活性-反应免疫和异源免疫。 利用这些策略，设计和合成了新的 可卡因苯甲酸酯水解的过渡态类似物 是提议的。这些类似物有望引发有效的抗体。 催化机理，如酸碱催化或共价催化； 具有较高的可卡因水解酶活性。

DESCRIPTION (Applicant's Abstract): Catalytic antibodies that degrade cocaine have potential as anti-addiction therapeutic agents. Nine such catalysts have been previously elicited and cloned and are being mutagenized abused to improve catalytic activity. However, the synthesis of transition-states analog is the first, critical step in the creation of catalytic antibodies and two new strategies have recently been reported for the generation of antibodies with especially high catalytic activity - reactive immunization and heterologous immunization. Utilizing these strategies, the design and synthesized novel transition-state analogs for the hydrolysis of the benzoyl ester of cocaine is proposed. These analogs are expected to elicit antibodies with potent catalytic mechanisms, such as acid-base catalysis or covalent catalysis, and high activity for the hydrolysis of cocaine.