尼古丁戒断治疗的一项酶学进展。
An enzymatic advance in nicotine cessation therapy.
作者信息
Xue Song, Kallupi Marsida, Zhou Bin, Smith Lauren C, Miranda Pedro O, George Olivier, Janda Kim D
机构信息
Departments of Chemistry, Immunology, Microbiology and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
出版信息
Chem Commun (Camb). 2018 Feb 13;54(14):1686-1689. doi: 10.1039/c7cc09134f.
Abstract
A nicotine-degrading enzyme termed NicA2 was altered (NicA2-J1) through fusion of an albumin binding domain to increase its half-life. Examination of NicA2-J1 in vivo demonstrated a complete blockade of brain nicotine access, which in turn blunted nicotine's psychoactive effects. These data further support development of pharmacokinetic nicotine cessation therapeutics.
摘要
一种名为NicA2的尼古丁降解酶通过与白蛋白结合域融合进行改造（NicA2-J1），以延长其半衰期。对NicA2-J1进行的体内研究表明，它完全阻断了尼古丁进入大脑，进而减弱了尼古丁的精神活性作用。这些数据进一步支持了药代动力学尼古丁戒烟疗法的开发。
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