An enzymatic advance in nicotine cessation therapy.
An enzymatic advance in nicotine cessation therapy.
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DOI：
10.1039/c7cc09134f
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发表时间：
2018-02-13
期刊：
影响因子：
--
通讯作者：
Janda KD
中科院分区：
文献类型：
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作者：
Xue S ;Kallupi M ;Zhou B ;Smith LC ;Miranda PO ;George O ;Janda KD
通过融合白蛋白结合结构域来改变称为NicA 2的尼古丁降解酶（NicA 2-J1）以增加其半衰期。在体内对NicA 2-J1的检查表明，它完全阻断了大脑尼古丁的进入，这反过来又减弱了尼古丁的精神活性作用。这些数据进一步支持药代动力学尼古丁戒烟治疗的开发。
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.