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. 2018 Feb 13;54(14):1686-1689.
doi: 10.1039/c7cc09134f.

An enzymatic advance in nicotine cessation therapy

Song Xue  1 , Marsida Kallupi, Bin Zhou, Lauren C Smith, Pedro O Miranda, Olivier George, Kim D Janda
Affiliations

An enzymatic advance in nicotine cessation therapy

Song Xue et al. Chem Commun (Camb). .

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.

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Conflict of interest statement

Conflicts of interest

There are no conflicts to declare.

Figures

Fig.1
Fig.1
Pharmacokinetics of NicA2 and NicA2-J1 in rat serum.
Fig. 2
Fig. 2
Effect of NicA2-J1 during nicotine withdrawal in rats. NicA2-J1 blocks total withdrawal score (A), hyperalgesia (B) and irritability like behaviour (C) during withdrawal. (Sal: saline; Nico: nicotine)
Fig. 3
Fig. 3
Nicotine concentrations in rat blood (A) after 1 or 5 days and brains (B) after 7 days of NicA2-J1 administration. (ND: not detected)
See this image and copyright information in PMC

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