Molecular Characterization of Off-Target Activities of Telithromycin: a Potential Role for Nicotinic Acetylcholine Receptors

被引：52

作者：

Bertrand, Daniel ^{[1
]}

Bertrand, Sonia ^{[1
]}

Neveu, Estelle ^{[1
]}

Fernandes, Prabhavathi ^{[2
]}

机构：

[1] HiQScreen Sarl, CH-1206 Geneva, Switzerland

[2] Cempra Pharmaceut Inc, Chapel Hill, NC 27514 USA

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2010年 / 54卷 / 12期

关键词：

SYSTEM;

D O I：

10.1128/AAC.00840-10

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Adverse effects have limited the clinical use of telithromycin. Preferential inhibition of the nicotinic acetylcholine receptors (nAChR) at the neuromuscular junction (alpha 3 beta 2 and NMJ), the ciliary ganglion of the eye (alpha 3 beta 4 and alpha 7), and the vagus nerve innervating the liver (alpha 7) could account for the exacerbation of myasthenia gravis, the visual disturbance, and the liver failure seen with telithromycin use. The studies presented here enable the prediction of expected side effects of macrolides in development, such as solithromycin (CEM-101).

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收藏

页码：5399 / 5402

页数：4

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