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

Daniel Bertrand | Zendy; Sonia Bertrand | Zendy; Estelle Neveu | Zendy; Prabhavathi Fernandes | Zendy

Open Access

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

Author(s) -

Daniel Bertrand,

Sonia Bertrand,

Estelle Neveu,

Prabhavathi Fernandes

Publication year - 2010

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00840-10

Subject(s) - telithromycin , nicotinic agonist , acetylcholine receptor , acetylcholine , myasthenia gravis , neuromuscular junction , ketolide , nicotinic acetylcholine receptor , cholinergic , pharmacology , vagus nerve , receptor , biology , medicine , immunology , neuroscience , stimulation , antibacterial agent , microbiology and biotechnology , antibiotics

Adverse effects have limited the clinical use of telithromycin. Preferential inhibition of the nicotinic acetylcholine receptors (nAChR) at the neuromuscular junction (α3β2 and NMJ), the ciliary ganglion of the eye (α3β4 and α7), and the vagus nerve innervating the liver (α7) 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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