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• W2346936918 startingPage "288" @default.
• W2346936918 abstract "The nicotinic acetylcholine receptor (nAChR) belongs to a superfamily of pentameric ligand-gated ion channels involved in many physiologic and pathologic processes. Among nAChRs, receptors comprising the <i>α</i>7 subunit are unique because of their high Ca²⁺ permeability and fast desensitization. nAChR agonists elicit a transient ion flux response that is further sustained by the release of calcium from intracellular sources. Owing to the dual ionotropic/metabotropic nature of <i>α</i>7 receptors, signaling pathways are activated. The <i>α</i>7 subunit is highly expressed in the nervous system, mostly in regions implicated in cognition and memory and has therefore attracted attention as a novel drug target. Additionally, its dysfunction is associated with several neuropsychiatric and neurologic disorders, such as schizophrenia and Alzheimer’s disease. <i>α</i>7 is also expressed in non-neuronal cells, particularly immune cells, where it plays a role in immunity, inflammation, and neuroprotection. Thus, <i>α</i>7 potentiation has emerged as a therapeutic strategy for several neurologic and inflammatory disorders. With unique activation properties, the receptor is a sensitive drug target carrying different potential binding sites for chemical modulators, particularly agonists and positive allosteric modulators. Although macroscopic and single-channel recordings have provided significant information about the underlying molecular mechanisms and binding sites of modulatory compounds, we know just the tip of the iceberg. Further concerted efforts are necessary to effectively exploit <i>α</i>7 as a drug target for each pathologic situation. In this article, we focus mainly on the molecular basis of activation and drug modulation of <i>α</i>7, key pillars for rational drug design." @default.
• W2346936918 created "2016-06-24" @default.
• W2346936918 creator A5015191263 @default.
• W2346936918 creator A5047559151 @default.
• W2346936918 date "2016-05-09" @default.
• W2346936918 modified "2023-10-14" @default.
• W2346936918 title "Understanding the Bases of Function and Modulation of <i>α</i>7 Nicotinic Receptors: Implications for Drug Discovery" @default.
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