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Rapid CommunicationMinireview—A Latin American Perspective on Ion Channels

Understanding the Bases of Function and Modulation of α7 Nicotinic Receptors: Implications for Drug Discovery

Jeremías Corradi and Cecilia Bouzat
Molecular Pharmacology September 2016, 90 (3) 288-299; DOI: https://doi.org/10.1124/mol.116.104240
Jeremías Corradi
Instituto de Investigaciones Bioquímicas de Bahía Blanca, Universidad Nacional del Sur, CONICET/UNS, Bahía Blanca, Argentina
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Cecilia Bouzat
Instituto de Investigaciones Bioquímicas de Bahía Blanca, Universidad Nacional del Sur, CONICET/UNS, Bahía Blanca, Argentina
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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 α7 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 α7 receptors, signaling pathways are activated. The α7 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. α7 is also expressed in non-neuronal cells, particularly immune cells, where it plays a role in immunity, inflammation, and neuroprotection. Thus, α7 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 α7 as a drug target for each pathologic situation. In this article, we focus mainly on the molecular basis of activation and drug modulation of α7, key pillars for rational drug design.

Footnotes

    • Received March 7, 2016.
    • Accepted May 5, 2016.
  • This work was supported by grants from Universidad Nacional del Sur (UNS), Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), FONCYT, and the Bill and Melinda Gates Foundation to C.B.

  • dx.doi.org/10.1124/mol.116.104240.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 90 (3)
Molecular Pharmacology
Vol. 90, Issue 3
1 Sep 2016
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Rapid CommunicationMinireview—A Latin American Perspective on Ion Channels

α7 Modulation

Jeremías Corradi and Cecilia Bouzat
Molecular Pharmacology September 1, 2016, 90 (3) 288-299; DOI: https://doi.org/10.1124/mol.116.104240

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Rapid CommunicationMinireview—A Latin American Perspective on Ion Channels

α7 Modulation

Jeremías Corradi and Cecilia Bouzat
Molecular Pharmacology September 1, 2016, 90 (3) 288-299; DOI: https://doi.org/10.1124/mol.116.104240
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  • Article
    • Visual Overview
    • Abstract
    • Introduction
    • nAChR Structure and Function
    • α7 in the Nervous System in Healthy and Disease States
    • Extraneuronal α7 and Its Pleiotropic Roles
    • α7 Pharmacology and Ion Selectivity
    • α7 Channel Kinetics
    • α7 Modulation as a Therapeutic Strategy
    • α7 Allosteric Binding Sites
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  • Conversion of an Inward into an Outward Rectifier Channel
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