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Review ArticleReview Article

Seeking Structural Specificity: Direct Modulation of Pentameric Ligand-Gated Ion Channels by Alcohols and General Anesthetics

Rebecca J. Howard, James R. Trudell and R. Adron Harris
Leslie A. Morrow, ASSOCIATE EDITOR
Pharmacological Reviews April 2014, 66 (2) 396-412; DOI: https://doi.org/10.1124/pr.113.007468
Rebecca J. Howard
Department of Chemistry, Skidmore College, Saratoga Springs, New York (R.J.H.); Department of Anesthesia, Stanford University School of Medicine, Stanford, California (J.R.T.); and Waggoner Center for Alcohol and Addiction Research, The University of Texas at Austin, Austin, Texas (R.A.H.)
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James R. Trudell
Department of Chemistry, Skidmore College, Saratoga Springs, New York (R.J.H.); Department of Anesthesia, Stanford University School of Medicine, Stanford, California (J.R.T.); and Waggoner Center for Alcohol and Addiction Research, The University of Texas at Austin, Austin, Texas (R.A.H.)
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R. Adron Harris
Department of Chemistry, Skidmore College, Saratoga Springs, New York (R.J.H.); Department of Anesthesia, Stanford University School of Medicine, Stanford, California (J.R.T.); and Waggoner Center for Alcohol and Addiction Research, The University of Texas at Austin, Austin, Texas (R.A.H.)
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Leslie A. Morrow
Department of Chemistry, Skidmore College, Saratoga Springs, New York (R.J.H.); Department of Anesthesia, Stanford University School of Medicine, Stanford, California (J.R.T.); and Waggoner Center for Alcohol and Addiction Research, The University of Texas at Austin, Austin, Texas (R.A.H.)
Roles: ASSOCIATE EDITOR
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Abstract

Alcohols and other anesthetic agents dramatically alter neurologic function in a wide range of organisms, yet their molecular sites of action remain poorly characterized. Pentameric ligand-gated ion channels, long implicated in important direct effects of alcohol and anesthetic binding, have recently been illuminated in renewed detail thanks to the determination of atomic-resolution structures of several family members from lower organisms. These structures provide valuable models for understanding and developing anesthetic agents and for allosteric modulation in general. This review surveys progress in this field from function to structure and back again, outlining early evidence for relevant modulation of pentameric ligand-gated ion channels and the development of early structural models for ion channel function and modulation. We highlight insights and challenges provided by recent crystal structures and resulting simulations, as well as opportunities for translation of these newly detailed models back to behavior and therapy.

Footnotes

  • This work was supported by the National Institutes of Health National Institute on Alcohol Abuse and Alcoholism [Grants R01-AA06399 (to R.A.H.) and R01-AA013378 (to J.R.T.)]; and startup funds from Skidmore College.

  • dx.doi.org/10.1124/pr.113.007468.

  • Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 66 (2)
Pharmacological Reviews
Vol. 66, Issue 2
1 Apr 2014
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Review ArticleReview Article

Ligand-Gated Ion Channel Alcohol Sites

Rebecca J. Howard, James R. Trudell and R. Adron Harris
Pharmacological Reviews April 1, 2014, 66 (2) 396-412; DOI: https://doi.org/10.1124/pr.113.007468

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Review ArticleReview Article

Ligand-Gated Ion Channel Alcohol Sites

Rebecca J. Howard, James R. Trudell and R. Adron Harris
Pharmacological Reviews April 1, 2014, 66 (2) 396-412; DOI: https://doi.org/10.1124/pr.113.007468
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  • Article
    • Abstract
    • I. Introduction
    • II. Functional Evidence for Modulation
    • III. The Evolution of Accurate Structural Models
    • IV. Crystallographic Contributions
    • V. From Structure Back to Function
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