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The Outer Pore and Selectivity Filter of TRPA1

TRPA1 (transient-receptor-potential-related ion channel with ankyrin domains) is a direct receptor or indirect effector for a wide variety of nociceptive signals, and thus is a compelling target for development of analgesic pharmaceuticals such as channel blockers. Recently, the structure of TRPA1 w...

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Autores principales: Christensen, Adam P., Akyuz, Nurunisa, Corey, David P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5100928/
https://www.ncbi.nlm.nih.gov/pubmed/27824920
http://dx.doi.org/10.1371/journal.pone.0166167
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author Christensen, Adam P.
Akyuz, Nurunisa
Corey, David P.
author_facet Christensen, Adam P.
Akyuz, Nurunisa
Corey, David P.
author_sort Christensen, Adam P.
collection PubMed
description TRPA1 (transient-receptor-potential-related ion channel with ankyrin domains) is a direct receptor or indirect effector for a wide variety of nociceptive signals, and thus is a compelling target for development of analgesic pharmaceuticals such as channel blockers. Recently, the structure of TRPA1 was reported, providing insights into channel assembly and pore architecture. Here we report whole-cell and single-channel current recordings of wild-type human TRPA1 as well as TRPA1 bearing point mutations of key charged residues in the outer pore. These measurements demonstrate that the glutamate at position 920 plays an important role in collecting cations into the mouth of the pore, by changing the effective surface potential by ~16 mV, while acidic residues further out have little effect on permeation. Electrophysiology experiments also confirm that the aspartate residue at position 915 represents a constriction site of the TRPA1 pore and is critical in controlling ion permeation.
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spelling pubmed-51009282016-11-18 The Outer Pore and Selectivity Filter of TRPA1 Christensen, Adam P. Akyuz, Nurunisa Corey, David P. PLoS One Research Article TRPA1 (transient-receptor-potential-related ion channel with ankyrin domains) is a direct receptor or indirect effector for a wide variety of nociceptive signals, and thus is a compelling target for development of analgesic pharmaceuticals such as channel blockers. Recently, the structure of TRPA1 was reported, providing insights into channel assembly and pore architecture. Here we report whole-cell and single-channel current recordings of wild-type human TRPA1 as well as TRPA1 bearing point mutations of key charged residues in the outer pore. These measurements demonstrate that the glutamate at position 920 plays an important role in collecting cations into the mouth of the pore, by changing the effective surface potential by ~16 mV, while acidic residues further out have little effect on permeation. Electrophysiology experiments also confirm that the aspartate residue at position 915 represents a constriction site of the TRPA1 pore and is critical in controlling ion permeation. Public Library of Science 2016-11-08 /pmc/articles/PMC5100928/ /pubmed/27824920 http://dx.doi.org/10.1371/journal.pone.0166167 Text en © 2016 Christensen et al http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/) , which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Research Article
Christensen, Adam P.
Akyuz, Nurunisa
Corey, David P.
The Outer Pore and Selectivity Filter of TRPA1
title The Outer Pore and Selectivity Filter of TRPA1
title_full The Outer Pore and Selectivity Filter of TRPA1
title_fullStr The Outer Pore and Selectivity Filter of TRPA1
title_full_unstemmed The Outer Pore and Selectivity Filter of TRPA1
title_short The Outer Pore and Selectivity Filter of TRPA1
title_sort outer pore and selectivity filter of trpa1
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5100928/
https://www.ncbi.nlm.nih.gov/pubmed/27824920
http://dx.doi.org/10.1371/journal.pone.0166167
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