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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2016
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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. |
format | Online Article Text |
id | pubmed-5100928 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
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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