Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies
Eukaryotic voltage-gated sodium channels play key roles in physiology and are targets for many toxins and medically important drugs. Physiology, pharmacology, and general architecture of the channels has long been the subject of intensive research in academia and industry. In particular, animal toxi...
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Frontiers Media S.A.
2018-08-01
|
| Series: | Frontiers in Pharmacology |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/article/10.3389/fphar.2018.00880/full |
| _version_ | 1831674790466813952 |
|---|---|
| author | Denis B. Tikhonov Boris S. Zhorov Boris S. Zhorov |
| author_facet | Denis B. Tikhonov Boris S. Zhorov Boris S. Zhorov |
| author_sort | Denis B. Tikhonov |
| collection | DOAJ |
| description | Eukaryotic voltage-gated sodium channels play key roles in physiology and are targets for many toxins and medically important drugs. Physiology, pharmacology, and general architecture of the channels has long been the subject of intensive research in academia and industry. In particular, animal toxins such as tetrodotoxin, saxitoxin, and conotoxins have been used as molecular probes of the channel structure. More recently, X-ray structures of potassium and prokaryotic sodium channels allowed elaborating models of the toxin-channel complexes that integrated data from biophysical, electrophysiological, and mutational studies. Atomic level cryo-EM structures of eukaryotic sodium channels, which became available in 2017, show that the selectivity filter structure and other important features of the pore domain have been correctly predicted. This validates further employments of toxins and other small molecules as sensitive probes of fine structural details of ion channels. |
| first_indexed | 2024-12-20T03:50:48Z |
| format | Article |
| id | doaj.art-b75b4dccd868440db61c77936c0c8dc6 |
| institution | Directory Open Access Journal |
| issn | 1663-9812 |
| language | English |
| last_indexed | 2024-12-20T03:50:48Z |
| publishDate | 2018-08-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pharmacology |
| spelling | doaj.art-b75b4dccd868440db61c77936c0c8dc62022-12-21T19:54:28ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122018-08-01910.3389/fphar.2018.00880400645Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin StudiesDenis B. Tikhonov0Boris S. Zhorov1Boris S. Zhorov2Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, Saint Petersburg, RussiaSechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, Saint Petersburg, RussiaDepartment of Biochemistry and Biomedical Sciences, McMaster University, Hamilton, ON, CanadaEukaryotic voltage-gated sodium channels play key roles in physiology and are targets for many toxins and medically important drugs. Physiology, pharmacology, and general architecture of the channels has long been the subject of intensive research in academia and industry. In particular, animal toxins such as tetrodotoxin, saxitoxin, and conotoxins have been used as molecular probes of the channel structure. More recently, X-ray structures of potassium and prokaryotic sodium channels allowed elaborating models of the toxin-channel complexes that integrated data from biophysical, electrophysiological, and mutational studies. Atomic level cryo-EM structures of eukaryotic sodium channels, which became available in 2017, show that the selectivity filter structure and other important features of the pore domain have been correctly predicted. This validates further employments of toxins and other small molecules as sensitive probes of fine structural details of ion channels.https://www.frontiersin.org/article/10.3389/fphar.2018.00880/fullconotoxinshomology modelingligand dockinglocal anestheticstetrodotoxin |
| spellingShingle | Denis B. Tikhonov Boris S. Zhorov Boris S. Zhorov Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies Frontiers in Pharmacology conotoxins homology modeling ligand docking local anesthetics tetrodotoxin |
| title | Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies |
| title_full | Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies |
| title_fullStr | Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies |
| title_full_unstemmed | Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies |
| title_short | Predicting Structural Details of the Sodium Channel Pore Basing on Animal Toxin Studies |
| title_sort | predicting structural details of the sodium channel pore basing on animal toxin studies |
| topic | conotoxins homology modeling ligand docking local anesthetics tetrodotoxin |
| url | https://www.frontiersin.org/article/10.3389/fphar.2018.00880/full |
| work_keys_str_mv | AT denisbtikhonov predictingstructuraldetailsofthesodiumchannelporebasingonanimaltoxinstudies AT borisszhorov predictingstructuraldetailsofthesodiumchannelporebasingonanimaltoxinstudies AT borisszhorov predictingstructuraldetailsofthesodiumchannelporebasingonanimaltoxinstudies |