The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating
The outer vestibule of voltage-gated Na+ channels is formed by extracellular loops connecting the S5 and S6 segments of all four domains (“P-loops”), which fold back into the membrane. Classically, this structure has been implicated in the control of ion permeation and in toxin blockage. However, co...
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2010-04-01
|
| Series: | Marine Drugs |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1660-3397/8/4/1373/ |
| _version_ | 1798041549134626816 |
|---|---|
| author | René Cervenka Touran Zarrabi Peter Lukacs Hannes Todt |
| author_facet | René Cervenka Touran Zarrabi Peter Lukacs Hannes Todt |
| author_sort | René Cervenka |
| collection | DOAJ |
| description | The outer vestibule of voltage-gated Na+ channels is formed by extracellular loops connecting the S5 and S6 segments of all four domains (“P-loops”), which fold back into the membrane. Classically, this structure has been implicated in the control of ion permeation and in toxin blockage. However, conformational changes of the outer vestibule may also result in alterations in gating, as suggested by several P-loop mutations that gave rise to gating changes. Moreover, partial pore block by mutated toxins may reverse gating changes induced by mutations. Therefore, toxins that bind to the outer vestibule can be used to modulate channel gating. |
| first_indexed | 2024-04-11T22:23:03Z |
| format | Article |
| id | doaj.art-95888472ae674f309854c41ea04805ff |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-04-11T22:23:03Z |
| publishDate | 2010-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-95888472ae674f309854c41ea04805ff2022-12-22T03:59:59ZengMDPI AGMarine Drugs1660-33972010-04-01841373139310.3390/md8041373The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as GatingRené CervenkaTouran ZarrabiPeter LukacsHannes TodtThe outer vestibule of voltage-gated Na+ channels is formed by extracellular loops connecting the S5 and S6 segments of all four domains (“P-loops”), which fold back into the membrane. Classically, this structure has been implicated in the control of ion permeation and in toxin blockage. However, conformational changes of the outer vestibule may also result in alterations in gating, as suggested by several P-loop mutations that gave rise to gating changes. Moreover, partial pore block by mutated toxins may reverse gating changes induced by mutations. Therefore, toxins that bind to the outer vestibule can be used to modulate channel gating.http://www.mdpi.com/1660-3397/8/4/1373/tetrodotoxinsaxitoxinsodium channeluse-dependent blockrate-dependent blockouter vestibule |
| spellingShingle | René Cervenka Touran Zarrabi Peter Lukacs Hannes Todt The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating Marine Drugs tetrodotoxin saxitoxin sodium channel use-dependent block rate-dependent block outer vestibule |
| title | The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating |
| title_full | The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating |
| title_fullStr | The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating |
| title_full_unstemmed | The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating |
| title_short | The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating |
| title_sort | outer vestibule of the na channel toxin receptor and modulator of permeation as well as gating |
| topic | tetrodotoxin saxitoxin sodium channel use-dependent block rate-dependent block outer vestibule |
| url | http://www.mdpi.com/1660-3397/8/4/1373/ |
| work_keys_str_mv | AT renecervenka theoutervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT touranzarrabi theoutervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT peterlukacs theoutervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT hannestodt theoutervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT renecervenka outervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT touranzarrabi outervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT peterlukacs outervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating AT hannestodt outervestibuleofthenachanneltoxinreceptorandmodulatorofpermeationaswellasgating |