Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels
Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could represent an interesting lead compound. Therefore, clathrodin was reinvestigated for its...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2014-04-01
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| Series: | Marine Drugs |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1660-3397/12/4/2132 |
| _version_ | 1797999630989918208 |
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| author | Steve Peigneur Aleš Žula Nace Zidar Fiona Chan-Porter Robert Kirby David Madge Janez Ilaš Danijel Kikelj Jan Tytgat |
| author_facet | Steve Peigneur Aleš Žula Nace Zidar Fiona Chan-Porter Robert Kirby David Madge Janez Ilaš Danijel Kikelj Jan Tytgat |
| author_sort | Steve Peigneur |
| collection | DOAJ |
| description | Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could represent an interesting lead compound. Therefore, clathrodin was reinvestigated for its potency and NaV channel subtype selectivity. Clathrodin and its synthetic analogues were subjected to screening on a broad range of NaV channel isoforms, both in voltage clamp and patch clamp conditions. Even though clathrodin was not found to exert any activity, some analogues were capable of modulating the NaV channels, hereby validating the pyrrole-2-aminoimidazole alkaloid structure as a core structure for future small molecule-based NaV channel modulators. |
| first_indexed | 2024-04-11T11:07:44Z |
| format | Article |
| id | doaj.art-ae4d9687a1d8427f8427040fc63d88ca |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-04-11T11:07:44Z |
| publishDate | 2014-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-ae4d9687a1d8427f8427040fc63d88ca2022-12-22T04:28:14ZengMDPI AGMarine Drugs1660-33972014-04-011242132214310.3390/md12042132md12042132Action of Clathrodin and Analogues on Voltage-Gated Sodium ChannelsSteve Peigneur0Aleš Žula1Nace Zidar2Fiona Chan-Porter3Robert Kirby4David Madge5Janez Ilaš6Danijel Kikelj7Jan Tytgat8Catholic University Leuven (KULeuven), Toxicology and Pharmacology, Herestraat 49-Box 922, 3000 Leuven, BelgiumUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, SloveniaUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, SloveniaXention Ltd., Iconix Park, London Road, Pampisford, Cambridge CB22 3EG, UKXention Ltd., Iconix Park, London Road, Pampisford, Cambridge CB22 3EG, UKXention Ltd., Iconix Park, London Road, Pampisford, Cambridge CB22 3EG, UKUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, SloveniaUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, SloveniaCatholic University Leuven (KULeuven), Toxicology and Pharmacology, Herestraat 49-Box 922, 3000 Leuven, BelgiumClathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could represent an interesting lead compound. Therefore, clathrodin was reinvestigated for its potency and NaV channel subtype selectivity. Clathrodin and its synthetic analogues were subjected to screening on a broad range of NaV channel isoforms, both in voltage clamp and patch clamp conditions. Even though clathrodin was not found to exert any activity, some analogues were capable of modulating the NaV channels, hereby validating the pyrrole-2-aminoimidazole alkaloid structure as a core structure for future small molecule-based NaV channel modulators.http://www.mdpi.com/1660-3397/12/4/2132clathrodinoroidinhymenidinvoltage-gated sodium channelssodium channel modulatorsponge |
| spellingShingle | Steve Peigneur Aleš Žula Nace Zidar Fiona Chan-Porter Robert Kirby David Madge Janez Ilaš Danijel Kikelj Jan Tytgat Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels Marine Drugs clathrodin oroidin hymenidin voltage-gated sodium channels sodium channel modulator sponge |
| title | Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels |
| title_full | Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels |
| title_fullStr | Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels |
| title_full_unstemmed | Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels |
| title_short | Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels |
| title_sort | action of clathrodin and analogues on voltage gated sodium channels |
| topic | clathrodin oroidin hymenidin voltage-gated sodium channels sodium channel modulator sponge |
| url | http://www.mdpi.com/1660-3397/12/4/2132 |
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