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Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channelsZidar, Nace ...We have prepared three alkaloids from the Agelas sponges, clathrodin, hymenidin and oroidin, and a series of their synthetic analogues, and evaluated their inhibitory effect against six isoforms of ... the Kv1 subfamily of voltage-gated potassium channels, Kv1.1-Kv1.6, expressed in Chinese Hamster ovary (CHO) cells using automated patch clamp electrophysiology assay. The most potent inhibitor was the (E)-N-(3-(2-amino-1H-imidazol-4-yl)allyl)-4,5-dichloro-1H-pyrrole-2-carboxamide (6g) with IC50 values between 1.4 and 6.1 microM against Kv1.3, Kv1.4, Kv1.5 and Kv1.6 channels. All compounds tested displayed selectivity against Kv1.1 and Kv1.2 channels. For confirmation of their activity and selectivity, compounds were additionally evaluated in the second independent system against Kv1.1-Kv1.6 and Kv10.1 channels expressed in Xenopus laevis oocytes under voltage clamp conditions where IC50 values against Kv1.3-Kv1.6 channels for the most active analogues (e.g. 6g) were lower than 1 microM. Because of the observed low sub-micromolar IC50 values and fairly low molecular weights, the prepared compounds represent good starting points for further optimisation towards more potent and selective voltage-gated potassium channel inhibitors.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 139, Oct. 2017, str. 232-241)Type of material - article, component partPublish date - 2017Language - englishCOBISS.SI-ID - 4360049
Author
Zidar, Nace |
Žula, Aleš |
Tomašič, Tihomir |
Rogers, Marc |
Kirby, Robert W. |
Tytgat, Jan |
Peigneur, Steve |
Kikelj, Danijel |
Ilaš, Janez |
Peterlin-Mašič, Lucija
Topics
Farmacevtska kemija |
voltage-gated potassium channel |
Kv1 |
modulator |
inhibitor |
clathrodin |
oroidin |
hymenidin
source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 139, Oct. 2017, str. 232-241)
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DRS, in which the journal is indexed
Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Zidar, Nace | 28905 |
Žula, Aleš | 33054 |
Tomašič, Tihomir | 28334 |
Rogers, Marc | |
Kirby, Robert W. | |
Tytgat, Jan | |
Peigneur, Steve | |
Kikelj, Danijel | 01463 |
Ilaš, Janez | 24400 |
Peterlin-Mašič, Lucija | 19317 |
Source: Personal bibliographies
and: SICRIS
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