Matches in SemOpenAlex for { <https://semopenalex.org/work/W2159579442> ?p ?o ?g. }
Showing items 1 to 94 of
94
with 100 items per page.
- W2159579442 endingPage "1017" @default.
- W2159579442 startingPage "1009" @default.
- W2159579442 abstract "Retigabine (RTG) is an anticonvulsant drug with a novel mechanism of action. It activates neuronal KCNQ-type K<sup>+</sup> channels by inducing a large hyperpolarizing shift of steady-state activation. To identify the structural determinants of KCNQ channel activation by RTG, we constructed a set of chimeras using the neuronal K<sub>v</sub>7.2 (<i>KCNQ2</i>) channel, which is activated by RTG, and the cardiac K<sub>v</sub>7.1 (<i>KCNQ1</i>) channel, which is not affected by this drug. Substitution of either the S5 or the S6 segment in K<sub>v</sub>7.2 by the respective parts of K<sub>v</sub>7.1 led to a complete loss of activation by RTG. Trp236 in the cytoplasmic part of S5 and the conserved Gly301 in S6 (K<sub>v</sub>7.2), considered as the gating hinge (Ala336 in K<sub>v</sub>7.1), were found to be crucial for the RTG effect: mutation of these residues could either knockout the effect in K<sub>v</sub>7.2 or restore it partially in K<sub>v</sub>7.1/K<sub>v</sub>7.2 chimeras. We propose that RTG binds to a hydrophobic pocket formed upon channel opening between the cytoplasmic parts of S5 and S6 involving Trp236 and the channel9s gate, which could well explain the strong shift in voltage-dependent activation." @default.
- W2159579442 created "2016-06-24" @default.
- W2159579442 creator A5012200757 @default.
- W2159579442 creator A5027802963 @default.
- W2159579442 creator A5034571694 @default.
- W2159579442 creator A5064140338 @default.
- W2159579442 creator A5071739030 @default.
- W2159579442 date "2005-01-20" @default.
- W2159579442 modified "2023-10-03" @default.
- W2159579442 title "The New Anticonvulsant Retigabine Favors Voltage-Dependent Opening of the K<sub>v</sub>7.2 (<i>KCNQ2</i>) Channel by Binding to Its Activation Gate" @default.
- W2159579442 cites W1491033866 @default.
- W2159579442 cites W1892342982 @default.
- W2159579442 cites W1969680395 @default.
- W2159579442 cites W1976255701 @default.
- W2159579442 cites W1987357626 @default.
- W2159579442 cites W1990039788 @default.
- W2159579442 cites W1997537641 @default.
- W2159579442 cites W2012422753 @default.
- W2159579442 cites W2013844266 @default.
- W2159579442 cites W2015642465 @default.
- W2159579442 cites W2035175313 @default.
- W2159579442 cites W2055766784 @default.
- W2159579442 cites W2057552859 @default.
- W2159579442 cites W2059690890 @default.
- W2159579442 cites W2103860767 @default.
- W2159579442 cites W2106207499 @default.
- W2159579442 cites W2124416664 @default.
- W2159579442 cites W2137263523 @default.
- W2159579442 cites W2140894987 @default.
- W2159579442 cites W2143070723 @default.
- W2159579442 cites W2149633241 @default.
- W2159579442 cites W2150315832 @default.
- W2159579442 cites W2159554438 @default.
- W2159579442 cites W2168858520 @default.
- W2159579442 doi "https://doi.org/10.1124/mol.104.010793" @default.
- W2159579442 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15662042" @default.
- W2159579442 hasPublicationYear "2005" @default.
- W2159579442 type Work @default.
- W2159579442 sameAs 2159579442 @default.
- W2159579442 citedByCount "236" @default.
- W2159579442 countsByYear W21595794422012 @default.
- W2159579442 countsByYear W21595794422013 @default.
- W2159579442 countsByYear W21595794422014 @default.
- W2159579442 countsByYear W21595794422015 @default.
- W2159579442 countsByYear W21595794422016 @default.
- W2159579442 countsByYear W21595794422017 @default.
- W2159579442 countsByYear W21595794422018 @default.
- W2159579442 countsByYear W21595794422019 @default.
- W2159579442 countsByYear W21595794422020 @default.
- W2159579442 countsByYear W21595794422021 @default.
- W2159579442 countsByYear W21595794422022 @default.
- W2159579442 countsByYear W21595794422023 @default.
- W2159579442 crossrefType "journal-article" @default.
- W2159579442 hasAuthorship W2159579442A5012200757 @default.
- W2159579442 hasAuthorship W2159579442A5027802963 @default.
- W2159579442 hasAuthorship W2159579442A5034571694 @default.
- W2159579442 hasAuthorship W2159579442A5064140338 @default.
- W2159579442 hasAuthorship W2159579442A5071739030 @default.
- W2159579442 hasConcept C12554922 @default.
- W2159579442 hasConcept C185592680 @default.
- W2159579442 hasConcept C194544171 @default.
- W2159579442 hasConcept C71240020 @default.
- W2159579442 hasConcept C8010536 @default.
- W2159579442 hasConcept C83743174 @default.
- W2159579442 hasConcept C86803240 @default.
- W2159579442 hasConceptScore W2159579442C12554922 @default.
- W2159579442 hasConceptScore W2159579442C185592680 @default.
- W2159579442 hasConceptScore W2159579442C194544171 @default.
- W2159579442 hasConceptScore W2159579442C71240020 @default.
- W2159579442 hasConceptScore W2159579442C8010536 @default.
- W2159579442 hasConceptScore W2159579442C83743174 @default.
- W2159579442 hasConceptScore W2159579442C86803240 @default.
- W2159579442 hasIssue "4" @default.
- W2159579442 hasLocation W21595794421 @default.
- W2159579442 hasLocation W21595794422 @default.
- W2159579442 hasOpenAccess W2159579442 @default.
- W2159579442 hasPrimaryLocation W21595794421 @default.
- W2159579442 hasRelatedWork W1964262438 @default.
- W2159579442 hasRelatedWork W1969238396 @default.
- W2159579442 hasRelatedWork W1987359194 @default.
- W2159579442 hasRelatedWork W2002540382 @default.
- W2159579442 hasRelatedWork W2009199467 @default.
- W2159579442 hasRelatedWork W2024815166 @default.
- W2159579442 hasRelatedWork W2072589449 @default.
- W2159579442 hasRelatedWork W2144257031 @default.
- W2159579442 hasRelatedWork W2900821546 @default.
- W2159579442 hasRelatedWork W3028303481 @default.
- W2159579442 hasVolume "67" @default.
- W2159579442 isParatext "false" @default.
- W2159579442 isRetracted "false" @default.
- W2159579442 magId "2159579442" @default.
- W2159579442 workType "article" @default.