Matches in SemOpenAlex for { <https://semopenalex.org/work/W2170591768> ?p ?o ?g. }
Showing items 1 to 98 of
98
with 100 items per page.
- W2170591768 endingPage "299" @default.
- W2170591768 startingPage "292" @default.
- W2170591768 abstract "The effect of Ca(2+)/calmodulin-dependent protein kinase II (CaMK II) on voltage-gated ion channels is widely studied through the use of specific CaMK II blockers such as 2-[N-(2-hydroxyethyl)]-N-(4methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine (KN-93). The present study demonstrates that KN-93 is a direct extracellular blocker of a wide range of cloned Kv channels from a number of different subfamilies. In all channels tested, the effect of 1 microM KN-93 was independent of CaMK II because 1 microM2-[N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine, phosphate (KN-92), an inactive analog of KN-93, caused similar inhibition of currents. In addition, dialysis of cells with 10 microM CaMK II inhibitory peptide fragment 281-301 (CIP) had no effect on current kinetics and did not prevent the inhibitory effect of KN-93. The IC(50) for block of the Kv1.5 channel (used as an example to determine the nature of KN-93 block) was 307 +/- 12 nM. KN-93 blocked open channels with little voltage dependence that did not alter the V(1/2) of channel activation. Removal of P/C-type inactivation by mutation of arginine 487 to valine in the outer pore region of Kv1.5 (R487V) greatly reduced KN-93 block, whereas enhancement of inactivation induced by mutation of threonine 462 to cysteine (T462C) increased the potency of KN-93 by 4-fold. This suggested that KN-93 acted through promotion and stabilization of C-type inactivation. Importantly, KN-93 was ineffective as a blocker when applied intracellularly, suggesting that CaMK II-independent effects of KN-93 on Kv channels can be circumvented by intracellular application of KN-93." @default.
- W2170591768 created "2016-06-24" @default.
- W2170591768 creator A5069034448 @default.
- W2170591768 creator A5083962653 @default.
- W2170591768 creator A5087088567 @default.
- W2170591768 date "2005-12-20" @default.
- W2170591768 modified "2023-09-24" @default.
- W2170591768 title "KN-93 (2-[<i>N</i>-(2-Hydroxyethyl)]-<i>N</i>-(4-methoxybenzenesulfonyl)]amino-<i>N</i>-(4-chlorocinnamyl)-<i>N</i>-methylbenzylamine), a Calcium/Calmodulin-Dependent Protein Kinase II Inhibitor, Is a Direct Extracellular Blocker of Voltage-Gated Potassium Channels" @default.
- W2170591768 cites W1549930627 @default.
- W2170591768 cites W1966907929 @default.
- W2170591768 cites W1968040743 @default.
- W2170591768 cites W2017583361 @default.
- W2170591768 cites W2021438486 @default.
- W2170591768 cites W2047302188 @default.
- W2170591768 cites W2084366254 @default.
- W2170591768 cites W2085048839 @default.
- W2170591768 cites W2099642662 @default.
- W2170591768 cites W2100922563 @default.
- W2170591768 cites W2105859090 @default.
- W2170591768 cites W2107763854 @default.
- W2170591768 cites W2108765087 @default.
- W2170591768 cites W2126688997 @default.
- W2170591768 cites W2127964350 @default.
- W2170591768 cites W2128180812 @default.
- W2170591768 cites W2141584191 @default.
- W2170591768 cites W2164829352 @default.
- W2170591768 cites W2474502530 @default.
- W2170591768 cites W565127267 @default.
- W2170591768 doi "https://doi.org/10.1124/jpet.105.097618" @default.
- W2170591768 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16368898" @default.
- W2170591768 hasPublicationYear "2005" @default.
- W2170591768 type Work @default.
- W2170591768 sameAs 2170591768 @default.
- W2170591768 citedByCount "107" @default.
- W2170591768 countsByYear W21705917682012 @default.
- W2170591768 countsByYear W21705917682013 @default.
- W2170591768 countsByYear W21705917682014 @default.
- W2170591768 countsByYear W21705917682015 @default.
- W2170591768 countsByYear W21705917682016 @default.
- W2170591768 countsByYear W21705917682017 @default.
- W2170591768 countsByYear W21705917682018 @default.
- W2170591768 countsByYear W21705917682019 @default.
- W2170591768 countsByYear W21705917682020 @default.
- W2170591768 countsByYear W21705917682021 @default.
- W2170591768 countsByYear W21705917682022 @default.
- W2170591768 countsByYear W21705917682023 @default.
- W2170591768 crossrefType "journal-article" @default.
- W2170591768 hasAuthorship W2170591768A5069034448 @default.
- W2170591768 hasAuthorship W2170591768A5083962653 @default.
- W2170591768 hasAuthorship W2170591768A5087088567 @default.
- W2170591768 hasConcept C11960822 @default.
- W2170591768 hasConcept C150109051 @default.
- W2170591768 hasConcept C181199279 @default.
- W2170591768 hasConcept C184235292 @default.
- W2170591768 hasConcept C185592680 @default.
- W2170591768 hasConcept C2775880066 @default.
- W2170591768 hasConcept C2776414213 @default.
- W2170591768 hasConcept C2778565530 @default.
- W2170591768 hasConcept C29688787 @default.
- W2170591768 hasConcept C515207424 @default.
- W2170591768 hasConcept C55493867 @default.
- W2170591768 hasConcept C71240020 @default.
- W2170591768 hasConcept C97029542 @default.
- W2170591768 hasConceptScore W2170591768C11960822 @default.
- W2170591768 hasConceptScore W2170591768C150109051 @default.
- W2170591768 hasConceptScore W2170591768C181199279 @default.
- W2170591768 hasConceptScore W2170591768C184235292 @default.
- W2170591768 hasConceptScore W2170591768C185592680 @default.
- W2170591768 hasConceptScore W2170591768C2775880066 @default.
- W2170591768 hasConceptScore W2170591768C2776414213 @default.
- W2170591768 hasConceptScore W2170591768C2778565530 @default.
- W2170591768 hasConceptScore W2170591768C29688787 @default.
- W2170591768 hasConceptScore W2170591768C515207424 @default.
- W2170591768 hasConceptScore W2170591768C55493867 @default.
- W2170591768 hasConceptScore W2170591768C71240020 @default.
- W2170591768 hasConceptScore W2170591768C97029542 @default.
- W2170591768 hasIssue "1" @default.
- W2170591768 hasLocation W21705917681 @default.
- W2170591768 hasLocation W21705917682 @default.
- W2170591768 hasOpenAccess W2170591768 @default.
- W2170591768 hasPrimaryLocation W21705917681 @default.
- W2170591768 hasRelatedWork W1484512746 @default.
- W2170591768 hasRelatedWork W2007222575 @default.
- W2170591768 hasRelatedWork W2039948658 @default.
- W2170591768 hasRelatedWork W2051546871 @default.
- W2170591768 hasRelatedWork W2052334095 @default.
- W2170591768 hasRelatedWork W2052424891 @default.
- W2170591768 hasRelatedWork W2056481979 @default.
- W2170591768 hasRelatedWork W2068940962 @default.
- W2170591768 hasRelatedWork W2087473022 @default.
- W2170591768 hasRelatedWork W3034530439 @default.
- W2170591768 hasVolume "317" @default.
- W2170591768 isParatext "false" @default.
- W2170591768 isRetracted "false" @default.
- W2170591768 magId "2170591768" @default.
- W2170591768 workType "article" @default.