| http://purl.uniprot.org/citations/20430843 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/20430843 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/20430843 | http://www.w3.org/2000/01/rdf-schema#comment | "Large conductance Ca(2+)-activated K(+) (BK) channels are known to be regulated by both intracellular Ca(2+) and voltage. Although BK channel modulators have been identified, there is a paucity of information regarding the molecular entities of this channel that govern interaction with blockers and activators. Using both whole-cell and single-channel electrophysiological studies we have characterized the possible role that a threonine residue in the pore region of the channel has on function and interaction with BK channel modulators. A threonine-to-serine substitution at position 352 (T352S) resulted in a 59-mV leftward shift in the voltage-dependent activation curve. Single-channel conductance was 236 pS for the wild-type channel and 100 pS for the T352S mutant, measured over the range -80 mV to +80 mV. In addition, there was an almost 10-fold reduction in the potency of the BK channel inhibitor 1-[1-hexyl-6-(methyloxy)-1H-indazol-3-yl]-2-methyl-1-propanone (HMIMP), the IC(50) values being 4.3 +/- 0.3 and 38.2 +/-3.3 nM for wild-type and mutant channel, respectively. There was no significant difference between wild type and the mutant channel in response to inhibition by iberiotoxin. The IC(50) was 8.1 +/- 0.3 nM for the wild type and 7.7 +/-0.3 nM for the mutant channel. Here, we have identified a residue in the pore region of the BK channel that alters voltage sensitivity and reduces the potency of the blocker HMIMP."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.org/dc/terms/identifier | "doi:10.1124/jpet.110.166017"xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.org/dc/terms/identifier | "doi:10.1124/jpet.110.166017"xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Lin Z."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Lin Z."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Xu X."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Xu X."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Gordon E."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Gordon E."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Lozinskaya I.M."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Lozinskaya I.M."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Semus S.F."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/author | "Semus S.F."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/date | "2010"xsd:gYear |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/date | "2010"xsd:gYear |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/name | "J. Pharmacol. Exp. Ther."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/name | "J. Pharmacol. Exp. Ther."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/pages | "402-409"xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/pages | "402-409"xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/title | "Characterizing the role of Thr352 in the inhibition of the large conductance Ca2+-activated K+ channels by 1-[1-Hexyl-6-(methyloxy)-1H-indazol-3-yl]-2-methyl-1-propanone."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/title | "Characterizing the role of Thr352 in the inhibition of the large conductance Ca2+-activated K+ channels by 1-[1-Hexyl-6-(methyloxy)-1H-indazol-3-yl]-2-methyl-1-propanone."xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/volume | "334"xsd:string |
| http://purl.uniprot.org/citations/20430843 | http://purl.uniprot.org/core/volume | "334"xsd:string |