FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1998450521> ?p ?o ?g. }

• W1998450521 endingPage "307" @default.
• W1998450521 startingPage "301" @default.
• W1998450521 abstract "Block of cardiac hERG K+ channels by the antihistamine terfenadine and the prokinetic agent cisapride is associated with prolonged ventricular repolarization and an increased risk of ventricular arrhythmia. Here, we used a site-directed mutagenesis approach to determine the molecular determinants of hERG block by terfenadine and cisapride. Wild-type and mutant hERG channels were heterologously expressed in Xenopus laevis oocytes and characterized by measuring whole cell currents with two-microelectrode voltage clamp techniques. Mutation of T623, S624, Y652, or F656 to Ala reduced channel sensitivity to block by terfenadine. The same mutations reduced sensitivity to cisapride. These data confirm our previous findings that polar residues (T623, S624) located near the base of the pore helix and aromatic residues (Y652, F656) located in the S6 domain are key molecular determinants of the hERG drug binding site. Unlike methanesulfonanilides (dofetilide, MK-499, E-4031, ibutilide) or clofilium, mutation of V625, G648, or V659 did not alter the sensitivity of hERG channels to terfenadine or cisapride. As previously proposed by molecular modeling studies (Farid R, et al. Bioorg Med Chem. 2006;14:3160–3173), our findings suggest that different drugs can adopt distinct modes of binding to the central cavity of hERG." @default.
• W1998450521 created "2016-06-24" @default.
• W1998450521 creator A5002110232 @default.
• W1998450521 creator A5009709419 @default.
• W1998450521 creator A5026074309 @default.
• W1998450521 creator A5035295738 @default.
• W1998450521 creator A5065253647 @default.
• W1998450521 date "2008-01-01" @default.
• W1998450521 modified "2023-10-11" @default.
• W1998450521 title "Molecular Determinants of hERG Channel Block by Terfenadine and Cisapride" @default.
• W1998450521 cites W1966686987 @default.
• W1998450521 cites W1968098810 @default.
• W1998450521 cites W1975869151 @default.
• W1998450521 cites W1976692785 @default.
• W1998450521 cites W1987388257 @default.
• W1998450521 cites W1988608385 @default.
• W1998450521 cites W1992543313 @default.
• W1998450521 cites W2000392878 @default.
• W1998450521 cites W2003676394 @default.
• W1998450521 cites W2006090981 @default.
• W1998450521 cites W2006964534 @default.
• W1998450521 cites W2010545500 @default.
• W1998450521 cites W2018987751 @default.
• W1998450521 cites W2024225383 @default.
• W1998450521 cites W2042204350 @default.
• W1998450521 cites W2048248990 @default.
• W1998450521 cites W2049958044 @default.
• W1998450521 cites W2052445226 @default.
• W1998450521 cites W2060579130 @default.
• W1998450521 cites W2070624290 @default.
• W1998450521 cites W2074705578 @default.
• W1998450521 cites W2094349878 @default.
• W1998450521 cites W2099302673 @default.
• W1998450521 cites W2099727280 @default.
• W1998450521 cites W2107763854 @default.
• W1998450521 cites W2117669007 @default.
• W1998450521 cites W2128780696 @default.
• W1998450521 cites W2133592132 @default.
• W1998450521 cites W2138266550 @default.
• W1998450521 cites W2169279691 @default.
• W1998450521 cites W2311119413 @default.
• W1998450521 cites W2415594583 @default.
• W1998450521 cites W4238094939 @default.
• W1998450521 cites W83140495 @default.
• W1998450521 doi "https://doi.org/10.1254/jphs.08102fp" @default.
• W1998450521 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2845965" @default.
• W1998450521 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18987434" @default.
• W1998450521 hasPublicationYear "2008" @default.
• W1998450521 type Work @default.
• W1998450521 sameAs 1998450521 @default.
• W1998450521 citedByCount "96" @default.
• W1998450521 countsByYear W19984505212012 @default.
• W1998450521 countsByYear W19984505212013 @default.
• W1998450521 countsByYear W19984505212014 @default.
• W1998450521 countsByYear W19984505212015 @default.
• W1998450521 countsByYear W19984505212016 @default.
• W1998450521 countsByYear W19984505212017 @default.
• W1998450521 countsByYear W19984505212018 @default.
• W1998450521 countsByYear W19984505212019 @default.
• W1998450521 countsByYear W19984505212020 @default.
• W1998450521 countsByYear W19984505212021 @default.
• W1998450521 countsByYear W19984505212022 @default.
• W1998450521 countsByYear W19984505212023 @default.
• W1998450521 crossrefType "journal-article" @default.
• W1998450521 hasAuthorship W1998450521A5002110232 @default.
• W1998450521 hasAuthorship W1998450521A5009709419 @default.
• W1998450521 hasAuthorship W1998450521A5026074309 @default.
• W1998450521 hasAuthorship W1998450521A5035295738 @default.
• W1998450521 hasAuthorship W1998450521A5065253647 @default.
• W1998450521 hasBestOaLocation W19984505211 @default.
• W1998450521 hasConcept C118441451 @default.
• W1998450521 hasConcept C12554922 @default.
• W1998450521 hasConcept C126322002 @default.
• W1998450521 hasConcept C185592680 @default.
• W1998450521 hasConcept C2776119469 @default.
• W1998450521 hasConcept C2777796741 @default.
• W1998450521 hasConcept C2779303165 @default.
• W1998450521 hasConcept C2779362680 @default.
• W1998450521 hasConcept C71924100 @default.
• W1998450521 hasConcept C83743174 @default.
• W1998450521 hasConcept C86803240 @default.
• W1998450521 hasConcept C98274493 @default.
• W1998450521 hasConceptScore W1998450521C118441451 @default.
• W1998450521 hasConceptScore W1998450521C12554922 @default.
• W1998450521 hasConceptScore W1998450521C126322002 @default.
• W1998450521 hasConceptScore W1998450521C185592680 @default.
• W1998450521 hasConceptScore W1998450521C2776119469 @default.
• W1998450521 hasConceptScore W1998450521C2777796741 @default.
• W1998450521 hasConceptScore W1998450521C2779303165 @default.
• W1998450521 hasConceptScore W1998450521C2779362680 @default.
• W1998450521 hasConceptScore W1998450521C71924100 @default.
• W1998450521 hasConceptScore W1998450521C83743174 @default.
• W1998450521 hasConceptScore W1998450521C86803240 @default.
• W1998450521 hasConceptScore W1998450521C98274493 @default.
• W1998450521 hasIssue "3" @default.
• W1998450521 hasLocation W19984505211 @default.
• W1998450521 hasLocation W19984505212 @default.
• W1998450521 hasLocation W19984505213 @default.

• next