FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2800698897> ?p ?o ?g. }

• W2800698897 endingPage "769" @default.
• W2800698897 startingPage "760" @default.
• W2800698897 abstract "Current mandated preclinical tests for drug-induced proarrhythmia are very sensitive, but not sufficiently specific. This has led to concern that there is a high attrition rate of potentially safe drugs that could have been beneficial to patients. The comprehensive in vitro proarrhythmia initiative has proposed new metrics based around in silico risk predictions, which are informed, among other things, by measures of human ether-à-go-go-related gene channel (hERG) block kinetics. However, high-throughput patch-clamp systems set to collect these data largely operate at ambient temperature, whereas the simulations for risk prediction are carried out at physiologic temperature. The aims of this study were to: 1) determine to what degree kinetics of drug block of hERG are temperature-dependent, 2) assess the impact of any temperature dependence of drug binding kinetics on repolarization in silico, and 3) identify whether a common set of Q₁₀ scalars can be used to extrapolate kinetic data gathered at ambient to physiologic temperatures for use in in silico proarrhythmic risk prediction. We show that, for a range of drugs, kinetics of block are temperature-dependent and, furthermore, that the degree of temperature dependence is different for each drug. As a result, no common set of Q₁₀ scalars could describe the observed range of temperature dependencies. These results suggest that if accurate physiologic temperature models of the kinetics of drug binding are important for in silico risk prediction, the in vitro data should be acquired at physiologic temperature." @default.
• W2800698897 created "2018-05-17" @default.
• W2800698897 creator A5035538956 @default.
• W2800698897 creator A5044267250 @default.
• W2800698897 creator A5048222625 @default.
• W2800698897 creator A5060826983 @default.
• W2800698897 date "2018-05-04" @default.
• W2800698897 modified "2023-09-27" @default.
• W2800698897 title "The Temperature Dependence of Kinetics Associated with Drug Block of hERG Channels Is Compound-Specific and an Important Factor for Proarrhythmic Risk Prediction" @default.
• W2800698897 cites W1563915010 @default.
• W2800698897 cites W1976584289 @default.
• W2800698897 cites W1991902077 @default.
• W2800698897 cites W1993689835 @default.
• W2800698897 cites W2011345948 @default.
• W2800698897 cites W2014912931 @default.
• W2800698897 cites W2018889879 @default.
• W2800698897 cites W2025697869 @default.
• W2800698897 cites W2049520769 @default.
• W2800698897 cites W2074527519 @default.
• W2800698897 cites W2099302673 @default.
• W2800698897 cites W2099532852 @default.
• W2800698897 cites W2107763854 @default.
• W2800698897 cites W2113927644 @default.
• W2800698897 cites W2115765852 @default.
• W2800698897 cites W2116581628 @default.
• W2800698897 cites W2120377742 @default.
• W2800698897 cites W2131700500 @default.
• W2800698897 cites W2150629896 @default.
• W2800698897 cites W2150947558 @default.
• W2800698897 cites W2268304733 @default.
• W2800698897 cites W2328454508 @default.
• W2800698897 cites W2367742786 @default.
• W2800698897 cites W2377416452 @default.
• W2800698897 cites W2415670168 @default.
• W2800698897 cites W2586121714 @default.
• W2800698897 cites W2588081908 @default.
• W2800698897 cites W2747733237 @default.
• W2800698897 cites W4236987721 @default.
• W2800698897 cites W878990122 @default.
• W2800698897 doi "https://doi.org/10.1124/mol.117.111534" @default.
• W2800698897 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29728448" @default.
• W2800698897 hasPublicationYear "2018" @default.
• W2800698897 type Work @default.
• W2800698897 sameAs 2800698897 @default.
• W2800698897 citedByCount "24" @default.
• W2800698897 countsByYear W28006988972018 @default.
• W2800698897 countsByYear W28006988972019 @default.
• W2800698897 countsByYear W28006988972020 @default.
• W2800698897 countsByYear W28006988972021 @default.
• W2800698897 countsByYear W28006988972022 @default.
• W2800698897 countsByYear W28006988972023 @default.
• W2800698897 crossrefType "journal-article" @default.
• W2800698897 hasAuthorship W2800698897A5035538956 @default.
• W2800698897 hasAuthorship W2800698897A5044267250 @default.
• W2800698897 hasAuthorship W2800698897A5048222625 @default.
• W2800698897 hasAuthorship W2800698897A5060826983 @default.
• W2800698897 hasBestOaLocation W28006988971 @default.
• W2800698897 hasConcept C104317684 @default.
• W2800698897 hasConcept C121332964 @default.
• W2800698897 hasConcept C12554922 @default.
• W2800698897 hasConcept C126322002 @default.
• W2800698897 hasConcept C146403970 @default.
• W2800698897 hasConcept C148898269 @default.
• W2800698897 hasConcept C185263204 @default.
• W2800698897 hasConcept C185592680 @default.
• W2800698897 hasConcept C2775905019 @default.
• W2800698897 hasConcept C2777008848 @default.
• W2800698897 hasConcept C2779362680 @default.
• W2800698897 hasConcept C2780035454 @default.
• W2800698897 hasConcept C55493867 @default.
• W2800698897 hasConcept C62520636 @default.
• W2800698897 hasConcept C71924100 @default.
• W2800698897 hasConcept C83743174 @default.
• W2800698897 hasConcept C86803240 @default.
• W2800698897 hasConcept C98274493 @default.
• W2800698897 hasConceptScore W2800698897C104317684 @default.
• W2800698897 hasConceptScore W2800698897C121332964 @default.
• W2800698897 hasConceptScore W2800698897C12554922 @default.
• W2800698897 hasConceptScore W2800698897C126322002 @default.
• W2800698897 hasConceptScore W2800698897C146403970 @default.
• W2800698897 hasConceptScore W2800698897C148898269 @default.
• W2800698897 hasConceptScore W2800698897C185263204 @default.
• W2800698897 hasConceptScore W2800698897C185592680 @default.
• W2800698897 hasConceptScore W2800698897C2775905019 @default.
• W2800698897 hasConceptScore W2800698897C2777008848 @default.
• W2800698897 hasConceptScore W2800698897C2779362680 @default.
• W2800698897 hasConceptScore W2800698897C2780035454 @default.
• W2800698897 hasConceptScore W2800698897C55493867 @default.
• W2800698897 hasConceptScore W2800698897C62520636 @default.
• W2800698897 hasConceptScore W2800698897C71924100 @default.
• W2800698897 hasConceptScore W2800698897C83743174 @default.
• W2800698897 hasConceptScore W2800698897C86803240 @default.
• W2800698897 hasConceptScore W2800698897C98274493 @default.
• W2800698897 hasIssue "1" @default.
• W2800698897 hasLocation W28006988971 @default.
• W2800698897 hasLocation W28006988972 @default.
• W2800698897 hasOpenAccess W2800698897 @default.
• W2800698897 hasPrimaryLocation W28006988971 @default.

• next