FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2069394025> ?p ?o ?g. }

• W2069394025 endingPage "2303" @default.
• W2069394025 startingPage "2295" @default.
• W2069394025 abstract "ABSTRACT Dronedarone and amiodarone are cationic lipophilic benzofurans used to treat cardiac arrhythmias. They also have activity against the parasitic protozoan Trypanosoma cruzi , the causative agent of Chagas' disease. They function by disrupting intracellular Ca 2+ homeostasis of the parasite and by inhibiting membrane sterol (ergosterol) biosynthesis. Amiodarone also has activity against Leishmania mexicana , suggesting that dronedarone might likewise be active against this organism. This might be of therapeutic interest, since dronedarone is thought to have fewer side effects in humans than does amiodarone. We show here that dronedarone effectively inhibits the growth of L. mexicana promastigotes in culture and, more importantly, has excellent activity against amastigotes inside infected macrophages (the clinically relevant form) without affecting the host cell, with the 50% inhibitory concentrations against amastigotes being 3 orders of magnitude lower than those obtained previously with T. cruzi amastigotes (0.65 nM versus 0.75 μM). As with amiodarone, dronedarone affects intracellular Ca 2+ homeostasis in the parasite, inducing an elevation of intracellular Ca 2+ levels. This is achieved by rapidly collapsing the mitochondrial membrane potential and inducing an alkalinization of acidocalcisomes at a rate that is faster than that observed with amiodarone. We also show that dronedarone inhibits parasite oxidosqualene cyclase, a key enzyme in ergosterol biosynthesis known to be vital for survival. Overall, our results suggest the possibility of repurposing dronedarone as a treatment for cutaneous, and perhaps other, leishmaniases." @default.
• W2069394025 created "2016-06-24" @default.
• W2069394025 creator A5001560186 @default.
• W2069394025 creator A5009311148 @default.
• W2069394025 creator A5013527064 @default.
• W2069394025 creator A5025498016 @default.
• W2069394025 creator A5026924669 @default.
• W2069394025 creator A5029686118 @default.
• W2069394025 creator A5030721294 @default.
• W2069394025 creator A5051545514 @default.
• W2069394025 creator A5074609647 @default.
• W2069394025 creator A5080397665 @default.
• W2069394025 creator A5091224802 @default.
• W2069394025 date "2014-04-01" @default.
• W2069394025 modified "2023-10-18" @default.
• W2069394025 title "Dronedarone, an Amiodarone Analog with Improved Anti-Leishmania mexicana Efficacy" @default.
• W2069394025 cites W1833793080 @default.
• W2069394025 cites W1968217711 @default.
• W2069394025 cites W1985588649 @default.
• W2069394025 cites W1991674117 @default.
• W2069394025 cites W2021381859 @default.
• W2069394025 cites W2044500356 @default.
• W2069394025 cites W2046655254 @default.
• W2069394025 cites W2053190507 @default.
• W2069394025 cites W2060259273 @default.
• W2069394025 cites W2102328887 @default.
• W2069394025 cites W2102678982 @default.
• W2069394025 cites W2109261582 @default.
• W2069394025 cites W2125297875 @default.
• W2069394025 cites W2134581187 @default.
• W2069394025 cites W2141260882 @default.
• W2069394025 cites W2145146508 @default.
• W2069394025 cites W2147705199 @default.
• W2069394025 cites W2149404851 @default.
• W2069394025 cites W2161618149 @default.
• W2069394025 cites W2404924867 @default.
• W2069394025 cites W4251530540 @default.
• W2069394025 doi "https://doi.org/10.1128/aac.01240-13" @default.
• W2069394025 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4023776" @default.
• W2069394025 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24492373" @default.
• W2069394025 hasPublicationYear "2014" @default.
• W2069394025 type Work @default.
• W2069394025 sameAs 2069394025 @default.
• W2069394025 citedByCount "29" @default.
• W2069394025 countsByYear W20693940252014 @default.
• W2069394025 countsByYear W20693940252015 @default.
• W2069394025 countsByYear W20693940252016 @default.
• W2069394025 countsByYear W20693940252017 @default.
• W2069394025 countsByYear W20693940252018 @default.
• W2069394025 countsByYear W20693940252019 @default.
• W2069394025 countsByYear W20693940252020 @default.
• W2069394025 countsByYear W20693940252021 @default.
• W2069394025 countsByYear W20693940252022 @default.
• W2069394025 countsByYear W20693940252023 @default.
• W2069394025 crossrefType "journal-article" @default.
• W2069394025 hasAuthorship W2069394025A5001560186 @default.
• W2069394025 hasAuthorship W2069394025A5009311148 @default.
• W2069394025 hasAuthorship W2069394025A5013527064 @default.
• W2069394025 hasAuthorship W2069394025A5025498016 @default.
• W2069394025 hasAuthorship W2069394025A5026924669 @default.
• W2069394025 hasAuthorship W2069394025A5029686118 @default.
• W2069394025 hasAuthorship W2069394025A5030721294 @default.
• W2069394025 hasAuthorship W2069394025A5051545514 @default.
• W2069394025 hasAuthorship W2069394025A5074609647 @default.
• W2069394025 hasAuthorship W2069394025A5080397665 @default.
• W2069394025 hasAuthorship W2069394025A5091224802 @default.
• W2069394025 hasBestOaLocation W20693940251 @default.
• W2069394025 hasConcept C126322002 @default.
• W2069394025 hasConcept C136764020 @default.
• W2069394025 hasConcept C2777625466 @default.
• W2069394025 hasConcept C2778094803 @default.
• W2069394025 hasConcept C2779161974 @default.
• W2069394025 hasConcept C2779518148 @default.
• W2069394025 hasConcept C2781092759 @default.
• W2069394025 hasConcept C41008148 @default.
• W2069394025 hasConcept C55493867 @default.
• W2069394025 hasConcept C71924100 @default.
• W2069394025 hasConcept C71928629 @default.
• W2069394025 hasConcept C79879829 @default.
• W2069394025 hasConcept C86803240 @default.
• W2069394025 hasConcept C89423630 @default.
• W2069394025 hasConcept C98274493 @default.
• W2069394025 hasConcept C98319499 @default.
• W2069394025 hasConceptScore W2069394025C126322002 @default.
• W2069394025 hasConceptScore W2069394025C136764020 @default.
• W2069394025 hasConceptScore W2069394025C2777625466 @default.
• W2069394025 hasConceptScore W2069394025C2778094803 @default.
• W2069394025 hasConceptScore W2069394025C2779161974 @default.
• W2069394025 hasConceptScore W2069394025C2779518148 @default.
• W2069394025 hasConceptScore W2069394025C2781092759 @default.
• W2069394025 hasConceptScore W2069394025C41008148 @default.
• W2069394025 hasConceptScore W2069394025C55493867 @default.
• W2069394025 hasConceptScore W2069394025C71924100 @default.
• W2069394025 hasConceptScore W2069394025C71928629 @default.
• W2069394025 hasConceptScore W2069394025C79879829 @default.
• W2069394025 hasConceptScore W2069394025C86803240 @default.
• W2069394025 hasConceptScore W2069394025C89423630 @default.
• W2069394025 hasConceptScore W2069394025C98274493 @default.

• next