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A Pantetheinase-Resistant Pantothenamide with Potent, On Target, and Selective Antiplasmodial Activity

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dc.contributor.authorMacuamule, Cristiano
dc.contributor.authorTjhin, Erick
dc.contributor.authorJana, Collins E.
dc.contributor.authorBarnard, Leanne
dc.contributor.authorKoekemoer, Lizbe
dc.contributor.authorde Villiers, Marianne
dc.contributor.authorSaliba, Kevin
dc.contributor.authorStrauss, Erick
dc.date.accessioned2015-12-08T22:17:56Z
dc.date.issued2015
dc.date.updated2015-12-08T08:11:27Z
dc.description.abstractPantothenamides inhibit blood-stage Plasmodium falciparum with potencies (50% inhibitory concentration [IC50], 20 nM) similar to that of chloroquine. They target processes dependent on pantothenate, a precursor of the essential metabolic cofactor coenzyme A. However, their antiplasmodial activity is reduced due to degradation by serum pantetheinase. Minor modification of the pantothenamide structure led to the identification of -methyl-N-phenethyl-pantothenamide, a pantothenamide resistant to degradation, with excellent antiplasmodial activity (IC50, 52 6 nM), target specificity, and low toxicity. O
dc.identifier.issn0066-4804
dc.identifier.urihttp://hdl.handle.net/1885/31116
dc.publisherAmerican Society for Microbiology
dc.rightsAuthor/s retain copyrighten_AU
dc.sourceAntimicrobial Agents and Chemotherapy
dc.titleA Pantetheinase-Resistant Pantothenamide with Potent, On Target, and Selective Antiplasmodial Activity
dc.typeJournal article
dcterms.accessRightsOpen Accessen_AU
local.bibliographicCitation.issue6
local.bibliographicCitation.lastpage3668
local.bibliographicCitation.startpage3666
local.contributor.affiliationMacuamule, Cristiano, Stellenbosch University
local.contributor.affiliationTjhin, Erick, College of Medicine, Biology and Environment, ANU
local.contributor.affiliationJana, Collins E., Stellenbosch University
local.contributor.affiliationBarnard, Leanne, Stellenbosch University
local.contributor.affiliationKoekemoer, Lizbe, Stellenbosch University
local.contributor.affiliationde Villiers, Marianne, Stellenbosch University
local.contributor.affiliationSaliba, Kevin, College of Medicine, Biology and Environment, ANU
local.contributor.affiliationStrauss, Erick, University of Stellenbosch
local.contributor.authoruidTjhin, Erick, u4485090
local.contributor.authoruidSaliba, Kevin, u9707744
local.description.notesImported from ARIES
local.identifier.absfor060502 - Infectious Agents
local.identifier.absfor111501 - Basic Pharmacology
local.identifier.absfor110803 - Medical Parasitology
local.identifier.absseo920109 - Infectious Diseases
local.identifier.ariespublicationu4008405xPUB80
local.identifier.citationvolume59
local.identifier.doi10.1128/AAC.04970-14
local.identifier.scopusID2-s2.0-84929629237
local.type.statusPublished Version

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