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Statements

Subject Item
n2:RIV%2F61388963%3A_____%2F09%3A00329059%21RIV10-MSM-61388963
rdf:type
skos:Concept n13:Vysledek
dcterms:description
Plasmodium falciparum (Pf) relies on the purine salvage enzyme, hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT), for the synthesis of the mononucleotides. Acyclic nucleoside phosphonates (ANPs) are structural analogs of the mononucleotide product of the reaction and contain a purine base linked by different combinations of atoms to a phosphonate group. Ki values for 19 ANPs were determined for PfHGXPRT and human HGPRT. IC50 values for Pf grown in cell culture and the structures of human HGPRT in complex with three ANPs have been determined. These results provide a basis for the design of more potent and selective inhibitors as anti-malarial drugs with novel mode of action. Plasmodium falciparum (Pf) relies on the purine salvage enzyme, hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT), for the synthesis of the mononucleotides. Acyclic nucleoside phosphonates (ANPs) are structural analogs of the mononucleotide product of the reaction and contain a purine base linked by different combinations of atoms to a phosphonate group. Ki values for 19 ANPs were determined for PfHGXPRT and human HGPRT. IC50 values for Pf grown in cell culture and the structures of human HGPRT in complex with three ANPs have been determined. These results provide a basis for the design of more potent and selective inhibitors as anti-malarial drugs with novel mode of action.
dcterms:title
Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics
skos:prefLabel
Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics
skos:notation
RIV/61388963:_____/09:00329059!RIV10-MSM-61388963
n3:aktivita
n12:P n12:Z
n3:aktivity
P(1M0508), P(1QS400550501), Z(AV0Z40550506)
n3:cisloPeriodika
14
n3:dodaniDat
n9:2010
n3:domaciTvurceVysledku
n18:9345655 n18:9587217
n3:druhVysledku
n10:J
n3:duvernostUdaju
n16:S
n3:entitaPredkladatele
n6:predkladatel
n3:idSjednocenehoVysledku
319546
n3:idVysledku
RIV/61388963:_____/09:00329059
n3:jazykVysledku
n5:eng
n3:klicovaSlova
acyclic nucleoside phosphonates; phosphoribosyltransferase; enzyme inhibitors; Plasmodium falciparum
n3:klicoveSlovo
n11:Plasmodium%20falciparum n11:acyclic%20nucleoside%20phosphonates n11:enzyme%20inhibitors n11:phosphoribosyltransferase
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[0A920C90D4EA]
n3:nazevZdroje
Journal of Medicinal Chemistry
n3:obor
n15:CC
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
7
n3:projekt
n8:1QS400550501 n8:1M0508
n3:rokUplatneniVysledku
n9:2009
n3:svazekPeriodika
52
n3:tvurceVysledku
Hocková, Dana Skinner-Adams, T. S. Holý, Antonín Naesens, L. de Jersey, J. Guddat, L. W. Keough, D. T.
n3:wos
000268139900034
n3:zamer
n14:AV0Z40550506
s:issn
0022-2623
s:numberOfPages
9