About: Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics

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About: Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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. (en)
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 (en)
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 (en)
skos:notation	RIV/61388963:_____/09:00329059!RIV10-MSM-61388963
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(1M0508), P(1QS400550501), Z(AV0Z40550506)
http://linked.open...iv/cisloPeriodika	14
http://linked.open...vai/riv/dodaniDat	2010
http://linked.open...aciTvurceVysledku	Hocková, Dana Holý, Antonín
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav organické chemie a biochemie AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	319546
http://linked.open...ai/riv/idVysledku	RIV/61388963:_____/09:00329059
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acyclic nucleoside phosphonates; phosphoribosyltransferase; enzyme inhibitors; Plasmodium falciparum (en)
http://linked.open.../riv/klicoveSlovo	Plasmodium falciparum acyclic nucleoside phosphonates phosphoribosyltransferase enzyme inhibitors
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[0A920C90D4EA]
http://linked.open...i/riv/nazevZdroje	Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...vavai/riv/projekt	New Antivirals and Antineoplastics Novel antivirals and antineoplastics
http://linked.open...UplatneniVysledku	2009
http://linked.open...v/svazekPeriodika	52
http://linked.open...iv/tvurceVysledku	Holý, Antonín Hocková, Dana Guddat, L. W. Keough, D. T. Naesens, L. de Jersey, J. Skinner-Adams, T. S.
http://linked.open...ain/vavai/riv/wos	000268139900034
http://linked.open...n/vavai/riv/zamer	Regulace biologických procesů: Chemické modulátory vybraných systémů významných pro medicínu a zemědělství
issn	0022-2623
number of pages	9 (xsd:int)

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