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Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics
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SYSNO ASEP 0329059 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics Author(s) Keough, D. T. (AU)
Hocková, Dana (UOCHB-X) RID, ORCID
Holý, Antonín (UOCHB-X)
Naesens, L. (BE)
Skinner-Adams, T. S. (AU)
de Jersey, J. (AU)
Guddat, L. W. (AU)Number of authors 7 Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 52, č. 14 (2009), s. 4391-4399Number of pages 9 s. Language eng - English Country US - United States Keywords acyclic nucleoside phosphonates ; phosphoribosyltransferase ; enzyme inhibitors ; Plasmodium falciparum Subject RIV CC - Organic Chemistry R&D Projects 1M0508 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) 1QS400550501 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR) CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000268139900034 DOI 10.1021/jm900267n Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2010
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