Original title: Acyclic nucleoside bis-phosphonates as potent inhibitors of 6-oxopurine phosphoribosyltransferases
Authors: Špaček, Petr ; Keough, D. T. ; Vrbková, Silvie ; Slavětínská, Lenka ; Janeba, Zlatko ; Naesens, L. ; Edstein, M. D. ; Chavchich, M. ; Wang, T. H. ; de Jersey, J. ; Guddat, L. W. ; Hocková, Dana
Document type: Papers
Conference/Event: Symposium on Chemistry of Nucleic Acid Components /16./, Český Krumlov (CZ), 2014-06-08 / 2014-06-13
Year: 2014
Language: eng
Abstract: Hypoxanthine-guanin-(xanthine) phosphoribosyltransferase (HG(X)PRT) is critical for the survival of malarial parasites Plasmodium falciparum and Plasmodium vivax. These parasites rely on HG(X)PRT to make 6-oxopurine nucleoside monophosphates. Specific acyclic nucleoside phosphonates (ANPs) inhibit HG(X)PRT and thus have an anti-plasmodial activity. Crystal structures of human HGPRT in complex with several ANP-based inhibitors suggested that attachment of the second phosphonate group which could occupy the pyrophosphate binding site may lead to increased affinity of these compounds.
Keywords: enzyme inhibitors; nucleotide analogues; Plasmodium
Project no.: GAP207/11/0108 (CEP)
Funding provider: GA ČR
Host item entry: Chemistry of Nucleic Acid Components. 16th Symposium, ISBN 978-80-86241-50-0

Institution: Institute of Organic Chemistry and Biochemistry AS ČR (web)
Document availability information: Fulltext is available at the institute of the Academy of Sciences.
Original record: http://hdl.handle.net/11104/0234448

Permalink: http://www.nusl.cz/ntk/nusl-174776


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