Matches in SemOpenAlex for { <https://semopenalex.org/work/W2038007589> ?p ?o ?g. }
- W2038007589 endingPage "2526" @default.
- W2038007589 startingPage "2513" @default.
- W2038007589 abstract "Acyclic nucleoside phosphonates (ANPs) that contain a 6-oxopurine base are good inhibitors of the Plasmodium falciparum (Pf) and Plasmodium vivax (Pv) 6-oxopurine phosphoribosyltransferases (PRTs). Chemical modifications based on the crystal structure of 2-(phosphonoethoxy)ethylguanine (PEEG) in complex with human HGPRT have led to the design of new ANPs. These novel compounds contain a second phosphonate group attached to the ANP scaffold. {[(2-[(Guanine-9H-yl)methyl]propane-1,3-diyl)bis(oxy)]bis(methylene)}diphosphonic acid (compound 17) exhibited a Ki value of 30 nM for human HGPRT and 70 nM for Pf HGXPRT. The crystal structure of this compound in complex with human HGPRT shows that it fills or partially fills three critical locations in the active site: the binding sites of the purine base, the 5′-phosphate group, and pyrophosphate. This is the first HG(X)PRT inhibitor that has been able to achieve this result. Prodrugs have been synthesized resulting in IC50 values as low as 3.8 μM for Pf grown in cell culture, up to 25-fold lower compared to the parent compounds." @default.
- W2038007589 created "2016-06-24" @default.
- W2038007589 creator A5026188443 @default.
- W2038007589 creator A5032132180 @default.
- W2038007589 creator A5033601129 @default.
- W2038007589 creator A5040952323 @default.
- W2038007589 creator A5045287501 @default.
- W2038007589 creator A5045317036 @default.
- W2038007589 creator A5072438230 @default.
- W2038007589 creator A5072638559 @default.
- W2038007589 creator A5075935485 @default.
- W2038007589 creator A5079853523 @default.
- W2038007589 creator A5079877032 @default.
- W2038007589 creator A5081640914 @default.
- W2038007589 creator A5084003680 @default.
- W2038007589 date "2013-03-19" @default.
- W2038007589 modified "2023-09-30" @default.
- W2038007589 title "Acyclic Nucleoside Phosphonates Containing a Second Phosphonate Group Are Potent Inhibitors of 6-Oxopurine Phosphoribosyltransferases and Have Antimalarial Activity" @default.
- W2038007589 cites W1506669191 @default.
- W2038007589 cites W1969503178 @default.
- W2038007589 cites W1974210041 @default.
- W2038007589 cites W1979606430 @default.
- W2038007589 cites W1982471331 @default.
- W2038007589 cites W1990392794 @default.
- W2038007589 cites W1994659943 @default.
- W2038007589 cites W1996545576 @default.
- W2038007589 cites W2004854565 @default.
- W2038007589 cites W2005940694 @default.
- W2038007589 cites W2015005155 @default.
- W2038007589 cites W2016175830 @default.
- W2038007589 cites W2020251171 @default.
- W2038007589 cites W2031573500 @default.
- W2038007589 cites W2037183326 @default.
- W2038007589 cites W2051692507 @default.
- W2038007589 cites W2057789922 @default.
- W2038007589 cites W2062597360 @default.
- W2038007589 cites W2065220877 @default.
- W2038007589 cites W2067428749 @default.
- W2038007589 cites W2072369647 @default.
- W2038007589 cites W2072621169 @default.
- W2038007589 cites W2075053778 @default.
- W2038007589 cites W2080287563 @default.
- W2038007589 cites W2081595602 @default.
- W2038007589 cites W2086943438 @default.
- W2038007589 cites W2088191303 @default.
- W2038007589 cites W2092079765 @default.
- W2038007589 cites W2105668259 @default.
- W2038007589 cites W2111163381 @default.
- W2038007589 cites W2114367386 @default.
- W2038007589 cites W2116697852 @default.
- W2038007589 cites W2124026197 @default.
- W2038007589 cites W2146992057 @default.
- W2038007589 cites W2151383900 @default.
- W2038007589 cites W2153380936 @default.
- W2038007589 cites W2158452526 @default.
- W2038007589 cites W2163341755 @default.
- W2038007589 cites W2180229411 @default.
- W2038007589 cites W233628489 @default.
- W2038007589 cites W2949819425 @default.
- W2038007589 cites W2952441129 @default.
- W2038007589 cites W2953388699 @default.
- W2038007589 cites W4248872320 @default.
- W2038007589 doi "https://doi.org/10.1021/jm301893b" @default.
- W2038007589 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23448281" @default.
- W2038007589 hasPublicationYear "2013" @default.
- W2038007589 type Work @default.
- W2038007589 sameAs 2038007589 @default.
- W2038007589 citedByCount "57" @default.
- W2038007589 countsByYear W20380075892013 @default.
- W2038007589 countsByYear W20380075892014 @default.
- W2038007589 countsByYear W20380075892015 @default.
- W2038007589 countsByYear W20380075892016 @default.
- W2038007589 countsByYear W20380075892017 @default.
- W2038007589 countsByYear W20380075892018 @default.
- W2038007589 countsByYear W20380075892019 @default.
- W2038007589 countsByYear W20380075892020 @default.
- W2038007589 countsByYear W20380075892021 @default.
- W2038007589 countsByYear W20380075892022 @default.
- W2038007589 countsByYear W20380075892023 @default.
- W2038007589 crossrefType "journal-article" @default.
- W2038007589 hasAuthorship W2038007589A5026188443 @default.
- W2038007589 hasAuthorship W2038007589A5032132180 @default.
- W2038007589 hasAuthorship W2038007589A5033601129 @default.
- W2038007589 hasAuthorship W2038007589A5040952323 @default.
- W2038007589 hasAuthorship W2038007589A5045287501 @default.
- W2038007589 hasAuthorship W2038007589A5045317036 @default.
- W2038007589 hasAuthorship W2038007589A5072438230 @default.
- W2038007589 hasAuthorship W2038007589A5072638559 @default.
- W2038007589 hasAuthorship W2038007589A5075935485 @default.
- W2038007589 hasAuthorship W2038007589A5079853523 @default.
- W2038007589 hasAuthorship W2038007589A5079877032 @default.
- W2038007589 hasAuthorship W2038007589A5081640914 @default.
- W2038007589 hasAuthorship W2038007589A5084003680 @default.
- W2038007589 hasConcept C104317684 @default.
- W2038007589 hasConcept C155647269 @default.
- W2038007589 hasConcept C181199279 @default.
- W2038007589 hasConcept C185592680 @default.
- W2038007589 hasConcept C2776543447 @default.