A new family of covalent inhibitors block nucleotide binding to the active site of pyruvate kinase

Biochemical Journal

Volumn 448, Issue 1, 2012, Pages 67-72

  Morgan, Hugh P ^a   Walsh, Martin J ^b   Blackburn, Elizabeth A ^a   Wear, Martin A ^a   Boxer, Matthew B ^b   Shen, Min ^b   Veith, Henrike ^b   McNae, Iain W ^a   Nowicki, Matthew W ^a   Michels, Paul A M ^c   Auld, Douglas S ^b   Fothergill Gilmore, Linda A ^a   Walkinshaw, Malcolm D ^a  

^a UNIVERSITY OF EDINBURGH   (United Kingdom)

^b NATIONAL HUMAN GENOME RESEARCH INSTITUTE   (United States)

^c DE DUVE INSTITUTE   (Belgium)

Author keywords

Covalent inhibitor; Leishmania mexicana; Lysine covalent modification; Nucleotide binding; Pyruvate kinase; Saccharin analogue

Indexed keywords

4 [(1,1 DIOXO 1,2 BENZOTHIAZOL 3 YL)SULFANYL]BENZOIC ACID; ARGININE; ENZYME INHIBITOR; LYSINE; NUCLEOTIDE; PYRUVATE KINASE; SACCHARIN DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; COVALENT BOND; CRYSTAL STRUCTURE; ENZYME ACTIVE SITE; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; QUANTITATIVE ANALYSIS;

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; ANIMALS; ARGININE; BENZOATES; CATALYTIC DOMAIN; CONSERVED SEQUENCE; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; ISOENZYMES; LEISHMANIA MEXICANA; LYSINE; MODELS, MOLECULAR; PROTEIN BINDING; PROTEIN CONFORMATION; PYRUVATE KINASE; RECOMBINANT PROTEINS; SACCHARIN; SPECIES SPECIFICITY; STRUCTURE-ACTIVITY RELATIONSHIP; SURAMIN;

EID: 84867806188     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20121014     Document Type: Article

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