Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(Trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid

Biochemistry

Volumn 42, Issue 20, 2003, Pages 6043-6056

  Zhang, Yan ^a   Desharnais, Joel ^a   Marsilje, Thomas H ^a   Li, Chenglong ^a   Hedrick, Michael P ^a   Gooljarsingh, Lata T ^b   Tavassoli, Ali ^b   Benkovic, Stephen J ^b   Olson, Arthur J ^a   Boger, Dale L ^a   Wilson, Ian A ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b PENNSYLVANIA STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBOXYLIC ACIDS; CELLS; CRYSTAL STRUCTURE; SYNTHESIS (CHEMICAL); TUMORS;

SELECTIVE INHIBITORS;

ENZYME INHIBITION;

10 (TRIFLUOROACETYL) 5,10 DIDEAZAACYCLIC 5,6,7,8 TETRAHYDROFOLIC ACID; 10 FORMYLTETRAHYDROFOLIC ACID; FOLIC ACID DERIVATIVE; LOMETREXOL; PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE; PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE INHIBITOR; TETRAHYDROFOLIC ACID DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CANCER CELL CULTURE; CANCER INHIBITION; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; DRUG BINDING; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TRANSPORT; ESCHERICHIA COLI; HUMAN; HUMAN CELL; MOLECULAR INTERACTION; NONHUMAN; PRIORITY JOURNAL;

BINDING SITES; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ELECTROSTATICS; ENZYME INHIBITORS; ESCHERICHIA COLI; HUMANS; HYDROXYMETHYL AND FORMYL TRANSFERASES; KINETICS; MACROMOLECULAR SUBSTANCES; MODELS, MOLECULAR; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE; PROTEIN CONFORMATION; RECOMBINANT PROTEINS; TETRAHYDROFOLATES;

ESCHERICHIA COLI;

EID: 0037846072     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi034219c     Document Type: Article

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