A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo

Journal of Biological Chemistry

Volumn 280, Issue 10, 2005, Pages 9160-9169

  Olivero, Alan G ^a   Eigenbrot, Charles ^a   Goldsmith, Richard ^a   Robarge, Kirk ^a   Artis, Dean R ^a,d   Flygare, John ^a   Rawson, Thomas ^a   Sutherlin, Daniel P ^a   Kadkhodayan, Saloumeh ^a   Beresini, Maureen ^a   Elliott, Linda O ^a   DeGuzman, Geralyn G ^a   Banner, David W ^b   Ultsch, Mark ^a   Marzec, Ulla ^c,e   Hanson, Stephen R ^c,e   Refino, Canio ^a   Bunting, Stuart ^a   Kirchhofer, Daniel ^a  

^a GENENTECH INC   (United States)

^b F HOFFMANN LA ROCHE LTD   (Switzerland)

^c EMORY UNIVERSITY   (United States)

^d PLEXXIKON INC   (United States)

^e OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ASSAYS; CARDIOVASCULAR SYSTEM; COAGULATION; CRYSTAL STRUCTURE; GROWTH KINETICS; PROTEINS; TISSUE;

RECOGNITION PACKET; SERINE PROTEASES; THROMBOSIS-RELATED DISORDER; TISSUE FACTOR (TF);

ENZYME INHIBITION;

4 AMINOBENZAMIDINE; BLOOD CLOTTING FACTOR 7A; BLOOD CLOTTING FACTOR 7A INHIBITOR; G 17905; GLUTAMINE; GLYCINE; SERINE PROTEINASE; THROMBOPLASTIN; TRYPTASE; UNCLASSIFIED DRUG; 4 (2 (3 AMINOBENZENESULFONYLAMINO) 1 (3,5 DIETHOXY 2 FLUOROPHENYL) 2 OXOETHYLAMINO) 2 HYDROXYBENZAMIDINE; 4-(2-(3-AMINOBENZENESULFONYLAMINO)-1-(3,5-DIETHOXY-2-FLUOROPHENYL)-2-OXOETHYLAMINO)-2-HYDROXYBENZAMIDINE; BENZAMIDINE DERIVATIVE; SULFONAMIDE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTERIOVENOUS SHUNT; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG INHIBITION; FIBRIN DEPOSITION; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; THROMBOGENESIS; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; HUMAN; HYDROGEN BOND; KINETICS; METABOLISM; PROTEIN CONFORMATION; THROMBOSIS; X RAY CRYSTALLOGRAPHY;

ANIMALIA; PAPIO HAMADRYAS; THROMBUS;

BENZAMIDINES; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; FACTOR VIIA; HUMANS; HYDROGEN BONDING; KINETICS; MODELS, MOLECULAR; PROTEIN BINDING; PROTEIN CONFORMATION; SULFONAMIDES; THROMBOSIS;

EID: 20144389170     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M409068200     Document Type: Article

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