Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism

Biochemistry

Volumn 50, Issue 5, 2011, Pages 738-751

  Iwata, Hidehisa ^a   Imamura, Shinichi ^a   Hori, Akira ^a   Hixon, Mark S ^b   Kimura, Hiroyuki ^a   Miki, Hiroshi ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b Takeda San Diego Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BINDING MECHANISMS; BIOCHEMICAL CHARACTERIZATION; COMPETITIVE INHIBITION; DISSOCIATION RATE CONSTANT; FLUORESCENT TRACERS; IN-VIVO; LIGAND DISPLACEMENT; LIPID KINASE; PHARMACOKINETIC PROFILES; PLATELET-DERIVED GROWTH FACTOR RECEPTORS; PRE-INCUBATION; PROTEIN KINASE; PYRIDAZINE; RESIDENCE TIME; SOLID TUMORS; TIME-DEPENDENT; TUMOR ANGIOGENESIS; TYPE II KINASE INHIBITOR; TYROSINE KINASE; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR; VEGFR-2;

AMINO ACIDS; DISSOCIATION; LIGANDS; OXYGEN; PEPTIDES; RATE CONSTANTS; TUMORS;

ENZYMES;

ADENOSINE TRIPHOSPHATE; AXITINIB; IMIDAZO[1,2 B]PYRIDAZINE DERIVATIVE; PAZOPANIB; PLATELET DERIVED GROWTH FACTOR BETA RECEPTOR; PLATELET DERIVED GROWTH FACTOR RECEPTOR; PROTEIN TYROSINE KINASE INHIBITOR; SORAFENIB; SUNITINIB; TAK 593; UNCLASSIFIED DRUG; VASCULOTROPIN RECEPTOR; VASCULOTROPIN RECEPTOR 2;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING AFFINITY; BINDING KINETICS; COMPETITIVE INHIBITION; CONTROLLED STUDY; DISSOCIATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; ENZYME ASSAY; ENZYME BINDING; ENZYME INHIBITION; ENZYME SPECIFICITY; HUMAN; IC 50; PRIORITY JOURNAL; TUMOR VASCULARIZATION;

AZABICYCLO COMPOUNDS; HUMANS; KINETICS; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PYRAZOLES; RECEPTORS, PLATELET-DERIVED GROWTH FACTOR; RECEPTORS, VASCULAR ENDOTHELIAL GROWTH FACTOR;

EID: 79952096135     PISSN: 00062960     EISSN: 15204995     Source Type: Journal    
DOI: 10.1021/bi101777f     Document Type: Article

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