Direct small-molecule kinase activation: Novel approaches for a new era of drug discovery

Current Opinion in Drug Discovery and Development

Volumn 12, Issue 5, 2009, Pages 585-596

  Simpson, Graham L ^a   Hughes, Jennifer A ^a   Washio, Yoshiaki ^a   Bertrand, Sophie M ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Activation; Drug discovery; Kinase; Medicinal chemistry; Molecular biology; Novel target; Protein protein interaction; Screening; Small molecule activator; Upregulation

Indexed keywords

2 CYCLOHEXYL 1 (4 METHANESULFONYLPHENYL)CYCLOPROPANECARBOXYLIC ACID 2 THIAZOLYLAMIDE; 5 AMINO 4 IMIDAZOLECARBOXAMIDE RIBOSIDE; A 769662; ANACARDIC ACID; ANTINEOPLASTIC AGENT; AURORA A KINASE; AURORA B KINASE; AURORA C KINASE; BISTRATENE A; BRYOSTATIN 1; DIACYLGLYCEROL; ENZYME ACTIVATOR; GKA 50; GLUCOKINASE; GLUCOSE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE KINASE; INDOLACTAM V; INGENOL 3 ANGELATE; INSULIN RECEPTOR; METFORMIN; NORASTERRIQUINONE B1; OCTAPEPTIDE; PEP 005; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1; PHOSPHOTRANSFERASE; PROTEIN KINASE C; PROTEIN TYROSINE KINASE; PT 1; RO 28 1675; TLK 19781; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; BINDING SITE; CLINICAL TRIAL; DIABETES MELLITUS; DRUG DEVELOPMENT; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG TARGETING; ENZYME ACTIVATION; HUMAN; INSULIN RESISTANCE; ISCHEMIA; NONHUMAN; OBESITY; REVIEW;

ALLOSTERIC REGULATION; ANIMALS; DRUG DESIGN; DRUG DISCOVERY; ENZYME ACTIVATION; ENZYME ACTIVATORS; GLUCOKINASE; HUMANS; MOLECULAR STRUCTURE; PHOSPHORYLATION; PROTEIN CONFORMATION; PROTEIN KINASE C; PROTEIN KINASES; PROTEIN-SERINE-THREONINE KINASES; RECEPTOR, INSULIN; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 70149122987     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

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