Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening

Journal of Biological Chemistry

Volumn 285, Issue 24, 2010, Pages 18838-18846

  Bobkova, Ekaterina V ^a   Weber, Michael J ^a   Xu, Zangwei ^a   Zhang, Yan Ling ^a   Jung, Joon ^a   Blume Jensen, Peter ^a   Northrup, Alan ^a   Kunapuli, Priya ^a   Andersen, Jannik N ^a   Kariv, Ilona ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION LOOPS; ANGIOGENESIS; ATP-BINDING; BIOPHYSICAL STUDIES; CANCER CELL GROWTH; CATALYTIC MECHANISMS; COMPUTATIONAL ANALYSIS; DOSE-RESPONSE STUDY; FOCAL POINTS; FUSION PEPTIDES; HYDROPHOBIC MOTIFS; KINASE DOMAINS; KINASE INHIBITORS; KINASE SUBSTRATES; LIGAND-BINDING SITES; MECHANISM OF ACTION; N-TERMINALS; PEPTIDE SUBSTRATES; PHOSPHOINOSITIDE 3-KINASE; PHOSPHOINOSITIDES; PROTEIN KINASE; RAPID EQUILIBRIUM; SCREENING ASSAYS; SIGNALING PATHWAYS; SUBSTRATE RECOGNITION; THERMAL SHIFT; THROUGHPUT SCREENING; TR-FRET;

ASSAYS; BINDING ENERGY; BINDING SITES; BIOCHEMISTRY; CHEMICAL ACTIVATION; GROWTH KINETICS; HYDROPHOBICITY; LIGANDS; PEPTIDES; SCAFFOLDS; THROUGHPUT;

SUBSTRATES;

ADENOSINE TRIPHOSPHATE; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1 INHIBITOR; PROTEIN KINASE B; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CATALYSIS; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SELECTIVITY; DRUG SPECIFICITY; DRUG STRUCTURE; ENZYME KINETICS; ENZYME SUBSTRATE; HIGH THROUGHPUT SCREENING; IC 50; MOLECULAR MODEL; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; AMINO ACID MOTIFS; ANIMALS; BINDING SITES; BIOPHYSICS; DRUG DESIGN; ENZYME INHIBITORS; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMANS; KINETICS; MODELS, MOLECULAR; PEPTIDES; PROTEIN BINDING; PROTEIN-SERINE-THREONINE KINASES; SIGNAL TRANSDUCTION;

EID: 77953305214     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M109.089946     Document Type: Article

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