Development of high-throughput TR-FRET and AlphaScreen® assays for identification of potent inhibitors of PDK1

Journal of Biomolecular Screening

Volumn 14, Issue 10, 2009, Pages 1257-1262

  Xu, Zangwei ^a   Nagashima, Kumiko ^a   Sun, Dongyu ^a   Rush, Thomas ^a   Northrup, Alan ^a   Andersen, Jannik N ^a   Kariv, Ilona ^a   Bobkova, Ekaterina V ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

AlphaScreen ; Focused screen; PDK1; Tetracyclic kinase inhibitor; TR FRET

Indexed keywords

ANTINEOPLASTIC AGENT; AZAINDOLE DERIVATIVE; BX 795; INDAZOLE DERIVATIVE; INDENYLPYRAZOLE DERIVATIVE; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1 INHIBITOR; PROTEIN KINASE B; S6 KINASE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BIOTINYLATION; CANCER CELL; CONTROLLED STUDY; DRUG SCREENING; ENZYMATIC ASSAY; ENZYME ACTIVITY; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMAN; HUMAN CELL; IC 50; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; BIOTINYLATION; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; KINETICS; PEPTIDES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PROTO-ONCOGENE PROTEINS C-AKT; REPRODUCIBILITY OF RESULTS; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TIME FACTORS;

EID: 70349963770     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057109349356     Document Type: Article

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