Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells

ACS Medicinal Chemistry Letters

Volumn 7, Issue 3, 2016, Pages 223-228

  Koehler, Michael F T ^a   Bergeron, Philippe ^a   Blackwood, Elizabeth M ^a   Bowman, Krista ^a   Clark, Kevin R ^a   Firestein, Ron ^a   Kiefer, James R ^a   Maskos, Klaus ^c   McCleland, Mark L ^a   Orren, Linda ^a   Salphati, Laurent ^a   Schmidt, Steve ^a   Schneider, Elisabeth V ^b,c   Wu, Jiansheng ^a   Beresini, Maureen H ^a  

^a GENENTECH INC   (United States)

^b PROTEROS BIOSTRUCTURES GMBH   (Germany)

^c MAX PLANCK INSTITUTE OF BIOCHEMISTRY   (Germany)

Author keywords

CDK8; cyclin C; kinase inhibitor

Indexed keywords

ANTINEOPLASTIC AGENT; CYCLIN C; CYCLIN DEPENDENT KINASE INHIBITOR; FLAVOPIRIDOL; HYDROGEN; STAT1 PROTEIN;

ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; BINDING ASSAY; COLORECTAL CARCINOMA; CONTROLLED STUDY; CRYSTALLIZATION; DRUG BINDING; DRUG DESIGN; DRUG POTENCY; DRUG SOLUBILITY; DRUG SPECIFICITY; DRUG STRUCTURE; EC50; EFFUSION; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; ENZYME SUBSTRATE; FOLLOW UP; HCT116 CELL LINE; HUMAN; HYDROGEN BOND; IC50; LIPOPHILICITY; MOUSE; NONHUMAN; PH; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; RAT;

EID: 84960925593     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00278     Document Type: Article

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