Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8

ACS Medicinal Chemistry Letters

Volumn 7, Issue 6, 2016, Pages 595-600

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

^a GENENTECH INC   (United States)

^b PROTEROS BIOSTRUCTURES GMBH   (Germany)

^c MAX PLANCK INSTITUTE OF BIOCHEMISTRY   (Germany)

^d NONE

Author keywords

CDK8; DMG out; inhibitor; Sorafenib

Indexed keywords

BENZOTHIOPHENE DERIVATIVE; CYCLIN C; CYCLIN DEPENDENT KINASE 8; CYCLIN DEPENDENT KINASE INHIBITOR; FLAVOPIRIDOL; SHORT HAIRPIN RNA; SORAFENIB; STAT1 PROTEIN;

ANTIPROLIFERATIVE ACTIVITY; ARTICLE; BINDING ASSAY; CLUSTERED REGULARLY INTERSPACED SHORT PALINDROMIC REPEAT; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG SOLUBILITY; FLUORESCENCE RESONANCE ENERGY TRANSFER; HCT116 CELL LINE; HINGE REGION; HYDROGEN BOND; PHARMACOPHORE; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; RACEMIC MIXTURE;

EID: 84974539464     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.6b00044     Document Type: Article

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