Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol

Journal of Biological Chemistry

Volumn 290, Issue 8, 2015, Pages 4573-4589

  Goedken, Eric R ^a   Argiriadi, Maria A ^a   Banach, David L ^a   Fiamengo, Bryan A ^a   Foley, Sage E ^a   Frank, Kristine E ^a   George, Jonathan S ^a   Harris, Christopher M ^a   Hobson, Adrian D ^a   Ihle, David C ^a   Marcotte, Douglas ^a   Merta, Philip J ^a   Michalak, Mark E ^a   Murdock, Sara E ^a   Tomlinson, Medha J ^a   Voss, Jeffrey W ^a  

^a ABBVIE INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BIOCHEMISTRY;

ACTIVE SITE; JANUS KINASE; SELECTIVE INHIBITORS;

BIOLOGY;

ADENOSINE TRIPHOSPHATE; CYSTEINE; DIMETHYL SULFOXIDE; ELECTROPHILE; INTERLEUKIN 6; JANUS KINASE 1; JANUS KINASE 3; JANUS KINASE 3 INHIBITOR; STAT3 PROTEIN; STAT5 PROTEIN; THIOL; TOFACITINIB; JAK3 PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR;

ANIMAL CELL; ARTICLE; AUTOIMMUNE DISEASE; BINDING COMPETITION; CELL ASSAY; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMAN; HUMAN CELL; IN VITRO STUDY; LIQUID CHROMATOGRAPHY; NONHUMAN; PRIORITY JOURNAL; PROTEIN INDUCTION; TANDEM MASS SPECTROMETRY; X RAY CRYSTALLOGRAPHY; ANALOGS AND DERIVATIVES; ANTAGONISTS AND INHIBITORS; AUTOIMMUNE DISEASES; CELL LINE; CHEMISTRY; ENZYMOLOGY; GENETICS; METABOLISM;

ADENOSINE TRIPHOSPHATE; AUTOIMMUNE DISEASES; CATALYTIC DOMAIN; CELL LINE; HUMANS; JANUS KINASE 3; PROTEIN KINASE INHIBITORS;

EID: 84929486174     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M114.595181     Document Type: Article

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