CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

Proceedings of the National Academy of Sciences of the United States of America

Volumn 112, Issue 34, 2015, Pages 10768-10773

  Hammitzsch, Ariane ^a   Tallant, Cynthia ^b   Fedorov, Oleg ^b   O'Mahony, Alison ^c   Brennan, Paul E ^b   Hay, Duncan A ^b,e   Martinez, Fernando O ^a   Al Mossawi, M Hussein ^a   De Wit, Jelle ^a   Vecellio, Matteo ^a   Wells, Christopher ^b,f   Wordsworth, Paul ^a   Müller, Susanne ^b   Knapp, Stefan ^a,b,d   Bowness, Paul ^a  

^a UNIVERSITY OF OXFORD   (United Kingdom)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c DiscoveRx Corporation   (United States)

^d GOETHE UNIVERSITY   (Germany)

^e EVOTEC UK LTD   (United Kingdom)

^f CARDIFF UNIVERSITY   (United Kingdom)

Author keywords

Ankylosing spondylitis; Bromodomain; CBP p300; Epigenetic inhibitors; Th17

Indexed keywords

4 (4 CHLOROPHENYL) 2,3,9 TRIMETHYL 6H THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE 6 ACETIC ACID TERT BUTYL ESTER; BRD2 PROTEIN; BRD4 PROTEIN; BROMODOMAIN INHIBITOR; CBP 30; GAMMA INTERFERON; GELATINASE B; GRANULOCYTE MACROPHAGE COLONY STIMULATING FACTOR; INTERLEUKIN 10; INTERLEUKIN 17; INTERLEUKIN 17F; INTERLEUKIN 1ALPHA; INTERLEUKIN 2; INTERLEUKIN 21; INTERLEUKIN 22; INTERLEUKIN 23 RECEPTOR; INTERLEUKIN 6; INTERLEUKIN 8; INTERSTITIAL COLLAGENASE; MONOCYTE CHEMOTACTIC PROTEIN 1; PROTEIN; TISSUE PLASMINOGEN ACTIVATOR; TRANSCRIPTION FACTOR T BET; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; VASCULAR CELL ADHESION MOLECULE 1; (+)-JQ1 COMPOUND; AZEPINE DERIVATIVE; BENZIMIDAZOLE DERIVATIVE; CBP30 COMPOUND; HISTONE ACETYLTRANSFERASE PCAF; IL17A PROTEIN, HUMAN; IMMUNOSUPPRESSIVE AGENT; ISOXAZOLE DERIVATIVE; RECOMBINANT PROTEIN; TRIAZOLE DERIVATIVE;

ANKYLOSING SPONDYLITIS; ANTIINFLAMMATORY ACTIVITY; ARTICLE; BINDING KINETICS; BLEACHING; CD4+ T LYMPHOCYTE; CELL VIABILITY; CONTROLLED STUDY; CYTOKINE PRODUCTION; CYTOKINE RELEASE; DOWN REGULATION; ENZYME LINKED IMMUNOSORBENT ASSAY; GENE EXPRESSION; HUMAN; HUMAN CELL; HYDROGEN BOND; IMMUNOCOMPETENT CELL; ISOTHERMAL TITRATION CALORIMETRY; LYMPHOCYTE SUBPOPULATION; NUCLEAR LOCALIZATION SIGNAL; PHENOTYPE; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN PROTEIN INTERACTION; PSORIATIC ARTHRITIS; TH1 CELL; TH17 CELL; ADULT; AGED; ANTAGONISTS AND INHIBITORS; BIOSYNTHESIS; CALORIMETRY; CELL CULTURE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; DRUG SCREENING; FEMALE; GENE EXPRESSION REGULATION; GENETICS; IMMUNOLOGY; KINETICS; MALE; METABOLISM; MIDDLE AGED; PATHOLOGY; PROTEIN CONFORMATION; PROTEIN TERTIARY STRUCTURE; SECRETION (PROCESS); STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ADULT; AGED; ARTHRITIS, PSORIATIC; AZEPINES; BENZIMIDAZOLES; CALORIMETRY; CD4-POSITIVE T-LYMPHOCYTES; CELLS, CULTURED; CRYSTALLOGRAPHY, X-RAY; DRUG EVALUATION, PRECLINICAL; FEMALE; GENE EXPRESSION REGULATION; HUMANS; IMMUNOSUPPRESSIVE AGENTS; INTERLEUKIN-17; ISOXAZOLES; KINETICS; MALE; MIDDLE AGED; MODELS, MOLECULAR; MOLECULAR STRUCTURE; P300-CBP TRANSCRIPTION FACTORS; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; RECOMBINANT PROTEINS; SPONDYLITIS, ANKYLOSING; STRUCTURE-ACTIVITY RELATIONSHIP; TH17 CELLS; TRIAZOLES;

EID: 84940533695     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1501956112     Document Type: Article

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