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  • Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine
    [作者:HAGEL MARGIT; NIU DEQIANG; ST MARTIN THIA; SHEETS MICHAEL P; QIAO LIXIN; BERNARD HUGUES; KARP RUSSELL M; ZHU ZHENDONG; LABENSKI MATTHEW T; CHATURVEDI PRASOON; NACHT MARIANA; WESTLIN WILLIAM F; PETTER RUSSELL C; SINGH JUSWINDER,期刊:NATURE CHEMICAL BIOLOGY, 页码:22-24 , 文章类型: Article,,卷期:2011年7-1]
  • Designing selective inhibitors of proteases has proven problematic, in part because pharmacophores that confer potency exploit the conserved catalytic apparatus. We developed a fundamentally different approach by designi...
  • Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis
    [作者:DI PAOLO JULIE A; HUANG TAO; BALAZS MERCEDESZ; BARBOSA JAMES; BARCK KAI H; BRAVO BRANDON J; CARANO RICHARD A D; DARROW JAMES; DAVIES DOUGLAS R; DEFORGE LAURA E; DIEHL LAURI; FERRANDO RONALD; GALLION STEVEN L; GIANNETTI ANTHONY M; GRIBLING PETER; HUREZ VINCENT; HYMOWITZ SARAH G; JONES RANDALL; KROPF JEFFREY E; LEE WYNE P; MACIEJEWSKI PATRICIA M; MITCHELL SCOTT A; RONG HONG; STAKER BART L; WHITNEY J ANDREW; YEH SHERRY; YOUNG WENDY B; YU CHRISTINE; ZHANG JUAN; REIF KARIN; CURRIE KEVIN S,期刊:NATURE CHEMICAL BIOLOGY, 页码:41-50 , 文章类型: Article,,卷期:2011年7-1]
  • Bruton's tyrosine kinase (Btk) is a therapeutic target for rheumatoid arthritis, but the cellular and molecular mechanisms by which Btk mediates inflammation are poorly understood. Here we describe the discovery of CGI17...