发明公开
- 专利标题: MUTATED ABL KINASE DOMAINS
- 专利标题(中): 突变体ABL激酶结构域
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申请号: EP02782829.2申请日: 2002-10-04
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公开(公告)号: EP1436384A2公开(公告)日: 2004-07-14
- 发明人: BARTHE, Christophe , BRANFORD, Susan , CORBIN, Amie , DRUKER, Brian, Jay , DUYSTER, Justus , HOCHHAUS, Andreas , HUGHES, Timothy , KREIL, Sebastian , LEGUAY, Thibaut , MAHON, François-Xavier , MARIT, Gérald , MÜLLER, Martin , PESCHEL, Christian , PREUDHOMME, Claude , ROCHE LESTIENNE, Catherine , RUDZKI, Zbigniew
- 申请人: Novartis AG , Université Victor Segalen Bordeaux 2 , Technische Universität München , Oregon Health & Science University , Universität Heidelberg , CHRU DE LILLE,centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
- 申请人地址: Lichtstrasse 35 4056 Basel CH
- 专利权人: Novartis AG,Université Victor Segalen Bordeaux 2,Technische Universität München,Oregon Health & Science University,Universität Heidelberg,CHRU DE LILLE,centre Hospitalier Regional Universitaire de Lille,MEDVET SCIENCE PTY. LTD.
- 当前专利权人: Novartis AG,Université Victor Segalen Bordeaux 2,Technische Universität München,Oregon Health & Science University,Universität Heidelberg,CHRU DE LILLE,centre Hospitalier Regional Universitaire de Lille,MEDVET SCIENCE PTY. LTD.
- 当前专利权人地址: Lichtstrasse 35 4056 Basel CH
- 代理机构: Grubb, Philip William
- 优先权: US327389P 20011005; US328740P 20011012; US347351P 20020111
- 国际公布: WO2003031608 20030417
- 主分类号: C12N9/12
- IPC分类号: C12N9/12
摘要:
The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
公开/授权文献
- EP1436384B1 MUTATED ABL KINASE DOMAINS 公开/授权日:2009-06-17
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