发明名称 HUMAN PAPILLOMAVIRUS E2 TRANSACTIVATION DOMAIN/INHIBITOR CO-CRYSTAL AND X-RAY COORDINATES DEFINING THE INHIBITOR-BINDING POCKET
摘要 A crystallizable composition, comprising an PV E2 TAD-like polypeptide of SEQ ID NO.2 complexed with an inhibitor L. The invention also provides a method for producing the crystallized HPV E2 TAD-inhibitor complex (HPV E2 TAD-L) comprising: a) mixing purified HPV E2 TAD, contained in a purification buffer, with solublized inhibitor L to generate a complex solution containing the HPV E2 TAD-L complex; and b) crystallizing the complex from a) in a crystallization buffer. The invention also provides a method for producing crystallized apo HPV E2 TAD, comprising: a) mixing apo HPV E2 TAD, contained in a purification buffer, with a crystallization buffer.X-ray crystal structure coordinates the HPV E2 TAD-L complex, are also provided, which define an inhibitor binding pocket. The inhibitor binding pocket is useful for screening potential small molecule inhibitors that bind to the pocket.
申请公布号 WO03006495(A3) 申请公布日期 2003.07.31
申请号 WO2002CA01058 申请日期 2002.07.12
申请人 BOEHRINGER INGELHEIM INTERNATIONAL GMBH;CAMERON, DALE, R.;ARCHAMBAULT, JACQUES;YOAKIM, CHRISTIANE;WHITE, PETER;WANG, YONG 发明人 CAMERON, DALE, R.;ARCHAMBAULT, JACQUES;YOAKIM, CHRISTIANE;WHITE, PETER
分类号 C12N15/09;A61K45/00;A61P15/00;A61P17/12;A61P31/20;A61P35/00;C07D405/12;C07D417/12;C07K14/025 主分类号 C12N15/09
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