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1. 发明授权

US07167801B2 Method of identifying potential inhibitors of human papillomavirus protein E2 using x-ray atomic coordinates 有权
标题翻译：使用x射线原子坐标识别人乳头瘤病毒蛋白E2的潜在抑制剂的方法
公开(公告)号：US07167801B2
公开(公告)日：2007-01-23
申请号：US10193460
申请日：2002-07-11
申请人： Dale R. Cameron , Jacques Archambault , Christiane Yoakim , Peter White , Yong Wang
发明人： Dale R. Cameron , Jacques Archambault , Christiane Yoakim , Peter White , Yong Wang
IPC分类号： G06F7/58
CPC分类号： C07D405/12 , C07D417/12 , C07K14/005 , C07K2299/00 , C12N2710/20022
摘要： A crystallizable composition, comprising an human papillomavirus (HPV-11) E2 transactivation domain (TAD)-like polypeptide of SEQ ID NO. 2 complexed with an inhibitor L (sodium (2R,3R,4S,5R)-5-(3,4-dichlorophenyl)-5′-methyl-1′,3′-dioxo-4-({[4-(1,2,3-thiadiazol-4-yl)phenyl]amino}carbonyl)-1′,3′,4,5-tetrahydro-3H-spiro[furan-2,2′-indene]-3-carboxylate). 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 that may be inhibitors of papillomavirus infection.
摘要翻译：一种可结晶组合物，其包含SEQ ID NO.1的人乳头状瘤病毒（HPV-11）E2反式激活结构域（TAD）样多肽。 2与抑制剂L（（2R，3R，4S，5R）-5-（3,4-二氯苯基）-5'-甲基-1'，3'-二氧代-4 - （{[4-（1 ，2,3-噻二唑-4-基）苯基]氨基}羰基）-1'，3'，4,5-四氢-3H-螺[呋喃-2,2'-茚] -3-羧酸乙酯）。本发明还提供了一种生产结晶的HPV E2 TAD抑制剂复合物（HPV E2 TAD-L）的方法，包括：a）将纯化缓冲液中纯化的HPV E2 TAD与溶出的抑制剂L混合以产生含有 HPV E2 TAD-L复合物; 和b）从结晶缓冲液中的a）结晶复合物。本发明还提供了一种用于生产结晶apo HPV E2 TAD的方法，其包括：a）将包含在纯化缓冲液中的apo HPV E2 TAD与结晶缓冲液混合。还提供X射线晶体结构协调HPV E2 TAD-L复合物，其定义了抑制剂结合口袋。抑制剂结合口袋可用于筛选结合口袋的可能是乳头瘤病毒感染抑制剂的潜在小分子抑制剂。

2. 发明申请

US20050287554A1 Regions of papilloma virus E1 helicase involved in E1 oligomerization 审中-公开
公开(公告)号：US20050287554A1
公开(公告)日：2005-12-29
申请号：US11112784
申请日：2005-04-22
申请人： Jacques Archambault
发明人： Jacques Archambault
IPC分类号： G01N33/50 , A61K38/00 , A61K39/00 , C07K14/025 , C12N15/09 , C12N15/37 , C12Q1/68 , C12Q1/70 , G01N33/15 , G01N33/53 , G01N33/539 , G01N33/566 , G01N33/569 , G01N33/573
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , C12N2710/20022 , C12Q1/708 , G01N33/56983 , G01N33/573 , G01N2333/025 , G01N2500/00
摘要： There is provided an amino acid sequence comprised within the PV E1 protein region A delineated by amino acids 352 and 439, and any derivative variant or fragment thereof, necessary for the oligomerization of the E1 protein. This amino acid sequence is capable of self-association and of associating with the full length E1 protein and any derivative, variant or fragment thereof comprising the sequence of this invention. A specific aspect of this first embodiment, the amino acid domain of this invention delimited by amino acids 353 to 438 of the PV E1 protein. More particularly, the amino acid domain of this invention is as defined by SEQ ID NO. 2. There is also provided a cross-linking assay to directly measure the level of oligomerization (or inhibition thereof) of the E1 protein. In accordance with a fourth embodiment of this invention, there is provided a N-terminally truncated E1 protein. More particularly, one aspect of this fourth embodiment encompasses the E1 protein delimited by amino acid 72 to 649 (SEQ ID NO. 78).

3. 发明授权

US06916622B2 Regions of papilloma virus E1 helicase involved in E1 oligomerization 有权
标题翻译：乳头瘤病毒E1解旋酶区域参与E1寡聚化
公开(公告)号：US06916622B2
公开(公告)日：2005-07-12
申请号：US10339268
申请日：2003-01-09
申请人： Jacques Archambault
发明人： Jacques Archambault
IPC分类号： G01N33/50 , A61K38/00 , A61K39/00 , C07K14/025 , C12N15/09 , C12N15/37 , C12Q1/68 , C12Q1/70 , G01N33/15 , G01N33/53 , G01N33/539 , G01N33/566 , G01N33/569 , G01N33/573
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , C12N2710/20022 , C12Q1/708 , G01N33/56983 , G01N33/573 , G01N2333/025 , G01N2500/00
摘要： There is provided an amino acid sequence comprised within the PV E1 protein region A delineated by amino acids 352 and 439, and any derivative variant or fragment thereof, necessary for the oligomerization of the E1 protein. This amino acid sequence is capable of self-association and of associating with the full length E1 protein and any derivative, variant or fragment thereof comprising the sequence of this invention. A specific aspect of this first embodiment, the amino acid domain of this invention delimited by amino acids 353 to 438 of the PV E1 protein. More particularly, the amino acid domain of this invention is as defined by SEQ ID NO. 2. There is also provided a cross-linking assay to directly measure the level of oligomerization (or inhibition thereof) of the E1 protein. In accordance with a fourth embodiment of this invention, there is provided a N-terminally truncated E1 protein. More particularly, one aspect of this fourth embodiment encompasses the E1 protein delimited by amino acid 72 to 649 (SEQ ID NO. 78).
摘要翻译：提供了由E1蛋白的寡聚化所必需的PV E1蛋白质区域A所描绘的氨基酸序列，以及由氨基酸352和439所描绘的任何衍生变体或片段。该氨基酸序列能够自身结合并与全长E1蛋白及其包含本发明序列的任何衍生物，变体或片段缔合。本第一实施方案的具体方面，本发明的氨基酸结构域由PV E1蛋白质的氨基酸353至438界定。更具体地，本发明的氨基酸结构域如SEQ ID NO：还提供了直接测量E1蛋白的低聚（或抑制）水平的交联测定法。根据本发明的第四个实施方案，提供了N-末端截短的E1蛋白。更具体地，该第四实施方案的一个方面包括由氨基酸72至649（SEQ ID NO：78）限定的E1蛋白。

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