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公开(公告)号：US20050244819A1
公开(公告)日：2005-11-03
申请号：US11082251
申请日：2005-03-15
申请人： Ting-Jen Cheng , Chen-Chen Kan
发明人： Ting-Jen Cheng , Chen-Chen Kan
IPC分类号： C07H21/00 , C07H21/02 , C07K14/16 , C12N9/38 , C12N9/50 , C12N9/72 , C12N15/867 , C12Q1/37 , C12Q1/70 , G01N33/569
CPC分类号： C07K14/005 , C07K2319/50 , C07K2319/61 , C12N9/2471 , C12N9/503 , C12N9/506 , C12N2740/16222 , C12Q1/37 , C12Y302/01023 , G01N33/56988 , G01N2500/10
摘要： Compositions and methods for identifying agents that inhibit protease activity are provided. In particular, polynucleotides, recombinant expression vectors, and host cells are provided that may be used in a bacterial cell-based assay for identifying agents that are inhibitors of protease activity, such as inhibitors of HIV protease activity. The bacterial cells express a precursor of a protease and encode a reporter polypeptide that contains a protease recognition sequence, which can be cleaved by the mature, catalytically active protease such that the reporter activity of the reporter polypeptide is decreased or eliminated.
摘要翻译： 提供了用于鉴定抑制蛋白酶活性的试剂的组合物和方法。 特别地，提供了多核苷酸，重组表达载体和宿主细胞，其可用于基于细菌细胞的测定中，用于鉴定作为蛋白酶活性抑制剂的试剂，例如HIV蛋白酶活性的抑制剂。 细菌细胞表达蛋白酶的前体，并编码含有蛋白酶识别序列的报道多肽，其可被成熟的催化活性蛋白酶切割，使得报道多肽的报道活性降低或消除。
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公开(公告)号：US06787327B2
公开(公告)日：2004-09-07
申请号：US10265012
申请日：2002-10-04
申请人： Chen-Chen Kan , Ting-Jen Cheng
发明人： Chen-Chen Kan , Ting-Jen Cheng
IPC分类号： C12Q134
摘要： The present invention provides human tyrosine-DNA phosphodiesterases (TDPs). In particular, the present invention provides novel recombinant nucleic acids and proteins, including mutant TDPs, vectors, and TDP-producing cells, as well as co-factors for enzyme activity. The present invention further provides methods for high through-put enzymatic assay systems utilizing the TDPs of the present invention.
摘要翻译： 本发明提供人酪氨酸 - 磷酸二酯酶（TDP）。 特别地，本发明提供新的重组核酸和蛋白质，包括突变体TDP，载体和产生TDP的细胞，以及酶活性的辅因子。 本发明还提供了利用本发明的TDP的高通量酶分析系统的方法。
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公开(公告)号：US06753416B2
公开(公告)日：2004-06-22
申请号：US09939833
申请日：2001-08-28
申请人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
发明人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
IPC分类号： C07H2104
摘要： A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
摘要翻译： 含有血管内皮生长因子受体2（VEGFR2 / KDR）的催化激酶结构域的蛋白质构建体的一个2.4“晶体结构是血管生成中的关键酶，在非配位的磷酸化状态下已被确定。 该蛋白质构建体含有修饰的催化接头，并且具有与体内激酶活性相当的含有整个KID的构建体。 得到的构建物保持与野生型KID相当的体外激酶活性，更重要的是允许蛋白质的完全结晶，使得其可以通过X射线晶体学表征。 本发明还公开了X射线晶体学数据用于鉴定和构建可能的治疗化合物以治疗各种疾病状况。
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公开(公告)号：US06784285B1
公开(公告)日：2004-08-31
申请号：US09506906
申请日：2000-02-18
申请人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
发明人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
IPC分类号： C07K100
摘要： A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
摘要翻译： 含有血管内皮生长因子受体2（VEGFR2 / KDR）的催化激酶结构域的蛋白质构建体的一个2.4“晶体结构是血管生成中的关键酶，已经在非配位的磷酸化状态下被确定。 该蛋白质构建体含有修饰的催化接头，并且具有与体内激酶活性相当的含有整个KID的构建体。 得到的构建物保持与野生型KID相当的体外激酶活性，更重要的是允许蛋白质的完全结晶，使得其可以通过X射线晶体学表征。 本发明还公开了X射线晶体学数据用于鉴定和构建可能的治疗化合物以治疗各种疾病状况。
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公开(公告)号：US06316603B1
公开(公告)日：2001-11-13
申请号：US09390326
申请日：1999-09-07
申请人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
发明人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
IPC分类号： C07K100
摘要： A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
摘要翻译： 含有血管内皮生长因子受体2（VEGFR2 / KDR）的催化激酶结构域的蛋白质构建体的2.4晶体结构是血管生成中的关键酶，已经在未配位的磷酸化状态下测定。 该蛋白质构建体含有修饰的催化接头，并且具有与体内激酶活性相当的含有整个KID的构建体。 得到的构建物保持与野生型KID相当的体外激酶活性，更重要的是允许蛋白质的完全结晶，使得其可以通过X射线晶体学表征。 本发明还公开了用于鉴定和构建可能的治疗化合物的X射线晶体学数据在治疗各种疾病状况
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公开(公告)号：US06849721B2
公开(公告)日：2005-02-01
申请号：US09939754
申请日：2001-08-28
申请人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
发明人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
IPC分类号： G01N23/20 , C07K14/71 , C12N9/12 , C12N15/09 , C12Q1/48 , G01N33/15 , G01N33/50 , G01N37/00 , C07K1/00 , C12P21/06 , C12N9/00 , A01N43/04 , C07H21/02
摘要： A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of the x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
摘要翻译： 含有血管内皮生长因子受体2（VEGFR2 / KDR）的催化激酶结构域的蛋白质构建体的一个2.4“晶体结构是血管生成中的关键酶，已经在非配位的磷酸化状态下被确定。 该蛋白质构建体含有修饰的催化接头，并且具有与体内激酶活性相当的含有整个KID的构建体。 得到的构建物保持与野生型KID相当的体外激酶活性，更重要的是允许蛋白质的完全结晶，使得其可以通过X射线晶体学表征。 本发明还公开了用于鉴定和构建可能的治疗化合物的X射线晶体学数据在治疗各种疾病状况中的用途。
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公开(公告)号：US06794146B2
公开(公告)日：2004-09-21
申请号：US09939832
申请日：2001-08-28
申请人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
发明人： Michele A. McTigue , Chris Pinko , Camran V. Parast , Michael R. Gehring , Chen-Chen Kan , Krzysztof Appelt , John A. Wickersham , Richard E. Showalter , Anna M. Tempcyzk-Russell , Barbara Mroczkowski , Jesus E. Villafranca
IPC分类号： G01N3353
摘要： A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
摘要翻译： 含有血管内皮生长因子受体2（VEGFR2 / KDR）的催化激酶结构域的蛋白质构建体的一个2.4“晶体结构是血管生成中的关键酶，已经在非配位的磷酸化状态下被确定。 该蛋白质构建体含有修饰的催化接头，并且具有与体内激酶活性相当的含有整个KID的构建体。 得到的构建物保持与野生型KID相当的体外激酶活性，更重要的是允许蛋白质的完全结晶，使得其可以通过X射线晶体学表征。 本发明还公开了用于鉴定和构建可能的治疗化合物的X射线晶体学数据在治疗各种疾病状况中的用途。
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