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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：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：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：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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