发明名称 |
Modifications of the VEGF receptor-2 protein and methods of use |
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.
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申请公布号 |
US6849721(B2) |
申请公布日期 |
2005.02.01 |
申请号 |
US20010939754 |
申请日期 |
2001.08.28 |
申请人 |
AGOURON PHARMACEUTICALS, INC. |
发明人 |
MCTIGUE MICHELE A.;PINKO CHRIS;PARAST CAMRAN V.;GEHRING MICHAEL R.;KAN CHEN-CHEN;APPELT KRZYSZTOF;WICKERSHAM JOHN A.;SHOWALTER RICHARD E.;TEMPCYZK-RUSSELL ANNA M.;MROCZKOWSKI BARBARA;VILLAFRANCA JESUS E. |
分类号 |
G01N23/20;C07K14/71;C12N9/12;C12N15/09;C12Q1/48;G01N33/15;G01N33/50;G01N37/00;(IPC1-7):C07K1/00;C12P21/06;C12N9/00;A01N43/04;C07H21/02 |
主分类号 |
G01N23/20 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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