The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 01, 2005

Filed:

Aug. 28, 2001
Applicants:

Michele A. Mctigue, Encinitas, CA (US);

Chris Pinko, San Diego, CA (US);

Camran V. Parast, San Diego, CA (US);

Michael R. Gehring, Ramona, CA (US);

Chen-chen Kan, Del Mare, CA (US);

Krzysztof Appelt, Poway, CA (US);

John A. Wickersham, Escondido, CA (US);

Richard E. Showalter, Lakeside, CA (US);

Anna M. Tempcyzk-russell, San Diego, CA (US);

Barbara Mroczkowski, Encinitas, CA (US);

Jesus E. Villafranca, San Diego, CA (US);

Inventors:

Michele A. McTigue, Encinitas, CA (US);

Chris Pinko, San Diego, CA (US);

Camran V. Parast, San Diego, CA (US);

Michael R. Gehring, Ramona, CA (US);

Chen-Chen Kan, Del Mare, CA (US);

Krzysztof Appelt, Poway, CA (US);

John A. Wickersham, Escondido, CA (US);

Richard E. Showalter, Lakeside, CA (US);

Anna M. Tempcyzk-Russell, San Diego, CA (US);

Barbara Mroczkowski, Encinitas, CA (US);

Jesus E. Villafranca, San Diego, CA (US);

Assignee:

Agouron Pharmaceuticals, Inc., San Diego, CA (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07K 100 ; C12P 2106 ; C12N 900 ; A01N 4304 ; C07H 2102 ;
U.S. Cl.
CPC ...
Abstract

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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