Michael M Gehring

US Patent:

6753416, Jun 22, 2004

Filed:

Aug 28, 2001

Appl. No.:

09/939833

Inventors:

Michele A. McTigue - Encinitas CA
Chris Pinko - San Diego CA
Camran V. Parast - San Diego CA
Michael R. Gehring - Ramona CA
Chen-Chen Kan - Del Mare CA
Krzysztof Appelt - Poway CA
John A. Wickersham - Escondido CA
Richard E. Showalter - Lakeside CA
Barbara Mroczkowski - Encinitas CA
Jesus E. Villafranca - San Diego CA

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07H 2104

US Classification:

536 231, 435183, 530300, 530350

Abstract:

A 2. 4 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.

US Patent:

6784285, Aug 31, 2004

Filed:

Feb 18, 2000

Appl. No.:

09/506906

Inventors:

Michele A. McTigue - Encinitas CA
Chris Pinko - San Diego CA
Camran V. Parast - San Diego CA
Michael R. Gehring - Ramona CA
Chen-Chen Kan - Del Mare CA
Krzysztof Appelt - Poway CA
John A. Wickersham - Escondido CA
Richard E. Showalter - Lakeside CA
Barbara Mroczkowski - Encinitas CA
Jesus E. Villafranca - San Diego CA

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07K 100

US Classification:

530402, 435 71, 435183, 530350, 536 231

Abstract:

A 2. 4 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.

US Patent:

6794146, Sep 21, 2004

Filed:

Aug 28, 2001

Appl. No.:

09/939832

Inventors:

Michele A. McTigue - Encinitas CA
Chris Pinko - San Diego CA
Camran V. Parast - San Diego CA
Michael R. Gehring - Ramona CA
Chen-Chen Kan - Del Mare CA
Krzysztof Appelt - Poway CA
John A. Wickersham - Escondido CA
Richard E. Showalter - Lakeside CA
Barbara Mroczkowski - Encinitas CA
Jesus E. Villafranca - San Diego CA

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

G01N 3353

US Classification:

435 71, 530300, 530350, 530402, 536 231

Abstract:

A 2. 4 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.

US Patent:

6849721, Feb 1, 2005

Filed:

Aug 28, 2001

Appl. No.:

09/939754

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
Barbara Mroczkowski - Encinitas CA, US
Jesus E. Villafranca - San Diego CA, US

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07K 100
C12P 2106
C12N 900
A01N 4304
C07H 2102

US Classification:

530402, 435 691, 435183, 514 44, 536 231

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.

US Patent:

63166038, Nov 13, 2001

Filed:

Sep 7, 1999

Appl. No.:

9/390326

Inventors:

Michele A. McTigue - Encinitas CA
Chris Pinko - San Diego CA
Camran V. Parast - San Diego CA
Michael R. Gehring - Ramona CA
Chen-Chen Kan - Del Mare CA
Krzysztof Appelt - Poway CA
John A. Wickersham - Escondido CA
Richard E. Showalter - Lakeside CA
Barbara Mroczkowski - Encinitas CA
Jesus E. Villafranca - San Diego CA

Assignee:

Agouron Pharmaceuticals, Inc. - La Jolla CA

International Classification:

C07K 100
C07K 1400
C12N 900

US Classification:

530402

Abstract:

A 2. 4. ANG. 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.

Address:

2121 Allen Pkwy, Houston, TX 77019

VIN:

5TFRV54137X007972

Make:

TOYOTA

Model:

TUNDRA

Year:

2007