Barbara N Mroczkowski from Solomons, MD, age 70

Us Patents

Modifications Of The Vegf Receptor-2 Protein And Methods Of Use
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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.

Modifications Of The Vegf Receptor-2 Protein And Methods Of Use
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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.

Modifications Of The Vegf Receptor-2 Protein And Methods Of Use
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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.

Modifications Of The Vegf Receptor-2 Protein And Methods Of Use
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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.

Catalytic Domains Of The Human Hepatocyte Growth Factor Receptor Tyrosine Kinase, And Materials And Methods For Identification Of Inhibitors Thereof
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US Patent:

20040009568, Jan 15, 2004
Filed:

Mar 25, 2002
Appl. No.:

10/106938
Inventors:

Barbara Mroczkowski - Encinitas CA, US
Michael Hickey - San Diego CA, US
Michele McTigue - Encinitas CA, US
Brion Murray - San Diego CA, US
Hans Parge - San Diego CA, US
Jay Sarup - San Diego CA, US
Jeff Zhu - Carlsbad CA, US
International Classification:

G06F019/00
G01N033/48
G01N033/50
C12N009/12
C07K014/71
US Classification:

435/194000, 530/350000, 702/019000
Abstract:

The identification, isolation, purification, and characterization of the catalytic domain of the human hepatocyte growth factor receptor kinase (hHGFR) are described. A crystal structure of the hHGFR kinase domain is reported herein. This structure provides a three-dimensional description of the binding site of the hHGFR for structure-based design of small molecule inhibitors thereof as therapeutic agents. The kinase domain of human HGFR and its associated crystal structure is described for use in the discovery, identification and characeterization of modulators of human HGFR.

Pin1 Peptidyl-Prolyl Isomerase Polypeptides, Their Crystal Structures, And Use Thereof For Drug Design
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US Patent:

20040171019, Sep 2, 2004
Filed:

Dec 19, 2003
Appl. No.:

10/616003
Inventors:

David Matthews - Encinitas CA, US
Eleanor Dagostino - San Diego CA, US
Rose Ferre - Carlsbad CA, US
Smita Gaur - San Diego CA, US
Chuangxing Guo - San Diego CA, US
Xinjun Hou - San Diego CA, US
Stephen Margosiak - Escondido CA, US
Barbara Mroczkowski - Encinitas CA, US
Grace Nakayama - San Diego CA, US
Hans Parge - San Diego CA, US
Jeff Zhu - San Diego CA, US
Assignee:

Agouron Pharmaceuticals, Inc.
International Classification:

C12Q001/68
C07H021/04
C12N009/64
US Classification:

435/006000, 435/069100, 435/320100, 435/325000, 435/226000, 536/023200
Abstract:

Polypeptides containing the PIN1 peptidyl-prolyl isomerase domain but not containing the PIN1 WW domain are described. Also described are crystal structures of these polypeptides, including the crystal structure of a PIN1 PPIase:ligand complex. The structure coordinate data derived from these crystals provides a three-dimensional description of the substrate-binding site of PIN1 peptidyl-prolyl isomerase useful in drug discovery and design for the identification and design of modulators of PIN1 peptidyl-prolyl isomerase activity.

Modifications Of The Vegf Receptor-2 Protein And Methods Of Use
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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.