KEITH WILSON
Broker in Boston, MA

6387641, May 14, 2002

Dec 8, 1999

09/457040

Steven Bellon - Wellesly MA
Guy Bemis - Arlington MA
Keith Wilson - Boston MA
Matthew Fitzgibbon - Millis MA

Vertex Pharmaceuticals Incorporated - Cambridge MA

C12Q 148

435 15, 702 19, 702 22

This invention provides certain crystallized, protein kinase-ligand complexes, in particular P38-ligand complexes, and their structure coordinates. The structure coordinates are based on the structure of a phosphorylated P38 complex which has now been solved and which reveals new structural information useful for understanding the activated states of other, related kinase proteins as described herein. The key structural features of the proteins, particularly the shape of the substrate binding site, are useful in methods for designing or identifying selective inhibitors of the protein kinases, particularly P38 and in solving the structures of other proteins with similar features. The structure coordinates may be encoded in a data storage medium for use with a computer for graphical three-dimensional representation of the structure and for computer-aided molecular design of new inhibitors.

2003009, May 22, 2003

May 13, 2002

10/145862

Steven Bellon - Wellesly MA, US
Guy Bemis - Arlington MA, US
Keith Wilson - Boston MA, US
Matthew Fitzgibbon - Millis MA, US

G01N033/53, G06F019/00, G01N033/48, G01N033/50, C12N009/12

435/007100, 702/019000, 435/194000

This invention provides certain crystallized, protein kinase-ligand complexes, in particular P38-ligand complexes, and their structure coordinates. The structure coordinates are based on the structure of a phosphorylated P38 complex which has now been solved and which reveals new structural information useful for understanding the activated states of other, related kinase proteins as described herein. The key structural features of the proteins, particularly the shape of the substrate binding site, are useful in methods for designing or identifying selective inhibitors of the protein kinases, particularly P38 and in solving the structures of other proteins with similar features. The structure coordinates may be encoded in a data storage medium for use with a computer for graphical three-dimensional representation of the structure and for computer-aided molecular design of new inhibitors.

6849716, Feb 1, 2005

Aug 18, 2000

09/642749

Michael Shin-San Su - Newton MA, US
Ted Fox - Maynard MA, US
Keith Philip Wilson - Boston MA, US
Ursula A. Germann - Newton MA, US

Vertex Pharmaceuticals Incorporated - Cambridge MA

C12P 2104

530350, 530300, 435 691, 435 711

The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.

2003016, Sep 4, 2003

Jun 12, 2002

10/170663

Michael Su - Newton MA, US
Ted Fox - Maynard MA, US
Keith Wilson - Boston MA, US
Ursula Germann - Newton MA, US

Vertex Pharmaceuticals, Inc.

C12Q001/68, G06G007/48, G06G007/58, C12N009/99, C12P021/02

435/006000, 435/069200, 435/184000, 703/011000

The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.