James W Register

US Patent:

6670167, Dec 30, 2003

Filed:

Dec 14, 1999

Appl. No.:

09/460421

Inventors:

Ping Chen - San Diego CA
Mark Anderson - San Diego CA
Ya-Li Deng - San Diego CA
Smita Gaur - San Diego CA
Chen Chen Kan - Arcadia CA
Chun Luo - San Diego CA
Karen Lundgren - San Diego CA
Stephen Margosiak - Escondido CA
Binh Nguyen - San Diego CA
Patrick OConnor - San Diego CA
James Register - San Diego CA
Anna Tempczyk Russell - San Diego CA
Jay Sarup - San Diego CA

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07H 2104

US Classification:

43525233, 4352351, 435348, 43525411, 4352523, 435419, 435325, 4353201, 536 232, 536 235

Abstract:

The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1. 7 crystal structure of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer.