Inventors:
Ping Chen - San Diego CA, US
Mark Anderson - San Diego CA, US
Ya-Li Deng - San Diego CA, US
Smita Gaur - San Diego CA, US
Chen Kan - Arcadia CA, US
Chun Luo - San Diego CA, US
Karen Lundgren - San Diego CA, US
Stephen Margosiak - Escondido CA, US
Binh Nguyen - San Diego CA, US
Patrick O'Connor - San Diego CA, US
James Reqister - San Diego CA, US
Anna Russell - San Diego CA, US
Jay Sarup - San Diego CA, US
International Classification:
C12P021/02, C07H021/04, C12N009/12, C12N005/06
US Classification:
435/194000, 435/069100, 435/320100, 435/325000, 536/023200
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.