Catalytic domain of the human effector cell cycle checkpoint protein kinase materials and methods for identification of inhibitors thereof

US6670167B1 · kind B1 · utility

Assignee

• Agouron Pharmaceuticals, Inc. · US

Inventors

• Ping Chen · San Diego, US
• Mark B. Anderson · Salt Lake City, US
• Ya-Li Deng · San Diego, US
• Smita Gaur · San Diego, US
• Chen-Chen Kan · Lake Forest, US
• Chun Luo · San Diego, US
• Karen LUNDGREN · San Diego, US
• Stephen Margosiak · Escondido, US
• Binh Nguyen · Indianapolis, US
• Patrick O'Connor · San Diego, US
• James C. Register, III · Ames, US
• Anna Russell · Ramona, US
• Jay Sarup · San Diego, US

Key dates

• Filing date: Dec 14, 1999
• Grant date: Dec 30, 2003
• Expiry date: Dec 14, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12Q1/34
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7å 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.