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AssigneeAgouron Pharmaceuticals, Inc.
InventorsPing Chen, Mark Anderson, Ya-Li Deng, Smita Gaur, Chen Chen Kan, Chun Luo, Karen Lundgren, Stephen Margosiak, Binh Nguyen, Patrick O'Connor, James Register, Anna Tempczyk Russell, Jay Sarup
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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.
A composition comprising an isolated, purified polynucleotide, which encodes a catalytically active human ChkI kinase domain as represented by the polypeptide consisting of amino acids 1-291 of SEQ ID NO:2.
An expression vector comprising a polynucleotide encoding a catalytically active human ChkI kinase domain as represented by the polypeptide consisting of amino acids of amino acids 1-291 of SEQ ID NO:2 and a selectable marker.
A host cell stably transformed or transfected with a polynucleotide encoding a catalytically active human ChkI domain as represented by the polypeptide consisting of amino acids 1-291 of SEQ ID NO:2 in a manner allowing the expression in said host cell of the human ChkI kinase domain.
A composition comprising an isolated, purified polynucleotide, which encodes a catalytically active human ChkI kinase domain as represented by the polypeptide consisting of amino acids 16-289 of SEQ ID NO:2.
A composition comprising an isolated, purified polynucleotide, which encodes a catalytically active human ChkI kinase domain as represented by the polypeptide consisting of amino acids 16-291 of SEQ ID NO:2.
A composition comprising an isolated, purified polynucleotide, which encodes a catalytically active human ChkI kinase domain as represented by the polypeptide consisting of amino acids 1-289 of SEQ ID NO:2.
Dependencies are inferred from the claim text.