INVENTOR(S)- Zhu, Xiaotian
PATENT NUMBER- 06589758
PATENT APPLICATION NUMBER- 862154
DATE FILED- 2001-05-21
PATENT DATE- 2003-07-08
NUMBER OF CLAIMS- 36
EXEMPLARY CLAIMS- 1
FIGURES- 32
ART/GROUP UNIT- 1627
PATENT CLASS- Invention (utility) patent
PATENT ASSIGNEE(S)- Amgen Inc.
ASSIGNEE CITY- Thousand Oaks
ASSIGNEE STATE- CA
ATTORNEY, AGENT, OR FIRM- Howard, Mary Susan; Levy, Ron K.; Odre, Steven M.
U.S. PATENT CLASS- 435015000O
U.S. CLASSIFICATION REFS. - X435004000; X530350000
INTERNATIONAL PATENT CLASS- 7C12Q00148; C12Q00100; C07K00100
FOREIGN DOCUMENT REFERENCE(S)- WO 200070030
FOREIGN COUNTRY CODE- WOX

The invention relates to the three-dimensional structure of a crystal of a kinase enzyme complexed with a ligand. The three-dimensional structure of a protein kinase-ligand complex is disclosed. The invention also relates to methods of preparing such crystals. Kinase-ligand crystal structures wherein the ligand is an inhibitor molecule are useful for providing structural information that may be integrated into drug screening and drug design processes. Thus, the invention also relates to methods of using the crystal structure of kinase enzyme-ligand complexes for identifying, designing, selecting, or testing inhibitors of kinase enzymes, such inhibitors being useful as therapeutics for the treatment or modulation of i) diseases; ii) disease symptoms; or iii) the effect of other physiological events mediated by kinases; having one or more kinase enzymes involved in their pathology.

EXEMPLARY CLAIMS- 1. A crystal of a protein-ligand complex comprising a protein-ligand complex of a truncated Ick and a ligand, wherein the crystal effectively diffracts X-rays for the determination of the atomic coordinates of the protein-ligand complex to a resolution of greater than 5.0 Angstroms; and wherein the truncated lck: (a) comprises amino acids 225 to 508 of SEQ ID NO: 1 or an amino acid sequence that differs from amino acids 225 to 508 of SEQ ID NO: 1 by only conservative substitutions; and (b) retains the globular core of the corresponding full-length lck.