Detection of gleevec resistant mutations

Details Detection of gleevec resistant mutations Detection of gleevec resistant mutations

2007-10-17

2008-08-26

Monshipouri, Maryam (Department: 1656)

Chemistry: molecular biology and microbiology

Enzyme , proenzyme; compositions thereof; process for...

Transferase other than ribonuclease

C530S350000

Reexamination Certificate

active

07416873

ABSTRACT:
The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.

REFERENCES:
patent: 2003/0158105 (2003-08-01), Sawyers et al.
patent: WO 97/08184 (1997-03-01), None
Corbin et al., “Analysis of the Structural Basis of Specificity of Inhibition of Abl Kinase by STI571,”Am. Soc. Hematol. Washington DC (2000)—Abstract.
Warmuth et al., “Genetic Analysis of the ATP Binding Sites of HCK and ABL Kinases Reveal Distinct and Overlapping Determinants for the Specficity of the Tyrosine Kinase Inhibitors PP1 and STI571,”Am. Soc. Hematol., Washington DC (2000)—Abstract.
Gorre et al., “Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification,”Science293(5531):879-880 (2001).
Barthe et al., “Roots of Clinical Resistance to STI-571 Cancer Therapy,”Science293(5538):3 pages—2163a (2001).
Hockhaus et al., “Roots of Clinical Resistance to STI-571 Cancer Therapy,”Science293(5538):3 pages—2163a (2001).
Hofmann et al., “Ph+ Acute Lymphoblastic Leukemias Resistant to STI571 (Glivec) Have a Novel and Unique BCR-ABL Gene Mutation,”Am. Soc. Hematol. Washington DC (2001)—Abstract.
Druker et al., “Activity of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in the Blast Crisis of Chronic Myeloid Leukemia and Acute Lymphoblastic Leukemia with the Philadelphia Chromosome,”N. Engl. J. Med. 344(14):1038-1042 (2001).
Druker et al., “Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells,”Nature Medicine2(5):561-566 (1996).

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