17-AAG Treatment of Diseases Sensitive to c-KIT Down Regulation
Description of Invention:
This invention describes the use of 17-allylamino-17-demethoxygeldanamycin (17-AAG), a derivative of geldanamycin, which inhibits mutated KIT protein kinase activity (the product of proto-oncogene c-KIT). This kinase has been identified as the protein responsible for transformation of certain human cell types into pathologic cells. The invention is predicated on the discovery of a new method of inhibiting the activity of a mutated, constitutively active form of the tyrosine kinase, KIT. The method involves the administration of 17-AAG to a cell expressing the mutated KIT protein, whereby the activity level of KIT in the cell is reduced. The invention may prove to be useful for treating diseases such as mastocytosis, gastrointestinal stromal tumors (GIST), mast cell leukemia, myelogenenous leukemia, and testicular cancer, all of which are associated with mutations in the c-KIT proto-oncogene.
Inventors:
Gerard Fumo and Len Neckers (NCI)
Patent Status:
DHHS Reference No. E-256-2002 filed 22 Oct 2002
Portfolios: Cancer
Cancer -Therapeutics-Biological Response Modifiers-Other Cancer -Therapeutics-Conventional Chemotherapy-Other Cancer -Therapeutics
For Additional Information Please Contact: Adaku Nwachukwu J.D.
NIH Office of Technology Transfer
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Phone: 301 435-5560
Email: madua@mail.nih.gov
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