Glivec Research - Gleevec, Imatinib, Cancer, Treatment, Side-effects

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Kit as a human oncogenic tyrosine kinase.

Kitamura Y, Hirotab S

Shionogi Pharmaceutical Company, 3-1-1 Futaba-cho, Toyonaka, Osaka 561-0825, Japan. yukihiko.kitamura@shionogi.co.jp

Signals through Kit receptor tyrosine kinase are essential for development of erythrocytes, melanocytes, germ cells, mast cells and interstitial cells of Cajal (ICCs). Mice and rats with a double gene dose of loss-of-function mutations of Kit show depletion of these cells. Although human homozygotes with loss-of-function mutations of Kit have not been reported, gain-of-function mutations of Kit result in development of tumors from mast cells, germ cells and ICCs in humans. The ICC tumors are called gastrointestinal stromal tumors (GISTs), and GISTs are a good target for the Kit inhibitor imatinib mesylate. The interrelationship between the type of Kit gain-of-function mutations and the therapeutic effect of imatinib mesylate has been well characterized in GISTs. Kit is interesting from both a biological and clinical view-point.

Published 7 December 2004 in Cell Mol Life Sci, 61(23): 2924-31.
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