Case Presentation - Department of Surgery at SUNY Downstate ...

Molecularly Targeted Therapy• Since activation of Kit plays a crucial role in thepathogenesis of GIST, inhibition of Kit would betherapeutic.• Imatinib (Gleevec)) is a competitive and relativelyselective antagonist of ATP binding that blocksthe ability of c-Kit cto transfer phosphate groupsfrom ATP to tyrosine residues on substrateproteins, which in turn interrupts c-kit cmediatedsignal transduction.