2015 Antineoplastics

Critical Facts IconCRITICAL FACTS V: Drugs that interfere with protein function
(if med school is a Minnesota forest with millions of trees,
these are the red pines)

  1. Signal transduction inhibitors (STIs) like IMATINIB, ERLOTINIB and GEFITINIB bind to the ATP-binding site of tyrosine kinases (NOT the substrate binding site).  STIs generally have fewer side effects than conventional therapies because they are targeted toward the specific defect of a particular cancer:  IMATINIB to bcr‑abl in CML, and ERLOTINIB and GEFITINIB to EGFR which is overexpressed in many epithelial-derived cancers.
Email: Dr. Janet Fitzakerley | ©2015 University of Minnesota Medical School Duluth | Last modified: 11-apr-15 9:39 AM