Inhibitors of HER2/neu (erbB-2) signal transduction.
Signaling by the HER2 proto-oncogene product results in the activation of several biochemical pathways that in turn modulate the expression and function of molecules involved in cell proliferation and survival. It is well established that forced overexpression of HER2 results in transformation of nontumor cells, and that high levels of HER2 in tumors are associated with a more aggressive biological behavior. It is also clear that a subset of HER2-overexpressing tumors is dependent on HER2 function for proliferation and/or survival. Over the last few years, several elegant studies have dissected the biochemical mechanisms of HER2 signaling. This research has provided information about critical functional domains in HER2 that can be targeted with rational molecular approaches, some of which are already being implemented at the bedside. This report will focus on one of these anti-HER2 signaling strategies.
Arteaga
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CL
Department of Medicine, Vanderbilt University School of Medicine, 22nd Avenue S, 1956 TVC, Nashville, TN 37232-5536, USA.
Chinratanalab
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Carter
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D000818:Animals; D000911:Antibodies, Monoclonal / Q000627:therapeutic use; D061067:Antibodies, Monoclonal, Humanized; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002277:Carcinoma / Q000188:drug therapy / Q000235:genetics; D002986:Clinical Trials as Topic; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000627:therapeutic use*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D000077156:Gefitinib; D015972:Gene Expression Regulation, Neoplastic; D018734:Genes, erbB-2; D006801:Humans; D000090063:Proto-Oncogene Mas; D011799:Quinazolines; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000037:antagonists & inhibitors*; D015398:Signal Transduction / Q000187:drug effects*; D000068878:Trastuzumab
D000911:Antibodies, Monoclonal; D061067:Antibodies, Monoclonal, Humanized; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D066246:ErbB Receptors; D000077156:Gefitinib; D000090063:Proto-Oncogene Mas; D011799:Quinazolines; D018719:Erb-b2 Receptor Tyrosine Kinases; D000068878:Trastuzumab; C000715470:MAS1 protein, human