EGF receptor inhibition: attacks on multiple fronts.
The epidermal growth factor receptor (EGFR) drives tumor growth in a subset of human epithelial carcinomas. A crystallographic study by Li et al. in this issue of Cancer Cell provides the molecular basis for inhibition of EGFR by cetuximab (Erbitux), a monoclonal antibody that has been approved by the Food and Drug Administration as a therapeutic for advanced-stage colorectal cancers. Cetuximab targets one of the ligand binding domains of EGFR, thus preventing ligand activation of the receptor.
Hubbard
Stevan R
SR
Structural Biology Program, Skirball Institute of Biomolecular Medicine, New York University School of Medicine, New York, New York 10016, USA. hubbard@saturn.med.nyu.edu <hubbard@saturn.med.nyu.edu>
D000911:Antibodies, Monoclonal / Q000737:chemistry / Q000494:pharmacology*; D061067:Antibodies, Monoclonal, Humanized; D000936:Antigen-Antibody Complex / Q000737:chemistry; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D000068818:Cetuximab; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006801:Humans; D008958:Models, Molecular; D020836:Protein Structure, Quaternary; D017434:Protein Structure, Tertiary / Q000187:drug effects; D011940:Receptor Aggregation / Q000187:drug effects; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000737:chemistry; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000276:immunology; D000068878:Trastuzumab
D000911:Antibodies, Monoclonal; D061067:Antibodies, Monoclonal, Humanized; D000936:Antigen-Antibody Complex; D000970:Antineoplastic Agents; D000068818:Cetuximab; D066246:ErbB Receptors; D020794:Receptor Protein-Tyrosine Kinases; D018719:Erb-b2 Receptor Tyrosine Kinases; D000068878:Trastuzumab; C485206:pertuzumab