Abstract
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.
MeSH terms
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Antibodies, Monoclonal / chemistry
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Antibodies, Monoclonal / pharmacology*
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Antibodies, Monoclonal, Humanized
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Antigen-Antibody Complex / chemistry
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cetuximab
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ErbB Receptors / antagonists & inhibitors*
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ErbB Receptors / chemistry
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Humans
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Models, Molecular
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Protein Structure, Quaternary
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Protein Structure, Tertiary / drug effects
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Receptor Aggregation / drug effects
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Receptor Protein-Tyrosine Kinases / antagonists & inhibitors
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Receptor Protein-Tyrosine Kinases / chemistry
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Receptor, ErbB-2 / antagonists & inhibitors
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Receptor, ErbB-2 / chemistry
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Receptor, ErbB-2 / immunology
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Trastuzumab
Substances
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Antibodies, Monoclonal
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Antibodies, Monoclonal, Humanized
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Antigen-Antibody Complex
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Antineoplastic Agents
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ErbB Receptors
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Receptor Protein-Tyrosine Kinases
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Receptor, ErbB-2
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pertuzumab
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Trastuzumab
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Cetuximab