Targeting HER1/EGFR: a molecular approach to cancer therapy.

Arteaga C
Semin Oncol. 2003 30 (3 Suppl 7): 3-14

PMID: 12840796

The varying efficacy and toxicity of traditional cancer therapies has driven the development of novel target-based agents. Members of the HER (Human Epidermal Receptor) family, in particular epidermal growth factor receptor (HER1/EGFR), are attractive therapeutic targets because they are overexpressed and/or dysregulated in many solid tumors. Activation of HER1/EGFR mediated through ligand binding triggers a network of signaling processes that promote tumor cell proliferation, migration, adhesion, and angiogenesis, and decrease apoptosis. Therefore, inhibiting HER1/EGFR activity could effectively block downstream signaling events and, consequently, tumorigenesis. Various approaches are being investigated to target members of the HER family, particularly HER1/EGFR and HER2. At the forefront are monoclonal antibodies and small molecules that inhibit the receptor tyrosine kinase activity. Monoclonal antibodies have been developed that act against HER1/EGFR and HER2. Monoclonal antibodies block ligand binding and prevent ligand-induced activation. Tyrosine kinase inhibitors block receptor phosphorylation, preventing downstream signal transduction. Several HER1/EGFR-targeted agents are advanced in clinical development and attention is focused on optimizing their clinical use. While this process may prove challenging, it promises to be beneficial.

MeSH Terms (11)

Animals Antibodies, Monoclonal Antineoplastic Agents ErbB Receptors Humans Ligands Neoplasms Receptor, ErbB-2 Receptor, ErbB-3 Receptor, ErbB-4 Signal Transduction

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