FIGURE 1 | EGFR and the mode of action of cetuximab.

From the following article:

Cetuximab

Peter Kirkpatrick, Joanne Graham & Mohamed Muhsin

Nature Reviews Drug Discovery 3, 549-550 (July 2004)

doi:10.1038/nrd1445

Cetuximab

The epidermal growth factor receptor (EGFR) is one of four members of the erbB family of receptor tyrosine kinases, which consist of an extracellular domain that can bind ligands, a transmembrane domain and an intracellular tyrosine kinase domain8. A simplified illustration of the EGFR signal transduction pathway is shown. Binding of a ligand to EGFR causes receptor dimerization (either with another EGFR monomer or with another member of the erbB family), leading to tyrosine kinase activation8. The resultant receptor autophosphorylation initiates signal-transduction cascades involved in cell proliferation and survival8. Cetuximab blocks binding of ligands to EGFR, thereby inhibiting receptor phosphorylation and downstream events. Agents that inhibit the tyrosine kinase activity of EGFR have also been developed and, of these, one has been approved by the FDA so far: gefitinib (Iressa; AstraZeneca), for the treatment of advanced non-small-cell lung cancer. MAPK, mitogen-activated protein kinase; TGF-alpha, transforming growth factor-alpha; TK, tyrosine kinase domain.

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