Inhibition of Signaling by Overexpressed EGFR

Stable Identifier
Homo sapiens
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Recombinant monoclonal antibody Cetuximab acts as an antagonist of EGFR ligand binding, and is approved for the treatment of tumors that over-express wild-type EGFR receptor (Cunningham et al. 2004, Li et al. 2005, Burtness et al. 2005). Effective concentrations of covalent tyrosine kinase inhibitors (TKIs) inhibit wild-type EGFR, causing severe side effects (Zhou et al. 2009). Hence, covalent TKIs have not shown much promise in clinical trials (Reviewed by Pao and Chmielecki in 2010).
Literature References
PubMed ID Title Journal Year
15269313 Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer

Bleiberg, H, Humblet, Y, Mueser, M, Khayat, D, Chau, I, Cunningham, D, Bets, D, Verslype, C, Santoro, A, Harstrick, A, Siena, S, Van Cutsem, E

N Engl J Med 2004
20033049 Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

Zhou, W, Eck, MJ, Cortot, AB, Jänne, PA, Capelletti, M, Li, D, Padera, R, Engen, JR, Chen, L, Chirieac, L, Gray, NS, Iacob, RE, Wong, KK, Yun, CH, Ercan, D

Nature 2009
15837620 Structural basis for inhibition of the epidermal growth factor receptor by cetuximab

Ferguson, KM, Wiltzius, JJW, Schmitz, KR, Li, S, Kussie, P, Jeffrey, PD

Cancer Cell 2005
16314626 Phase III randomized trial of cisplatin plus placebo compared with cisplatin plus cetuximab in metastatic/recurrent head and neck cancer: an Eastern Cooperative Oncology Group study

Forastiere, AA, Burtness, B, Eastern Cooperative Oncology, Group, Flood, W, Goldwasser, MA, Mattar, B

J Clin Oncol 2005
20966921 Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

Chmielecki, J, Pao, W

Nat Rev Cancer 2010
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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