Structural basis for inhibition of the epidermal growth factor receptor by cetuximab.

By Shiqing Li, K. R. Schmitz, P. Jeffrey, J. Wiltzius, P. Kussie, K. Ferguson. Cancer Cell, 2005

1,128 citations recorded by the source corpus.

Subfields: Genetics, Oncology, Radiology, Nuclear Medicine and Imaging

View Paper: https://www.semanticscholar.org/paper/6518979e5adca0a8aa539aba73f2fe4133e8eb02

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In Oncology

1. P. Jänne
2. William Pao
3. Yigong Shi
4. J. Chmielecki
5. J. Engelman

In Radiology, Nuclear Medicine and Imaging

1. Yigong Shi

Citations in the corpus

• GC1118, an Anti-EGFR Antibody with a Distinct Binding Epitope and Superior Inhibitory Activity against High-Affinity EGFR Ligands (2015, methodology): “Our data and previous reports support the conclusion that both GC1118 and cetuximab maintain EGFR in the tethered conformation and block EGF binding to EGFR and subsequent EGFR dimerization (34).”
• Deep mutational scanning of an antibody against epidermal growth factor receptor using mammalian cell display and massively parallel pyrosequencing (2013, background): “4B).(11) Because humanization of murine antibodies retains the essential function of the murine CDRs in the context of human frameworks and crystal structures of humanized and parent antibodies show generally good retention of the murine CDR conformations,(12) the cetuximab Fab structure should serv”
• Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors (2016, positive): “We observe dramatic synergy of EAI045 with cetuximab, an antibody therapeutic that blocks EGFR dimerization 9,10 , rendering the kinase uniformly susceptible to the allosteric agent.”
• A glimpse of structural biology through X-ray crystallography. (2014, background): “Cetuximab, or Erbitux, which prevents both ligand binding and receptor dimerization through binding to domain III of the EGFR extracellular region (Li et al., 2005), has been approved for the treatment of metastatic colon cancer, NSCLC, and head and neck cancer.”
• Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer (2010, background): “As cetuximab interferes with EGFR ligand binding and subsequent receptor dimerization, EGFR mutations that confer ligand independence may abrogate the efficacy of this agen”
• Antibodies and cancer therapy: versatile platforms for cancer immunotherapy (2010, background): “and by preventing receptor dimerization, a crucial step for initiating EGFR-mediated signal transductio”