Highly Galactosylated Anti-EGFR (Cetuximab) Antibody (CAT#: BioBet-GA-004ZP) Datasheet

EGFR

epidermal growth factor receptor

The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor. Binding of the protein to a ligand induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation. Mutations in this gene are associated with lung cancer.

EGFR; epidermal growth factor receptor; ERBB; HER1; mENA; ERBB1; PIG61; NISBD2; proto-oncogene c-ErbB-1; cell growth inhibiting protein 40; erb-b2 receptor tyrosine kinase 1; cell proliferation-inducing protein 61; receptor tyrosine-protein kinase erbB-1; avian erythroblastic leukemia viral (v-erb-b) oncogene homolog

Plasma membrane, Extracellular region or secreted Cytosol, Endosome, Nucleus, Golgi apparatus, ER.

Its related pathways are DAG and IP3 signaling and Association Between Physico-Chemical Features and Toxicity Associated Pathways.

1.Receptor tyrosine kinases bind to EGF family ligands and activate several signal cascades to transduce extracellular signals into appropriate cellular responses (PubMed: 2790960, PubMed: 10805725, PubMed: 27153536). Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG, and HBEGF/heparin binding EGF (PubMed: 2790960, PubMed: 7679104, PubMed: 8144591, PubMed: 9419975, PubMed :15611079, PubMed:12297049, PubMed:27153536, PubMed:20837704). Ligand binding triggers homo- and/or heterodimerization of the receptor and autophosphorylation of key cytoplasmic residues. Phosphorylated receptors absorb adaptor proteins like GRB2, which in turn activate complex downstream signaling cascades. Activate at least 4 major downstream signal cascades, including RAS-RAF-MEK-ERK, PI3 kinase-akt, PLCgamma-PKC and STATs modules (PubMed: 27153536). It is also possible to activate the nf-kpa-b signal cascade (PubMed: 11116146). It can also directly phosphorylate other proteins such as RGS16 to activate its GTPase activity, and possibly couple EGF receptor signals with G protein-coupled receptor signals (PubMed: 11602604). It also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/ -catenin (PubMed: 11483589). Through the interaction with CCDC88A/GIV, it positively regulates cell migration, retains EGFR on the cell membrane after ligand stimulation, promotes EGFR signaling, and triggers cell migration (PubMed:20462955). Play a role in improving learning and memory performance (through similarity). 2. Isoform 2 can act as an antagonist of EGF. 3. (Microbial infection) It acts as a receptor for hepatitis C virus (HCV) in liver cells and promotes its entry into cells. HCV entry is mediated by promoting the formation of the CD81-CLDN1 receptor complex which is essential for HCV entry and enhancing the membrane fusion of cells expressing HCV envelope glycoprotein.

Cancer antibody; Signaling Transduction antibody

Phosphorylation at Ser-695 is partial and occurs only if Thr-693 is phosphorylated. Phosphorylation at Thr-678 and Thr-693 by PRKD1 inhibits EGF-induced MAPK8/JNK1 activation. Dephosphorylation by PTPRJ prevents endocytosis and stabilizes the receptor at the plasma membrane. Autophosphorylation at Tyr-1197 is stimulated by methylation at Arg-1199 and enhances interaction with PTPN6. Autophosphorylation at Tyr-1092 and/or Tyr-1110 recruits STAT3. Dephosphorylated by PTPN1 and PTPN2. Monoubiquitinated and polyubiquitinated upon EGF stimulation; which does not affect tyrosine kinase activity or signaling capacity but may play a role in lysosomal targeting. Polyubiquitin linkage is mainly through 'Lys-63', but linkage through 'Lys-48', 'Lys-11' and 'Lys-29' also occurs. Deubiquitination by OTUD7B prevents degradation. Ubiquitinated by RNF115 and RNF126 (By similarity). Methylated. Methylation at Arg-1199 by PRMT5 stimulates phosphorylation at Tyr-1197.

Protein Based Therapies
Monoclonal antibody (mAb)

IgG1

Cetuximab

Human

Human

Cetuximab is a recombinant human / mouse chimeric epidermal growth factor receptor (EGFR) monoclonal antibody that binds to the epidermal growth factor receptor. It was approved by the US Food and Drug Administration in February 2004 for combination therapy for metastatic colorectal cancer expressing EGFR. Cetuximab is also approved as a single drug for the treatment of patients with metastatic colorectal cancer with EGFR expression intolerance.

Metastatic Colorectal Cancer (MCRC)
Metastatic Squamous Cell Carcinoma of the Head and Neck
Advanced squamous cell carcinoma of the head and neck

Cetuximab
Cétuximab
Cetuximabum

Cetuximab binds to epidermal growth factor receptor (EGFr) on both normal and tumor cells and is widely used to treat metastatic CRC. EGFr is overexpressed in many colorectal cancers. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and TGFα, thereby reducing their effect on cell growth and metastasis. Mouse model experiments show that cetuximab can target tumor cells through antibody-dependent cell-mediated cytotoxicity (ADCC) and increase antitumor activity.

Cetuximab is used in combination with irinotecan, and is suitable for the treatment of metastatic colorectal cancer expressing EGFR in patients who are difficult to treat with irinotecan-based chemotherapy. Cetuximab monotherapy can be used to treat metastatic colorectal cancer expressing EGFR in patients who are intolerant to irinotecan-based chemotherapy.