EGFR

What is EGFR?

EGFR, also known as ErbB-1 or HER1, is an important transmembrane receptor of the epidermal growth factor receptors family. Besides EGFR, this family members also include HER2 (erbB2, NEU), HER3 (erbB3) and HER4 (erbB4). EGFR plays an important role in the physiological processes of cell growth, proliferation and differentiation. The abnormality of EGFR signal pathway is closely related to the occurrence of many diseases.

The Structure of EGFR

Human EGFR gene is located on chromosome 7p and encodes a single-chain transmembrane protein with a molecular weight of 134 kDa, which contains 1210 amino acid residues. The protein was further glycosylated at the 11th to 12th aspartic acid residues to form a mature EGFR, with a molecular weight of 170 kDa. EGFR is highly conserved in evolution, and the homology of EGFR between human and mouse is as high as 80%.

EGFR can be divided into three parts: extracellular region, transmembrane region and intracellular region.

The extracellular domain, the N-terminal of EGFR, contains 621 amino acid residues. This part contains the binding domain of the ligand EGF, which can mediate the binding of the ligand and EGFR.

The transmembrane region contains 23 amino acid residues, which is a hydrophobic region with helical structure.

The intracellular region consists of 542 amino acid residues, which can be divided into three parts: Proximal membrane region, tyrosine protein kinase region and C-terminal region.

The Expression of EGFR

EGFR is distributed on the surface of mammalian epithelial cells, fibroblasts, glial cells, keratinocytes and so on. EGFR is also expressed in a variety of human malignant tumor tissues and tumor cell lines.

Ligand of EGFR

EGFR ligand mainly include: Epidermal growth factor (EGF), transforming growth factor alpha (TGF-α), betacellulin (BTC), heparin-binding EGF (HBEGF) and epiregulin (EPR). EGF and TGF- α are the two most important ligands of EGFR.

The Function of EGFR

EGFR is located on the cell surface. After being activated by ligand, EGFR is dimerized and induces intrinsic protein kinase activation, and further activates downstream cellular signal pathways: Ras/Raf/MEK/ERK/MAPK pathway, PI3K/Akt (PKB) pathway and JAK/STAT pathway. Signal transduction ultimately mediates a series of processes such as cell differentiation, survival, migration, invasion, adhesion and cell damage repair.

EGFR is often overexpressed and out of control in human tumors, which is closely related to tumor cell proliferation, angiogenesis, tumor invasion, metastasis and inhibition of apoptosis.

Applications of EGFR in Treatment

The treatment methods targeting EGFR include monoclonal antibody drug intervention therapy and tyrosine kinase inhibitor drug intervention therapy.

Currently, there are 4 EGFR monoclonal antibodies approved for market worldwide, namely cetuximab, panizumab, neicastuzumab and neituzumab:

Cetuximab: trade name Aibituo. Indications are: metastatic head and neck cancer, non-metastatic head and neck cancer, metastatic colorectal cancer, non-small cell lung cancer and so on.

Necitumumab: is a monoclonal antibody. Necitumumab is used to treat certain types of non-small cell lung cancer, usually in combination with other cancer drugs.

Panitumumab: trade name Vectibix, is IgG2 monoclonal antibody, which has high affinity with EGFR. It can be used for the treatment of metastatic colorectal cancer after the failure of chemotherapy.

Nimotuzumab: is mainly used in combination with radiotherapy in the treatment of stage III/IV nasopharyngeal carcinoma with positive expression of epidermal growth factor receptor (EGFR).

Hot Products of EGFR

Recombinant Human Epidermal growth factor receptor(EGFR),partial (CSB-MP007479HU)

EGFR Antibodies

EGFR Antibodies for Homo sapiens (Human)

EGFR Antibodies for Drosophila melanogaster (Fruit fly)

EGFR Proteins

EGFR Proteins for Apis mellifera (Honeybee)

EGFR Proteins for Macaca mulatta (Rhesus macaque)

EGFR Proteins for Drosophila melanogaster (Fruit fly)

EGFR Proteins for Homo sapiens (Human)

EGFR Proteins for Gallus gallus (Chicken)

EGFR ELISA Kit

EGFR ELISA Kit for Mus musculus (Mouse)

EGFR ELISA Kit for Homo sapiens (Human)

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