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Human Epidermal Growth Factor receptor EGF R - Biotech, Pharma and Life Science Channel

09:53 EDT 18th June 2018 | BioPortfolio

The human epidermal growth factor receptor (HER) family members include EGFR (erbB1), HER2/neu (erbB2), HER3 (erbB3), and HER4 (erbB4) that are structurally related, and all except HER3 contain intracellular tyrosine kinase (tk) domain. All of the HER members, except HER2, bind to extracellular ligands

EGFR, a valid target in many epithelial malignancies, is a transmembrane protein with an extracellular ligand binding domain joined to an intracellular tyrosine kinase domain. Activation of EGFR induces a cascade of downstream signaling through several pathways, such as mitogenac tivated protein kinase (MAPK) and PI3-kinase / Akt/mTOR, resulting in cellular proliferation, differentiation, survival, motility, adhesion, and repair. EGFR is overexpressed or abnormally activated in several epithelial malignancies. Several antibodies targeting EGF-R and small molecules inhibiting the EGF-R tyrosine kinase have been approved and are used for treatment of colorectal cancer, squamous cell cancer of the head & neck or pancreatic cancer, respectively. EGF-R targeting therapeutics achieved 2008 sales of US$ 3.35 bln.

The pipeline of novel EGF-R targeting molecules is rather full and includes novel antibody as well as vaccine approaches and small molecules with a broader inhibition profile. At least six next generation antibodies against EGF-R are already in clinical development and more than ten biologics are preclinical R&D including dual target antibodies or vaccines. The small molecule pipeline is focused on dual EGF-R and Her2 as well as pan-Her tk inhibitors, but also includes multi-target EGF-R tk inhibitors.

Source; ReportLinker - Competitor Analysis: EGF-R Agonists and Antagonists

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Medical and Biotech [MESH] Definitions

A cell surface receptor involved in regulation of cell growth and differentiation. It is specific for EPIDERMAL GROWTH FACTOR and EGF related peptides including TRANSFORMING GROWTH FACTOR ALPHA, amphiregulin, and heparin-binding EGF-like growth factor. The binding of ligand to the receptor causes activation of its intrinsic tyrosine kinase activity and rapid internalization of the receptor-ligand complex into the cell.

A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. EPIDERMAL GROWTH FACTOR exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and epithelial cells.

A fibroblast growth factor that preferentially activates FIBROBLAST GROWTH FACTOR RECEPTOR 4. It was initially identified as an androgen-induced growth factor and plays a role in regulating growth of human BREAST NEOPLASMS and PROSTATIC NEOPLASMS.

A fibroblast growth factor receptor that is found in two isoforms. One receptor isoform is found in the MESENCHYME and is activated by FIBROBLAST GROWTH FACTOR 2. A second isoform of fibroblast growth factor receptor 2 is found mainly in EPITHELIAL CELLS and is activated by FIBROBLAST GROWTH FACTOR 7 and FIBROBLAST GROWTH FACTOR 10. Mutation of the gene for fibroblast growth factor receptor 2 can result in APERT SYNDROME.

A cell surface protein-tyrosine kinase receptor that is specific for NEUREGULINS. It has extensive homology to and can heterodimerize with the EGF Receptor (RECEPTOR, EPIDERMAL GROWTH FACTOR) and the erbB-2 receptor (RECEPTOR, ERBB-2). Overexpression of the erbB-3 receptor is associated with tumorigenesis.

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