EGF Receptor

EGF Receptor

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About EGF Receptor:

The epidermal growth factor receptor (EGFR, ErbB-1 or HER1 in humans) is a transmembrane protein. It is a receptor for members of the epidermal growth factor (EGF) family or extracellular protein ligands. It is a member of the ErbB family, which is a subfamily of four receptor tyrosine kinases. When EGFR expression or activity is affected by mutations, it can lead to cancer. Other diseases are associated with deficient signaling of the EGFR, including Alzheimer's, and overexpression is also related to a variety of tumour growths. EGFR-expressing tumours can be prevented from growing by interrupting EGFR signalling.

Epidermal Growth Factor Receptor Interactions
EGFR is activated by binding of its specific ligands, which include epidermal growth factor and transforming growth factor α. However, ErbB2 does not have a known direct activating ligand. It could be in an activated state constitutively or become active when heterodimerization with other family members (such as EGFR) occurs. EGFR transitions from an inactive monomeric form to active homodimer when it is activated by its growth factor ligands. EGFR can also pair with other members of the ErbB receptor family, which creates an activated heterodimer. EGFRs might also form in clusters, although the function of this is unclear. The activation of the EGF receptor is needed for the innate immune response in the human skin. It is also necessary for ductal development in the mammary glands.

EGFR Mechanism
The EGFR has various roles in human disease. Mutations causing EGFR overexpression have been linked to several different cancers, such as adenocarcinoma of the lung, glioblastoma and epithelian tumours of the head and neck. Mutations cause the EGFR to be constantly active, leading to uncontrolled cell division. Glioblastoma is often seen with a specific mutation, EGFRvIII. Inflammatory disease is another area linked to the EGFR, with incorrect signalling possibly related to skin conditions such as psoriasis and eczema. More research is required to define the roles that EGFR plays in these conditions.
In relation to wound healing and fibrosis, EGFR is an important factor in TGF-beta1 dependent fibroblast to myofibroblast differentiation. Progressive tissue fibrosis, which impairs tissue and organ function can be the result of persistence of myofibroblasts.

EGF Receptor Function
There are various ways EGFR is being used in medical applications. Anticancer therapeutics against EGFR (EGFR inhibitors) have been developed to lung cancer and colon cancer. A tyrosine kinase inhibitor has also been developed. There are therapeutic approaches that are designed to target the EGFR, such as monoclonal antibody inhibitors. Monoclonal antibodies block the extracellular ligand binding domain so signal molecules can't attach and activate the tyrosine kinase. It is also possible to use small molecules to inhibit EGFR tyrosine kinase so that EGFR can't activate itself.