Epidermal growth factor receptor

EGFREGF receptorEGFR inhibitorHER1ErbB1epidermal growth factor receptor (EGFR)EGFRvIIIepidermal growth factor (EGF) receptorepidermal growth factor receptor 2receptor, epidermal growth factor
The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands.wikipedia
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ErbB

EGFR familyEpidermal growth factor receptor familyEGF receptor family
The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4).
In humans, the family includes Her1 (EGFR, ErbB1), Her2 (Neu, ErbB2), Her3 (ErbB3), and Her4 (ErbB4).

Epidermal growth factor

EGFepidermal growth factor (EGF)epidermal growth factor-1
The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands. Epidermal growth factor receptor (EGFR) is a transmembrane protein that is activated by binding of its specific ligands, including epidermal growth factor and transforming growth factor α (TGFα) ErbB2 has no known direct activating ligand, and may be in an activated state constitutively or become active upon heterodimerization with other family members such as EGFR.
EGF binds to the epidermal growth factor receptor.

HER2/neu

HER2ERBB2HER-2
The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4).
HER2 is so named because it has a similar structure to human epidermal growth factor receptor, or HER1.

MAPK/ERK pathway

MAPK/ERKMAPKMAPK signaling pathway
These downstream signaling proteins initiate several signal transduction cascades, principally the MAPK, Akt and JNK pathways, leading to DNA synthesis and cell proliferation.
Receptor-linked tyrosine kinases such as the epidermal growth factor receptor (EGFR) are activated by extracellular ligands, such as epidermal growth factor (EGF).

Receptor (biochemistry)

receptorreceptorscellular receptors
The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands.

Adenocarcinoma of the lung

lung adenocarcinomaadenocarcinomapulmonary adenocarcinoma
Mutations that lead to EGFR overexpression (known as upregulation or amplification) have been associated with a number of cancers, including adenocarcinoma of the lung (40% of cases), anal cancers, glioblastoma (50%) and epithelian tumors of the head and neck (80-100%).
Common somatic mutations in lung adenocarcinoma affect many oncogenes and tumor suppressor genes, including TP53 (mutated in 46% of cases), EGFR (27%), KRAS (32%), KEAP1, STK11 and NF1.

Cetuximab

Erbitux
The identification of EGFR as an oncogene has led to the development of anticancer therapeutics directed against EGFR (called "EGFR inhibitors"), including gefitinib, erlotinib, afatinib, brigatinib and icotinib for lung cancer, and cetuximab for colon cancer.
Cetuximab is an epidermal growth factor receptor (EGFR) inhibitor used for the treatment of metastatic colorectal cancer, metastatic non-small cell lung cancer and head and neck cancer.

TGF alpha

transforming growth factor alphaTGF-αTGFA
Epidermal growth factor receptor (EGFR) is a transmembrane protein that is activated by binding of its specific ligands, including epidermal growth factor and transforming growth factor α (TGFα) ErbB2 has no known direct activating ligand, and may be in an activated state constitutively or become active upon heterodimerization with other family members such as EGFR. The EGFR is essential for ductal development of the mammary glands, and agonists of the EGFR such as amphiregulin, TGF-α, and heregulin induce both ductal and lobuloalveolar development even in the absence of estrogen and progesterone.
TGF-α is a transforming growth factor that is a ligand for the epidermal growth factor receptor, which activates a signaling pathway for cell proliferation, differentiation and development.

Gefitinib

Iressa
The identification of EGFR as an oncogene has led to the development of anticancer therapeutics directed against EGFR (called "EGFR inhibitors"), including gefitinib, erlotinib, afatinib, brigatinib and icotinib for lung cancer, and cetuximab for colon cancer. Gefitinib, erlotinib, brigatinib and lapatinib (mixed EGFR and ERBB2 inhibitor) are examples of small molecule kinase inhibitors.
Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.

ERBB3

HER3receptor, erbb-3erbB-3
The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4).
ErbB3 binding causes the allosteric activation of p110α, the lipid kinase subunit of PI3K, a function not found in either EGFR or ErbB2.

Afatinib

The identification of EGFR as an oncogene has led to the development of anticancer therapeutics directed against EGFR (called "EGFR inhibitors"), including gefitinib, erlotinib, afatinib, brigatinib and icotinib for lung cancer, and cetuximab for colon cancer.
It is mainly used to treat cases of NSCLC that harbour mutations in the epidermal growth factor receptor (EGFR) gene.

Osimertinib

AZD-9291AZD9291Tagrisso
More recently AstraZeneca has developed Osimertinib, a third generation tyrosine kinase inhibitor.
It is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor.

Zalutumumab

HuMax-EGFR
Other monoclonals in clinical development are zalutumumab, nimotuzumab, and matuzumab.
Zalutumumab (proposed trade name HuMax-EGFR) is a fully human IgG1 monoclonal antibody (mAb) directed towards the epidermal growth factor receptor (EGFR).

Erlotinib

TarcevaCP-358,774erlotinib hydrochloride
The identification of EGFR as an oncogene has led to the development of anticancer therapeutics directed against EGFR (called "EGFR inhibitors"), including gefitinib, erlotinib, afatinib, brigatinib and icotinib for lung cancer, and cetuximab for colon cancer. Gefitinib, erlotinib, brigatinib and lapatinib (mixed EGFR and ERBB2 inhibitor) are examples of small molecule kinase inhibitors.
It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).

Protein kinase

protein kinasestransmembranekinases
As a result, autophosphorylation of several tyrosine (Y) residues in the C-terminal domain of EGFR occurs.

Panitumumab

VectibixABX-EGF
Cetuximab and panitumumab are examples of monoclonal antibody inhibitors.
Panitumumab (INN), formerly ABX-EGF, is a fully human monoclonal antibody specific to the epidermal growth factor receptor (also known as EGF receptor, EGFR, ErbB-1 and HER1 in humans).

Myofibroblast

myofibroblastsmyofibroblasticmyofibroblastoid
EGFR has been shown to play a critical role in TGF-beta1 dependent fibroblast to myofibroblast differentiation.
Together with the co-activation of the non-canonical EGFR pathway, these events lead to upregulation of the ACTA2 gene and subsequent alpha smooth muscle actin protein production.

Matuzumab

Other monoclonals in clinical development are zalutumumab, nimotuzumab, and matuzumab.
It binds to the epidermal growth factor receptor (EGFR) with high affinity.

Mammary gland

mammaemammary glandsmammary
The EGFR is essential for ductal development of the mammary glands, and agonists of the EGFR such as amphiregulin, TGF-α, and heregulin induce both ductal and lobuloalveolar development even in the absence of estrogen and progesterone.
Important players include beta-1 integrin, epidermal growth factor receptor (EGFR), laminin-1/5, collagen-IV, matrix metalloproteinase(MMPs), heparan sulfate proteoglycans, and others.

Nimotuzumab

Theracim
Other monoclonals in clinical development are zalutumumab, nimotuzumab, and matuzumab.
Like cetuximab, nimotuzumab binds to the epidermal growth factor receptor (EGFR), a signalling protein that normally controls cell division.

Brigatinib

AP26113
The identification of EGFR as an oncogene has led to the development of anticancer therapeutics directed against EGFR (called "EGFR inhibitors"), including gefitinib, erlotinib, afatinib, brigatinib and icotinib for lung cancer, and cetuximab for colon cancer. Gefitinib, erlotinib, brigatinib and lapatinib (mixed EGFR and ERBB2 inhibitor) are examples of small molecule kinase inhibitors.
Brigatinib (marketed as Alunbrig) is a small-molecule targeted cancer therapy being developed by ARIAD Pharmaceuticals, Inc. Brigatinib acts as both a anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR) inhibitor.

Amphiregulin

AREG
The EGFR is essential for ductal development of the mammary glands, and agonists of the EGFR such as amphiregulin, TGF-α, and heregulin induce both ductal and lobuloalveolar development even in the absence of estrogen and progesterone.
This protein interacts with the Epidermal growth factor receptor (EGFR) to promote the growth of normal epithelial cells.

Glioblastoma

glioblastoma multiformeglioblastomasbrain cancer
Mutations that lead to EGFR overexpression (known as upregulation or amplification) have been associated with a number of cancers, including adenocarcinoma of the lung (40% of cases), anal cancers, glioblastoma (50%) and epithelian tumors of the head and neck (80-100%).

Lapatinib

GW572016TykerbTyverb
Gefitinib, erlotinib, brigatinib and lapatinib (mixed EGFR and ERBB2 inhibitor) are examples of small molecule kinase inhibitors.
It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways.

Veristrat

Some tests are aiming at predicting benefit from EGFR treatment, as Veristrat.
VeriStrat® is a test developed to evaluate patient prognosis and, additionally, predict benefit from cancer treatment by EGFR inhibitors.