How was EGFR discovered?
The discovery (in 1980) that the transforming protein of Rous sarcoma virus, v-src, has tyrosine-phosphorylation activity led to the discovery that EGFR is a tyrosine kinase acti- vated by binding EGF [1]. In 1984, the cDNA of human EGFR was isolated and characterized.
How many transmembrane helices are in EGFR?
24 residue
The transmembrane segment of EGFR is a 24 residue long single α-helix.
What is EGFR in Nsclc?
What is EGFR-positive cancer? EGFR (epidermal growth factor receptor) is a protein on cells that helps them grow. A mutation in the gene for EGFR can make it grow too much, which can cause cancer.
What is a Juxtamembrane domain?
The transmembrane (TM) and juxtamembrane (JM) regions of the ErbB family receptor tyrosine kinases connect the extracellular ligand-binding domain to the intracellular kinase domain. These results provide the basis of a mechanism for coupling ligand binding to kinase activation in the full-length receptor.
What is a Juxtamembrane region?
provide new insights into the EGFR activation process, highlighting the role of the juxtamembrane region, the cytoplasmic segment of the receptor that connects the transmembrane helix to the tyrosine kinase domain.
What is EGFR positive Nsclc?
EGFR-positive lung cancer represents about 10-15% of lung cancer in the United States and generally appears in adenocarcinoma subtype of non-small cell lung cancer. Patients with lung cancers with EGFR mutations tend to have minimal to no smoking history.
How is the catalytic activity of EGFR activated?
The catalytic activity of EGFR is switched on through allosteric activation of one kinase domain by another, and we show that if this is restricted to dimers, then sites in the tail that are proximal to the kinase domain are phosphorylated in only one subunit.
How does egegfr bind to intracellular ligands?
EGFR and one other member of the family (human epidermal growth factor receptor 4, HER4, also known as ErbB4) bind to specific ligands, and respond by activating their intracellular kinase domains.
What is the function of the epidermal growth factor receptor (EGFR)?
The epidermal growth factor receptor (EGFR) is activated by dimerization, but activation also generates higher-order multimers, whose nature and function are poorly understood.