Epidermal growth-factor receptor

The epidermal growth factor receptor (EGFR) is a prototype of a family of tyrosine kinase receptors. The natural ligands for the EGFR are epidermal growth factor (EGF) and transforming growth factor (TGF)-a. In cancerous tissue, these 

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The epidermal growth factor receptor 2 (HER-2) is a protein found on the surface of cells. Heterodimerization of HER-2 activates the enzyme tyrosine kinase, triggering reactions that cause the cells to grow and multiply. HER-2 is found at abnormally high levels on the surface of many types of cancer cells, which may divide excessively. Antibodies targeting HER-2 (e.g., trastuzumab) are used as antineoplastic agents. 

Epidermal Growth Factor Receptor Family Growth Factors... 

Harari PM (2004) Epidermal growth factor receptor inhibition strategies in oncology. Endocr. Relat. Cancer 11 689-708... 

Epidermal Growth Factor (EGF) Receptor Family Epidermal Growth Factor Receptor 2 (ErbB2) Epidural (Space)... 

Mechanism of Palytoxin Action on the Epidermal Growth Factor Receptor... 

PETERSON G and BARNES s (1993) Genistein and hiochanin A inhibit the growth of hiunan prostate cancer cells but not epidermal growth factor receptor tyrosine autophosphorylation. Prostate. 22 (4) 335-45. 

Cetuximab is a human/mouse antibody that binds to the epidermal growth factor receptor to block its stimulation. The pharmacokinetics of cetuximab demonstrate a volume of distribution that approximates the vascular space and a terminal half-life of 70 to 100 hours. Cetuximab has shown clinical activity in the treatment of colorectal cancer. An acnelike rash may appear on the face and upper torso 1 to 3 weeks after the start of therapy. Other side effects include hypersensitivity reactions, interstitial lung disease, fever, malaise, diarrhea, abdominal pain, and nausea and vomiting. 

Erlotinib, whose pharmacology is not entirely understood, is believed to inhibit the intracellular phosphorylation of the epidermal growth factor receptor. Erlotonib is about 60% absorbed after oral administration food increases bioavailability to almost 100%. The time to peak concentrations is... 

Additional genes and protein receptors are believed to be important in colorectal tumorigenesis. Cyclooxygenase 2 (COX-2), which is induced in colorectal cancer cells, influences apoptosis and other cellular functions in colon cells, and overexpression of the epidermal growth factor receptor (EGFR), a transmembrane glycoprotein involved... 

More recently attempts to generate highly selective quiescent affinity labels have been made for a number of protease and kinase targets. As examples, inhibitors of the Rhinovirus 3C protease (Mathews et al 1999) and of the epidermal growth factor receptors (Boschelli, 2002), both incorporating Michael acceptors to covalently inactivate cysteine residues in their target enzymes (Lowry and Richardson, 1981 Figure 8.6), have entered human clinical trials for the treatment of rhinovirus infection and cancer, respectively. 

Meisner H, Daga A, Buxton J et al 1997 Interactions of Drosophila Cbl with epidermal growth factor receptors and role of Cbl in R7 photoreceptor cell development. Mol Cell Biol 17 2217-... 

Gadella, T. W. J. and Jovin, T. M. (1995). Oligomerization of epidermal growth-factor receptors on A431 cells studied by time-resolved fluorescence imaging microscopy—a stereochemical model for tyrosine kinase receptor activation. J. Cell Biol. 129, 1543-58. 

Wolff AC, Hammond MEH, Schwartz JN, et al. American Society of Clinical Oncology/College of American Pathologists Guideline Recommendations for Human Epidermal Growth Factor Receptor 2 Testing in Breast Cancer. Arch. Pathol. Lab. Med. 2007 131 18-43. 

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