Cancer chemotherapy tyrosine kinase inhibitors

Erlotinib is an epidermal growth factor receptor inhibitor that inhibits intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor. It is indicated in the treatment of locally advanced or metastatic non-small-cell lung cancer after failure of at least 1 prior chemotherapy regimen. Erlotinib (Tarceva) is a human HER 1/EGER tyrosine kinase inhibitor with the following chemical formula A-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine. It is indicated in treatment of patients with locally advanced or metastatic non-small-cell lung cancer. 

Kloth JS, Pagani A, Verboom MC et al (2015) Incidence and relevance of QTc-interval prolongation caused by tyrosine kinase inhibitors. Br 1 Cancer 112 1011-1016 Korzeniowska K, Jankowski J, Cie lewicz A, JaWeeka A (2015) Current approcich for detection of sub-cfinical left ventricirlar dysfimetion associated with chemotherapy. Pharmacol Rep 67 1098-1102... 

Fry DW. Inhibition of the epidermal growth factor receptor family of tyrosine kinases as an approach to cancer chemotherapy progression from reversible to irreversible inhibitors. Pharmacol Ther 1999 82 207-218. 

Dr. Guy B. Faguet is particularly keen on imatinib mesylate, or Gleevec, against CML and is an advocate of the more fundamental gene therapy rather than the cell-toxic chemotherapy (e.g., Faguet, 2005, p. 46). He also notes it to be an inhibitor for tyrosine kinase. Interestingly, he skips the Warburg theory about cancer metabolism vs. normal cell metabolism and of enzymes and enzyme inhibitors. 

Protein kinase inhibitors (PKIs) provide a promising therapeutic strategy for cancer chemotherapy. Phosphorylation of proteins is a universal mechanism for the control of many cellular processes. The phosphorylation of proteins occurs when the y-phosphate group of ATP is transferred to either tyrosine or serine/threonine within proteins. One family of enzymes catalyses tyrosine phosphorylation and another serine/threonine phosphorylation. Tyrosine phosphorylation is up-regulated in tumour cells and thus provides a selective target for therapy. Although there are numerous protein kinase stmctures, they have some features in common and the active site of the enzyme consists... 

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