Oncogenic kinases

Blume-Jensen P, Hunter T (2001) Oncogenic kinase signalling. Nature 411 355-365... 

Blume-Jensen, P., and T. Hunter. Oncogenic kinase signaling. Nature. 411 355-365.2001. 

In 1966 Fischer and Krebs published their seminal work on protein phosphorylation and its regulatory function in cellular pathways.1 Since then, great strides have been made in our understanding of protein kinases, their functional roles in cellular processes, and their pathogenic roles in diseases. Bishop and Varmus received the 1989 Nobel Prize for their work on oncogenic kinases.2 In 2001, Nurse and Hunt were also awarded the Nobel Prize for their work in elucidating the role of cyclins and cyclin-dependent kinases in regulating cell cycles.3... 

Sunitinib (7),10 developed by Sugene/Pfizer, was approved in 2006 for the treatment of renal cell carcinoma (RCC). It is a VEGFR kinase inhibitor that slows down the angiogenesis of tumor endothelial cells, which provide nutrients and help tumor growth and metastasis. Sunitinib also blocks KIT, an oncogenic kinase that causes gastrointestinal stromal cell tumors. It was approved as a second-line anti-GSIT therapy for imatinib-resistant patients. 

Cragg MS, Harris C, Strasser A, Scott CL (2009) Unleashing the power of inhibitors of oncogenic kinases through BH3 mimetics. Nat Rev Cancer 9 321-326... 

Blame-Jensen, R, and Hunter, T. 2001. Oncogenic kinase pathway. Nature (London) 411 355-65. 

The prototype molecularly targeted therapeutic agent is imatinib, an inhibitor of the Bcr-Abl tyrosine kinase. This oncogenic kinase is produced by translocation of the Bcr locus on chromosome 9 to the c-Abl tyrosine kinase on chromosome 11, termed the Philadelphia chromosome because of its discovery in 1960 at the University of Pennsylvania School of Medicine by Peter Nowell and David Hungerford from the Institute for Cancer Research [9]. It was later demonstrated in 1973 by Janet Rowley that the Philadelphia translocation was responsible for a specific form of leukemia, chronic myelogenous leukemia (CML) [10], In 2001, imatinib was approved for treatment of CML patients, and produced remarkable results with more than 92% patients achieving 14-month progression-free survival on imatinib as a monotherapy. 

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