A topical collection in Cancers (ISSN 2072-6694).
Protein phosphorylation is one of the most critical mechanisms for regulating various cellular functions. Consequently, protein kinase dysfunctions have been associated with the development of various types and subtypes of human cancers. Some examples include amplification and overexpression of the epidermal growth factor receptor (EGFR) and the ERBB2 receptor in lung and breast tumors, mutation of the BRAF oncogene in a wide range of human tumors, and the chromosomal translocation known as the Philadelphia chromosome, which results in ABL1 tyrosine kinase activation.
In the drug discovery field, despite early skepticism on the potential and selectivity of protein kinase inhibitors, enormous progress has been made. New classes of drugs, such as antibodies to receptors, and small-molecule inhibitors, were developed and tested in the clinics. The success of such drugs (e.g., imatinib and trastuzumab) encouraged development of new, second-generation drugs, which target protein kinases in cancer. Moreover, kinases have been shown to be invaluable diagnostic, prognostic, and predictive biomarkers for many types of cancers. In addition to protein kinases, lipid kinases, such as phosphatidylinositol-3-kinase (PI3K) and phosphatidylinositol-4-kinase (PI4K), have also been involved in the pathology of many tumors. In this issue of Cancers, “Kinases and Cancers”, experts are invited to contribute original research papers or review articles that will provide further insights on the various functions of kinases in cancers, and on their role as drug targets and biomarkers.
Dr. Jonas Cicenas
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