Special Issue

Dear Colleagues,

The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues. Transferring γ-phosphate onto diverse substrates enables kinases to regulate key cellular functions. As many human diseases result from the mutation and overexpression of kinases, targeting of this enzyme class symbolizes an important strategy for drug development. Many of these kinases are associated with human cancer initiation and progression. The recent development of small-molecule kinase inhibitors for the treatment of diverse types of cancer has proven successful in clinical therapy. Kinase inhibitors represent targeted therapy resulting from the understanding of molecular genetics and molecular signaling pathways. This class of therapeutics represents a transformation from conventional chemotherapy to targeted cancer treatment. Nevertheless, many factors confound the clinical efficacy of these molecules. Specific tumor genetics, tumor microenvironment, drug resistance, and pharmacogenomics determine how useful a compound will be in the treatment of a given cancer. Due to the clinical importance of kinase inhibitors, multiple strategies are required to overcome resistance mechanisms and develop more effective targeted therapies. Moreover, kinase inhibitors are not only important for the treatment of cancer but also help us better understand the physiological roles of kinases. This Special Issue intends to serve as a compilation overviewing kinase signaling and kinase-targeted drug discovery and development in relation to oncology and highlighting the challenges and future potential for kinase-targeted cancer therapies.

Prof. Dr. Valentina De Falco
Guest Editor