Kinase Inhibitors in Targeted Cancer Therapy

Dear Colleagues,

The dysregulation of protein kinase activity plays a central role in the pathogenesis of several diseases. Thus, protein kinases have become one of the most important drug targets. They represent one of the largest gene families in eukaryotes, with more than 518 kinases in the human kinome, and are involved in cell division, cell death, transcription, and cell metabolism The success of imatinib, the first oral tyrosine kinase inhibitor approved by the Federal Drug Administration (FDA) in 2001 for chronic myelogenous leukemia, promoted the extensive use of kinase inhibitors (KIs) as anticancer agents.

KIs include small molecules as well as kinase-targeted antibodies and antibody conjugates. There are 62 FDA-approved small molecule kinase inhibitors, and about 180 are in clinical trials so far. However, despite the growing number of inhibitors, there are many limitations in their clinical use, such as the development of resistance and a low efficacy due to the activation of compensatory signaling pathways.

In this Special Issue entitled “Kinase Inhibitors as Targeted Cancer Therapy”, Pharmaceuticals welcomes original research articles and high-quality reviews focused on the investigation of novel small molecule-targeting protein kinases, as well as on structural and functional studies, increasing knowledge around these key enzymes.

Dr. Anna Carbone
Dr. Valeria Francesconi
Guest Editors

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