Kinase Inhibitors II

Dear Colleagues,

Since the discovery of protein phosphorylation as a post-translational modification in glycogen metabolism in the1960s, protein kinases (PK) and their opponents, phosphatases, have been crucial to many scientists. Approximately 2% of the human genome encodes for PKs, named the human “kinome”, consisting of 518 PKs and their splice variants. PKs typically use ATP for γ-phosphor-transfer reactions for OH-functions of serine, threonine, or tyrosine residues in proteins. In fact, the relatively simple attachment of a phosphate moiety induces critical conformational and functional changes of the substrate protein. Due to the powerful nature of protein modification involved in key cellular processes, such as signal transduction, cell cycle, metabolism, differentiation, and cell survival, PKs have to be strictly regulated in a physiological context. In contrast, their dysregulation leads to severe diseases, including cancer. In line with this notion, the first proto-oncogene c-SRC was identified as a non-receptor tyrosine kinase in 1978.

Today, PKs are validated and widely accepted targets for drug discovery, triggered significantly by the clinical success of imatinib in 2001. Thus far, more than 40 drugs have been FDA-approved and are on the market. The majority of compounds address tyrosine kinases, with their main therapeutical applications being cancer and inflammation. In addition to massive commercial drug discovery programs for the development of kinase inhibitors, academia has contributed a solid part to today´s knowledge on PK and their inhibitors. A wealth of biological studies towards the validation of PKs as drug targets, hit-compounds, lead structures, pharmacological tools, and ligand–protein complexes for the development of novel PK inhibitors are reported in literature. The topics cover various scientific areas, including molecular biology, biological and medicinal chemistry, and clinical applications.

This Special Issue of Molecules will focus on the exciting area of protein kinases and novel approaches in PK drug discovery.

Prof. Dr. Christian Peifer
Guest Editor

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