Pseudokinases: Prospects for expanding the therapeutic targets armamentarium

Pseudokinases are pseudoenzyme variants of the protein kinase superfamily that primarily signal through non-catalytic mechanisms. The aberrant expression of pseudokinases correlates with the pathogenesis of many human diseases. However, pseudokinases remain relatively untapped as therapeutic targets due to difficulties associated with regulating their biological functions. Many protein kinase- and few pseudokinase-specific inhibitors have been reported to influence the non-catalytic functions of active kinases, giving the hope that pseudokinases can also be exploited for therapeutic purposes. This chapter presents the structural characteristics of selected pseudokinases, their known roles in human diseases, and the progress made toward developing pseudokinase-centric therapies.