Kinases still remain the most favorable members of the druggable genome, and there are an increasing number of kinase inhibitors approved by the FDA to treat a variety of cancers. Here, we summarize recent developments in targeting kinases and pseudokinases with some examples. Targeting the cell cycle machinery garnered significant clinical success, however, a large section of the kinome remains understudied. We also review recent developments in the understanding of pseudokinases and discuss approaches on how to effectively target in cancer.
Keywords: CDK4/6; MAPK; RAF; allosteric regulation; cancer; inhibitors; kinome; molecular switch.
Copyright © 2022 Riegel, Vijayarangakannan, Kechagioglou, Bogucka and Rajalingam.