Recent advances in targeting protein kinases and pseudokinases in cancer biology

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY(2022)

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摘要
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.
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关键词
kinome, RAF, MAPK, CDK4/6, inhibitors, cancer, molecular switch, allosteric regulation
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