Kinase inhibitors: the road ahead

By F. Ferguson, Nathanael S. Gray. Nature reviews. Drug discovery, 2018

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Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials (2019, background): “No drugs have previously been reported to target CDK11, and inhibitors that are specific for single CDKs are difficult to discover due to the sequence similarity among these kinases (44).”
Integrated Proteogenomic Characterization of Clear Cell Renal Cell Carcinoma (2019, background): “Finally, we identified nine phospho-substrate events of eight kinases with inhibitors that are either FDAapproved or in clinical trials (Carles et al., 2018; Ferguson and Gray, 2018).”
Gastric cancer: a comprehensive review of current and future treatment strategies (2020, background): “For example, Imatinib, a BCR/ABL, c-KIT, and PDGFR potent inhibitor effective in treating chronic myelogenous leukemia (CML) and gastrointestinal stromal tumors (GISTs), in a phase II clinical study of metastatic gastric cancer showed no clinical efficacy or response [57].”
DOCKSTRING: Easy Molecular Docking Yields Better Benchmarks for Ligand Design (2021, neutral): “71 Our proposed objective anchors the LCK score to its median ( − 8.1) 2.4.”
PROteolysis TArgeting Chimeras (PROTACs) - Past, Present and Future (2019, background): “Targeting kinases with PROTACs enables modulation of both scaffolding and enzymatic functions as compared to occupancy driven pharmacology that only affects enzymatic function [81].”