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Nat Rev Drug Discov. 2018 May;17(5):353-377. doi: 10.1038/nrd.2018.21. Epub 2018 Mar 16.

Kinase inhibitors: the road ahead.

Author information

1
Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, United States.
2
Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, United States.

Abstract

Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been firmly demonstrated to play an essential role in virtually all major disease areas. Kinase inhibitor drug discovery programmes have recently broadened their focus to include an expanded range of kinase targets and therapeutic areas. In this Review, we provide an overview of the novel targets, biological processes and disease areas that kinase-targeting small molecules are being developed against, highlight the associated challenges and assess the strategies and technologies that are enabling efficient generation of highly optimized kinase inhibitors.

PMID:
29545548
DOI:
10.1038/nrd.2018.21

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