Journal
SEMINARS IN CANCER BIOLOGY
Volume 48, Issue -, Pages 53-61Publisher
ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD
DOI: 10.1016/j.semcancer.2017.04.016
Keywords
RSK, cancer; Cell signalling; MAPK; Protein kinase; Phosphorylation; Proliferation
Categories
Funding
- Canadian Cancer Society Research Institute (CCSRI)
- Cancer Research Society (CRS)
- Human Frontier Science Program (HFSP)
- Canadian Institutes for Health Research (CIHR)
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The 90 kDa ribosomal S6 kinase (RSK) family is a group of Ser/Thr protein kinases (RSK1-4) that function downstream of the Ras/mitogen-activated protein kinase (MAPK) signalling pathway. RSK regulates many substrates involved in cell survival, growth, and proliferation, and as such, deregulated RSK activity has been associated with multiple cancer types. RSK expression and activity are dysregulated in several malignancies, including breast, prostate, and lung cancer, and available evidence suggests that RSK may be a promising cancer therapeutic target. Current limitations include the lack of RSK inhibitors with suitable pharmacokinetics and selectivity toward particular isoforms. This review briefly describes the current knowledge on RSK activation and function, with a particular emphasis on RSK-dependent mechanisms associated with tumorigenesis and pharmacological inhibition.
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