作者: Katarzyna A. Ludwik , Deborah A. Lannigan
DOI: 10.1080/13543776.2016.1212839
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摘要: ABSTRACTIntroduction: The p90 ribosomal S6 kinases (RSK) are a family of Ser/Thr protein that downstream effectors MEK1/2-ERK1/2. Increased RSK activation is implicated in the etiology multiple pathologies, including numerous types cancers, cardiovascular disease, liver and lung fibrosis, infections.Areas covered: review summarizes patent scientific literature on small molecule modulators their potential use as therapeutics. patents were identified using World Intellectual Property Organization United States Patent Trademark Office databases. compounds described predominantly inhibitors, but activator also described. majority inhibitors not RSK-specific.Expert opinion: Based overwhelming evidence involved number diseases have high mortalities it seems surprising there no pharmacokinetic properties suitable for vivo use. MEK1/2 i...