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Leukaemia Biology Laboratory, Cancer Research UK Manchester Institute, The University of Manchester, Wilmslow Road, Manchester, M20 4BXIssue Date
2016-08
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LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase activity and has since been shown to have multiple essential roles in mammalian biology. Given its enzymatic activity and its high-level expression in many human malignancies, a significant recent focus has been the development of pharmacologic inhibitors. Here we summarize structural and biochemical knowledge of this important epigenetic regulator, with a particular emphasis on the functional and preclinical studies in oncology that have provided justification for the evaluation of tranylcypromine derivative LSD1 inhibitors in early phase clinical trials.Citation
LSD1: biologic roles and therapeutic targeting. 2016, 8 (8):1103-16 EpigenomicsJournal
EpigenomicsDOI
10.2217/epi-2016-0009PubMed ID
27479862Type
ArticleLanguage
enISSN
1750-192Xae974a485f413a2113503eed53cd6c53
10.2217/epi-2016-0009
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