LSD1: biologic roles and therapeutic targeting

Alba Maiques-Diaz, Tim Cp Somervaille

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
Pages (from-to)1103-16
Number of pages14
Issue number8
Publication statusPublished - Aug 2016


  • Journal Article

Research Beacons, Institutes and Platforms

  • Manchester Cancer Research Centre


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