LSD1: Biologic Roles and Therapeutic Targeting

Overview

Journal Epigenomics

Specialty Genetics

Date 2016 Aug 2

PMID 27479862

Citations 112

Authors

Alba Maiques-Diaz

Tim Cp Somervaille

Affiliations

Soon will be listed here.

Abstract

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.

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