Ontology highlight
ABSTRACT:
SUBMITTER: Prusevich P
PROVIDER: S-EPMC4076021 | biostudies-literature | 2014 Jun
REPOSITORIES: biostudies-literature
Prusevich Polina P Kalin Jay H JH Ming Shonoi A SA Basso Manuela M Givens Jeffrey J Li Xin X Li Xin X Hu Jianfei J Taylor Martin S MS Taylor Martin S MS Cieniewicz Anne M AM Hsiao Po-Yuan PY Huang Rong R Roberson Heather H Adejola Nkosi N Avery Lindsay B LB Casero Robert A RA Taverna Sean D SD Qian Jiang J Tackett Alan J AJ Ratan Rajiv R RR McDonald Oliver G OG Feinberg Andrew P AP Cole Philip A PA
ACS chemical biology 20140407 6
Lysine-specific demethylase 1 (LSD1) is an epigenetic enzyme that oxidatively cleaves methyl groups from monomethyl and dimethyl Lys4 of histone H3 (H3K4Me1, H3K4Me2) and can contribute to gene silencing. This study describes the design and synthesis of analogues of a monoamine oxidase antidepressant, phenelzine, and their LSD1 inhibitory properties. A novel phenelzine analogue (bizine) containing a phenyl-butyrylamide appendage was shown to be a potent LSD1 inhibitor in vitro and was selective ...[more]