Ontology highlight
ABSTRACT:
SUBMITTER: Kumarasinghe IR
PROVIDER: S-EPMC5837957 | biostudies-literature | 2018 Mar
REPOSITORIES: biostudies-literature
Kumarasinghe Isuru R IR Woster Patrick M PM
European journal of medicinal chemistry 20180207
Lysine-specific demethylase 1 (LSD1) is a chromatin-remodeling enzyme that plays an important role in cancer. Over-expression of LSD1 decreases methylation at histone 3 lysine 4, and aberrantly silences tumor suppressor genes. Inhibitors of LSD1 have been designed as chemical probes and potential antitumor agents. We recently reported the cyclic peptide 9, which potently and reversibly inhibits LSD1 (IC<sub>50</sub> 2.1 μM; K<sub>i</sub> 385 nM). Systematic alanine mutagenesis of 9 revealed resi ...[more]