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Showing 1–3 of 3 results
Advanced filters: Author: Jonatan Caroli Clear advanced filters

  • Next generation precision lysine-specific histone demethylase 1A (LSD1) covalent inhibitors which selectively block LSD1 enzyme activity by forming a compact N-formyl-FAD adduct have been developed, but the mechanism of adduct formation was unclear. Here, the authors show that the covalent inhibitor-FAD adduct undergoes a Grob fragmentation and elucidate the structure-activity relationships that promote this transformation.

    • Amanda L. Waterbury
    • Jonatan Caroli
    • Brian B. Liau
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-14

  • Lee, Barone et al. engineered a mutant form of LSD1, Y391K, which renders the nucleosome demethylase activity of LSD1 insensitive to Lys14 acetylation of histone H3, providing a useful tool to illuminate the functional consequences of disconnecting histone modification crosstalk.

    • Kwangwoon Lee
    • Marco Barone
    • Philip A. Cole
    Research
    Nature Chemical Biology
    Volume: 21, P: 227-237

  • This study suggests a mechanism by which LSD1 controls DNA methylation in mouse ESCs, independently of its lysine demethylase activity. The demethylase-independent function of LSD1 regulates the DNMT1 and UHRF1 protein stability through interaction with USP7 and HDAC1.

    • Sandhya Malla
    • Kanchan Kumari
    • Francesca Aguilo
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-24