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  • OER000003027.pdf.jpg
  • Journal article

  • GFI1 cooperates with IKAROS/IKZF1 to activate gene expression in T-cell acute lymphoblastic leukemia

    • Tác giả : Sun, Wenxiang (2021)

  • Growth factor independence-1 (GFI1) is a transcriptional repressor and master regulator of normal and malignant hematopoiesis. Repression by GFI1 is attributable to recruitment of LSD1-containing protein complexes via its SNAG domain. However, the full complement of GFI1 partners in transcriptional control is not known. We show that in T-ALL cells, GFI1 and IKAROS are transcriptional partners that co-occupy regulatory regions of hallmark T cell development genes.&...
  • OER000000193.pdf.jpg
  • Periodicals (Báo – Tạp chí)

  • METTL3 Inhibitors for Epitranscriptomic Modulation of Cellular Processes

    • Tác giả : Moroz-Omori, Elena V; Hoàng, Đan Chi (2020)

  • The methylase METTL3 is the writer enzyme of the N6-methyladenosine (m6A) modification of RNA. Using a structure-based drug discovery approach, we identified a METTL3 inhibitor (UZH1a) with potency in a biochemical assay of 280 nM, while its enantiomer UZH1b is 100 times less active. The crystal structure of the complex of METTL3 with UZH1a illustrates the interactions that make it selective against protein methyltransferases. We observed a dose-dependen...