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  • Periodicals (Báo – Tạp chí)

  • METTL3 Inhibitors for Epitranscriptomic Modulation of Cellular Processes

    • Authors : 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...
  • Periodicals (Báo – Tạp chí)

  • Mammal ian Cel l Prol iferation Requires Noncatalytic Functions of O-GlcNAc Transferase

    • Authors : Levine, Zebulon G. (2020)

  • Developed approaches to replace endogenous OGT with separation-of-function variants to investigate the importance of OGT’s enzymatic activities for cell viability. Using genetic complementation, we found that OGT’s glycosyltransferase function is required for cell growth but its protease function is dispensable. We next used complementation to construct a cell line with degron-tagged wild-type OGT. When OGT was degraded to very low levels, cells stopped proliferating b...
  • Journal article

  • Peripheral blood mononuclear cells preferentially activate 11-oxygenated androgens

    • Authors : - (2020)

  • PBMCs generated 8-fold higher amounts of the active 11-oxygenated androgen 11- ketotestosterone than the classic androgen testosterone from their respective precursors. We identified the enzyme AKR1C3 as the major reductive 17β-hydroxysteroid dehydrogenase in PBMCs responsible for both conversions and found that within the PBMC compartment natural killer cells are the major site of AKRC13 expression and activity. Steroid 5α-reductase type 1 c...
  • Journal article

  • Human trans-editing enzyme displays tRNA acceptor stem specificity and relaxed amino acid selectivity

    • Authors : Vargas-Rodriguez, Oscar; Bakhtina, Marina; McGowan, Daniel (2020)

  • Accurate translation of genetic information into proteins is vital for cell sustainability. ProXp-ala prevents proteome-wide Pro-to-Ala mutations by hydrolyzing misacylated Ala-tRNAPro, which is synthesized by prolyl-tRNA synthetase (ProRS). Bacterial ProXp-ala was previously shown to combine a size-based exclusion mechanism with conformational and chemical selection for the recognition of the alanyl moiety, while tRNAPro is selected via recognition of tRNA acceptor stem elements...