Bisubstrate UDP–peptide conjugates as human O-GlcNAc transferase inhibitors

  title={Bisubstrate UDP–peptide conjugates as human O-GlcNAc transferase inhibitors},
  author={Vladimir S Borodkin and Marianne Schimpl and Mehmet Gundogdu and Karim Rafie and Helge C. Dorfmueller and David A Robinson and Daan M. F. vanAalten},
  booktitle={The Biochemical journal},
Inhibitors of OGT (O-GlcNAc transferase) are valuable tools to study the cell biology of protein O-GlcNAcylation. We report OGT bisubstrate-linked inhibitors (goblins) in which the acceptor serine in the peptide VTPVSTA is covalently linked to UDP, eliminating the GlcNAc pyranoside ring. Goblin1 co-crystallizes with OGT, revealing an ordered C₃ linker and retained substrate-binding modes, and binds the enzyme with micromolar affinity, inhibiting glycosyltransfer on to protein and peptide… CONTINUE READING
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