OSMI-4-based PROTACs do not influence O-GlcNAc transferase and O-GlcNAcylation levels in cells

  • RSC Adv. 2025 Jul 18;15(31):25717-25723. doi: 10.1039/d5ra02801a.
Aleša Bricelj  1 ,  Doroteja Novak  1  2 ,  Lara Smrdel  1 ,  Christian Steinebach  3 ,  Izidor Sosič  1 ,  Marko Anderluh  1 ,  Martina Gobec  1
Affiliations
  • 1. Faculty of Pharmacy, University of Ljubljana Aškerčeva Cesta 7 SI-1000 Ljubljana Slovenia [email protected] [email protected].
  • 2. Department of Nuclear Medicine, University Medical Centre Ljubljana Zaloška 7 SI-1000 Ljubljana Slovenia.
  • 3. Pharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn 53121 Bonn Germany.
PMID: 40686638 DOI: 10.1039/d5ra02801a
Abstract

The O-GlcNAc transferase (OGT) inhibitors disclosed thus far are burdened with certain shortcomings. We have incorporated OSMI-4, a nanomolar OGT Inhibitor, into PROTACs. The prepared chimeras failed to induce effective OGT degradation or influence O-GlcNAcylation levels in MM.1S cells.

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