2. Academic Validation
  3. OSMI-4-based PROTACs do not influence O-GlcNAc transferase and O-GlcNAcylation levels in cells

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

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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