Table 3 The available inhibitors targeting OGT
Categories | Compound | IC50 (μM) | Advantages | Disadvantages | References |
|---|---|---|---|---|---|
Substrate and product analogs | Alloxan | 18 ± 1 | Cell-permeable | Potential off-target effects and general cellular toxicity | Konrad et al. (2002) |
|  | UDP- S -GlcNAc | 93 ± 15 | Sub-millimolar inhibitors | Lack of cell permeability | UniProt: a worldwide hub of protein knowledge (2019) |
|  | UDP- C-GlcNAc | 41 ± 7 | Sub-millimolar inhibitors | Lack of cell permeability, a weak hOGT inhibitor | Dorfmueller et al. (2011) |
|  | C-UDP | 9.0 ± 1.0 | Sub-millimolar inhibitors | Lack of cell permeability | Dorfmueller et al. (2011) |
| Â | UDP-5SGlcNAc | 5 | Cell-permeable | Affect N-glycosylation in cells and glycan synthesis outside the cells | Gloster et al. (2011) |
HTS-derived inhibitors | ST045849 | 53 ± 7 | Highly selective and cell-permeable | Potential off-target effects and cellular toxicity | Kamigaito et al. (2014) |
| Â | OSMI-1 | 2.7 | Cell-permeable, not alter cell surface N- or O-linked glycans, on-target activity | Â | Ortiz-Meoz et al. (2015) |
Bisubstrate inhibitor | goblin1 | 18 | Can synergize with goblin2 to enhance inhibition | Lack of cell permeability | Borodkin et al. (2014) |
| Â | goblin2 | 40 | Can synergize with goblin1 to enhance inhibition | Lack of cell permeability | Borodkin et al. (2014) |