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. Author manuscript; available in PMC: 2023 Jul 21.
Published in final edited form as: Cell. 2022 Jul 8;185(15):2657–2677. doi: 10.1016/j.cell.2022.06.016

Figure 3. Pharmacological inhibitors of glycosylation.

Figure 3.

(A) Protein O-GlcNAcylation can be blocked through the OGT inhibitors OSMI-1 and 5SGlcNAc, and the removal of O-GlcNAc can be targeted through the OGA inhibitor Thiamet G.

(B) N-glycosylation can be broadly inhibited using tunicamycin, which inhibits the attachment of GlcNAc-1-phosphate to dolichol phosphate (Dol-P) by GlcNAc-1-phosphate transferase (GPT).

(C) Glycans containing GlcNAc and GalNAc can be targeted using the glutamine mimics azaserine and DON, which target GFAT activity in hexosamine biosynthesis.

(D) “Look-alike” mimics of monosaccharides can inhibit specific modifications such as fucosylation (2F-Fuc and 2-deoxyGal) and sialylation (3F-Neu5Ac) or act as decoys for GTs in GAG biosynthesis (Naph-Xyl).