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. Author manuscript; available in PMC: 2011 Jan 18.
Published in final edited form as: J Am Soc Hypertens. 2009 Nov–Dec;3(6):374–387. doi: 10.1016/j.jash.2009.09.004

Table 1.

Pharmacological inhibitors that interfere with the O-GlcNAcylation process

Compound Name Chemical Formula Target Advantage Disadvantage References
[PUGNAc] graphic file with name nihms261242t1.jpg
 O-(2-acetamido-2-deoxy-D-glucopyranosylidene) amino-N-phenylcarbamate OGA Widely used; commercially available Exhibits nonspecific activity; including inhibition of β-hexosaminidase 40, 50, 51
[NAG-thiazoline] graphic file with name nihms261242t2.jpg
 1,2-dideoxy-2′-methyl-alpha-d-glucopyranoso[2,1-d]-Delta2′-thiazoline OGA Shows greater than 3000-fold selective inhibition of OGA over β-hexosaminidase Exhibits nonspecific activity; including inhibition of family 20 hexosaminidases 40, 52, 53
Nagstatin derivatives graphic file with name nihms261242t3.jpg OGA These inhibitors have been rationally designed using information about the enzyme active site Compounds are not commercially available 40, 54, 55
*[STZ] graphic file with name nihms261242t4.jpg
 Streptozotocin OGA — Very toxic Inhibitor due to its ability to generate reactive oxygen species 40, 47–49
[Alloxan] graphic file with name nihms261242t5.jpg
 2,4,5,6-tetraoxypyrimidine; 2,4,5,6-pyrimidinetetrone OGT Extensively used as an OGT inhibitor Multiple nonspecific effects, including inhibition of OGA, glucokinase and formation of superoxide radicals 45–47
[ST045849] graphic file with name nihms261242t6.jpg
 3-(2-adamantanylethyl)-2-[(4-chlorophenyl)azamethylene]-4-oxo-1,3-thiazaperhyd roine-6-carboxylic acid OGT — Few reports in the literature 44
[DON] graphic file with name nihms261242t7.jpg
 6-diazo-5-oxo-L-norleucine GFAT Well-established glutamine antagonist This compound inhibits various amidotransferases in a number of metabolic pathways that use glutamine as a substrate 25, 40, 57
[Azaserine] graphic file with name nihms261242t8.jpg
 O-diazoacetyl-L-serine GFAT The effects of this glutamine antagonist appear to be specific and nontoxic based on several criteria Like DON, it inhibits various amidotransferases in a number of metabolic pathways that use glutamine as a substrate 25, 40, 56

OGT, O-GlcNAc transferase or uridine diphospho-N-acetyl glucosamine; polypeptide β-N, acetylglucosaminyl transferase; OGA, O-GlcNAcase or β-N-acetylglucosaminidase; GFAT, glutamine:fructose-6-phosphate amidotransferase.

*

Streptozotocin (STZ) was suggested to be an inhibitor of OGA, via competitive inhibition.48 However, recent molecular studies using a galactose-linked STZ have indicated that OGA is not inhibited.49