FucT-VII Inhibitors
Chemical inhibitors of FucT-VII provide functional obstruction to its enzymatic activity through various mechanisms. 2F-Peracetyl fucose, as a fucose analogue, directly competes with natural substrates at the active site of FucT-VII, thereby blocking the attachment of fucose to glycoproteins. This competitive inhibition is crucial as it ensures that FucT-VII is unable to catalyze its primary function of fucosylation.
Further inhibition of FucT-VII occurs through the modulation of the glycosylation processing pathway, which is vital for providing properly folded and mature glycoproteins, the substrates for FucT-VII. Tunicamycin impedes the initial steps of N-linked glycosylation, thus preventing the formation of suitable glycoprotein substrates for FucT-VII and indirectly reducing its fucosylation activity. Swainsonine and Kifunensine target mannosidase II and mannosidase I, respectively, leading to the accumulation of misprocessed glycans, which are not optimal substrates for FucT-VII, culminating in the downregulation of its activity. Deoxynojirimycin and Castanospermine inhibit glucosidases, which are responsible for trimming glucose residues in the N-glycan maturation process. The accumulation of misfolded glycoproteins due to this inhibition ensures that FucT-VII lacks the properly processed substrates it needs for fucosylation. Celgosivir, a prodrug of castanospermine, also inhibits these glucosidases, exerting a similar effect. 1-Deoxymannojirimycin and Deoxymannojirimycin both inhibit mannosidase enzymes, leading to the accumulation of improperly processed glycans that are not suitable for the activity of FucT-VII. NB-DNJ (Miglustat) also inhibits glucosidases, further ensuring the disruption of N-glycan processing and indirectly inhibiting the fucosyltransferase activity of FucT-VII by limiting the production of mature glycoprotein substrates necessary for its enzymatic function.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $30.00 $52.00 $122.00 $367.00 | 25 | |
Brefeldin A disrupts the structure of the Golgi apparatus, where FucT-VII operates, thereby preventing the enzyme from accessing its substrates and carrying out its fucosylation function. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $169.00 $299.00 | 66 | |
Tunicamycin inhibits the initial steps of N-linked glycosylation, which is crucial for the proper folding and function of glycoproteins that are substrates for FucT-VII. Without these substrates, FucT-VII is unable to perform its fucosylation activity. | ||||||
Swainsonine | 72741-87-8 | sc-201362 sc-201362C sc-201362A sc-201362D sc-201362B | 1 mg 2 mg 5 mg 10 mg 25 mg | $135.00 $246.00 $619.00 $799.00 $1796.00 | 6 | |
Swainsonine inhibits the processing of N-glycans by targeting mannosidase II, which in turn leads to the accumulation of misprocessed glycans, depriving FucT-VII of its properly folded glycoprotein substrates necessary for fucosylation. | ||||||
Kifunensine | 109944-15-2 | sc-201364 sc-201364A sc-201364B sc-201364C | 1 mg 5 mg 10 mg 100 mg | $132.00 $529.00 $1005.00 $6125.00 | 25 | |
Kifunensine inhibits mannosidase I in the N-glycan processing pathway. This results in the accumulation of high-mannose glycans, which are not optimal substrates for FucT-VII, thus indirectly inhibiting the enzyme's activity. | ||||||
Deoxynojirimycin | 19130-96-2 | sc-201369 sc-201369A | 1 mg 5 mg | $72.00 $142.00 | ||
Deoxynojirimycin inhibits glucosidases I and II, enzymes involved in the processing of N-glycans. This leads to improper glycan processing, thereby indirectly inhibiting FucT-VII by reducing the availability of mature glycoprotein substrates required for fucosylation. | ||||||
Castanospermine | 79831-76-8 | sc-201358 sc-201358A | 100 mg 500 mg | $180.00 $620.00 | 10 | |
Castanospermine is an inhibitor of glucosidases, which are responsible for the processing of N-glycans. By inhibiting these enzymes, the glycoproteins remain improperly processed and cannot be used efficiently as substrates by FucT-VII, thus functionally inhibiting the enzyme. | ||||||
Celgosivir | 121104-96-9 | sc-488385 sc-488385A sc-488385B | 5 mg 25 mg 100 mg | $525.00 $902.00 $2700.00 | ||
Celgosivir, a prodrug of castanospermine, inhibits glucosidases involved in the N-glycan maturation pathway, resulting in the misprocessing of glycans that serve as substrates for FucT-VII, thereby indirectly inhibiting the fucosylation process. | ||||||
Deoxymannojirimycin hydrochloride | 84444-90-6 | sc-201360 sc-201360A | 1 mg 5 mg | $93.00 $239.00 | 2 | |
Deoxymannojirimycin inhibits mannosidase I and II, leading to the accumulation of misprocessed glycans. This results in a reduced supply of functional glycoprotein substrates for FucT-VII, effectively inhibiting the enzyme's fucosylation capability. | ||||||