UGT1A10 Inhibitors
UGT1A10 inhibitors encompass a range of chemical entities that can decrease the enzymatic activity of UGT1A10, an enzyme integral to the glucuronidation pathway, which aids in metabolizing and detoxifying various compounds. These inhibitors operate by direct or indirect interactions with the enzyme or its associated pathways. Chemicals such as Atazanavir, Gemfibrozil, and Curcumin exhibit direct inhibition by competitively binding to the active site of UGT1A10, thus impeding substrate access and processing. This form of inhibition is characterized by a reversible binding to the same site as the enzyme's substrates, altering the rate at which glucuronidation occurs.
Other inhibitors, such as Crizotinib and Nicotine, exert their effects indirectly. Crizotinib, primarily known as a kinase inhibitor, can modify the phosphorylation state of proteins involved in the regulation of UGT1A10, affecting the enzyme's stability and catalytic activity. Nicotine impacts enzyme expression, leading to alterations in UGT1A10 activity without directly interacting with the enzyme's active site. Compounds like Piperine and Chrysin disrupt enzyme function through non-specific interactions that can cause conformational changes in UGT1A10 or act as competitive inhibitors. These molecules are essential for investigating the enzyme's role in metabolic processes and can aid in understanding the pharmacokinetics of various drugs. Collectively, UGT1A10 inhibitors play a pivotal role in modulating the enzyme's activity and the glucuronidation pathway at large.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Atazanavir | 198904-31-3 | sc-207305 | 5 mg | $286.00 | 7 | |
Atazanavir is a known inhibitor of UDP-glucuronosyltransferases (UGTs). It interacts with the enzyme's active site, leading to a decrease in UGT1A10 activity by directly competing with the substrates of the enzyme for binding. | ||||||
Gemfibrozil | 25812-30-0 | sc-204764 sc-204764A | 5 g 25 g | $65.00 $262.00 | 2 | |
Gemfibrozil inhibits UGT1A10 by binding to its active site. This binding interferes with the enzyme's ability to catalyze the glucuronidation process, effectively reducing the clearance of UGT1A10 substrates. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin has been shown to modulate the activity of various UGT enzymes. It binds to UGT1A10, reducing its ability to metabolize substrates through direct interaction with the enzyme's active site. | ||||||
Fluconazole | 86386-73-4 | sc-205698 sc-205698A | 500 mg 1 g | $53.00 $84.00 | 14 | |
Fluconazole inhibits UGT1A10 by competing with endogenous substrates for the active site of the enzyme. This leads to reduced glucuronidation activity and lower substrate metabolism. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $62.00 $260.00 | 21 | |
Ketoconazole decreases UGT1A10 activity through competitive inhibition. It binds to the same site as the natural substrates, thus preventing proper functioning of the enzyme. | ||||||
Piperine | 94-62-2 | sc-205809 sc-205809A | 5 g 25 g | $36.00 $143.00 | 3 | |
Piperine inhibits various UGTs including UGT1A10 by binding non-specifically to the protein, altering its conformation and reducing its enzymatic activity. | ||||||
Phenylbutazone | 50-33-9 | sc-204843 | 5 g | $31.00 | 1 | |
Phenylbutazone is a nonselective inhibitor of UGT enzymes. It competes with substrates for the active site of UGT1A10, leading to decreased glucuronidation. | ||||||
Ciprofibrate | 52214-84-3 | sc-204689 sc-204689A | 25 mg 100 mg | $57.00 $169.00 | ||
Ciprofibrate inhibits UGT1A10 activity by competitive inhibition, where it directly competes with the natural substrates for binding at the enzyme's active site. | ||||||
Andrographolide | 5508-58-7 | sc-205594 sc-205594A | 50 mg 100 mg | $15.00 $39.00 | 7 | |
Andrographolide can inhibit UGT1A10 by binding to the active site, competing with endogenous substrates, and reducing the metabolic capacity of the enzyme. | ||||||
Chrysin | 480-40-0 | sc-204686 | 1 g | $37.00 | 13 | |
Chrysin is a flavonoid that inhibits UGT1A10 by binding directly to the enzyme, thus hindering the glucuronidation of its natural substrates. | ||||||