UGT1A3 Activators
UGT1A3 Activators are a class of chemicals that modulate the activity of the UGT1A3 protein by influencing the signaling pathways and transcription factors that control its expression. The activation process often involves the binding of these chemicals to specific nuclear receptors, which then translocate to the nucleus and interact with the promoter regions of the UGT1A3 gene, leading to an increase in mRNA transcription and subsequent enzyme synthesis. For instance, chemicals like phenobarbital and rifampicin activate nuclear receptors such as CAR and PXR, respectively. Upon activation, these receptors bind to DNA response elements that promote the transcription of the UGT1A3 gene, resulting in elevated levels of UGT1A3 enzyme within hepatocytes. The upregulation of UGT1A3 through these pathways indicates a dynamic regulation of enzyme activity in response to chemical signaling.
Further, compounds such as clofibrate and cholestyramine demonstrate the diverse mechanisms by which UGT1A3 can be activated. Clofibrate's engagement with PPARα leads to a cascade of transcriptional regulation that favors UGT1A3 expression. In contrast, cholestyramine indirectly stimulates UGT1A3 by reducing bile acid levels and consequently activating FXR, a known regulator of UGT enzymes. Other molecules, including retinoic acid and synthetic glucocorticoids like dexamethasone, also partake in the regulation of UGT1A3 by binding to their respective receptors and influencing gene expression. Collectively, these activators illustrate the multi-faceted nature of UGT1A3 regulation and underscore the importance of nuclear receptor-mediated pathways in modulating the activity of drug-metabolizing enzymes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $97.00 $328.00 $676.00 $1467.00 | 6 | |
Rifampicin acts as an agonist to the pregnane X receptor (PXR), which upon activation, binds to the UGT1A3 gene promoter regions. This binding enhances the transcription of the UGT1A3 gene, resulting in increased synthesis and activity of the UGT1A3 enzyme. | ||||||
Clofibrate | 637-07-0 | sc-200721 | 1 g | $33.00 | ||
Clofibrate activates peroxisome proliferator-activated receptors (PPARs), particularly PPARα. Activation of PPARα leads to an upregulation of UGT1A3 transcription through binding to peroxisome proliferator response elements (PPREs) in the UGT1A3 gene promoter. | ||||||
CHOLESTYRAMINE RESIN | 11041-12-6 | sc-507509 | 5 g | $210.00 | ||
Cholestyramine, a bile acid sequestrant, decreases intracellular bile acid pools, thereby activating nuclear farnesoid X receptor (FXR). FXR activation can lead to the upregulation of UGT1A3 expression, as FXR binds to response elements on the UGT1A3 promoter. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $66.00 $325.00 $587.00 $1018.00 | 28 | |
Retinoic acid, through its metabolite all-trans retinoic acid, activates retinoic acid receptors (RARs) which heterodimerize with retinoid X receptors (RXRs) and bind to retinoic acid response elements (RARE) in the UGT1A3 gene promoter, increasing UGT1A3 transcription. | ||||||
Omeprazole | 73590-58-6 | sc-202265 | 50 mg | $67.00 | 4 | |
Omeprazole induces UGT1A3 activity by activating nuclear receptors such as PXR. PXR, upon activation by omeprazole, binds to the UGT1A3 promoter region, enhancing the transcription and consequent activity of UGT1A3. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $91.00 $139.00 $374.00 | 36 | |
Dexamethasone, a synthetic glucocorticoid, activates the glucocorticoid receptor (GR). The activated GR can then bind to glucocorticoid response elements (GREs) in the UGT1A3 promoter region, potentially increasing UGT1A3 gene transcription and enzyme activity. | ||||||
Pioglitazone | 111025-46-8 | sc-202289 sc-202289A | 1 mg 5 mg | $55.00 $125.00 | 13 | |
Pioglitazone is a selective PPARγ agonist that can influence UGT enzymes by modulating the transcriptional activity of PPARγ, which may lead to altered UGT1A3 expression and activity, as PPARγ can bind to the promoter regions of certain UGT genes. | ||||||
L-3,3′,5-Triiodothyronine, free acid | 6893-02-3 | sc-204035 sc-204035A sc-204035B | 10 mg 100 mg 250 mg | $41.00 $77.00 $153.00 | ||
L-3,3′,5-Triiodothyronine, the active form of thyroid hormone, binds to thyroid hormone receptors which can heterodimerize with RXR and bind to thyroid hormone response elements (TREs) present in the promoter regions of some UGTs, potentially increasing the transcription and activity of UGT1A3. | ||||||
Rosiglitazone | 122320-73-4 | sc-202795 sc-202795A sc-202795C sc-202795D sc-202795B | 25 mg 100 mg 500 mg 1 g 5 g | $120.00 $326.00 $634.00 $947.00 $1259.00 | 38 | |
Rosiglitazone, a PPARγ agonist, modulates UGT expression by activating PPARγ, leading to altered transcription of UGT genes, including potentially UGT1A3, though the direct impact on UGT1A3 specifically may require further investigation. | ||||||
Silymarin group, mixture of isomers | 65666-07-1 | sc-301806 | 50 g | $325.00 | ||
Silymarin has been demonstrated to upregulate certain UGT enzymes, although the exact mechanism is not fully elucidated. It is suggested to modulate transcription factors that regulate UGT expression, which could result in increased UGT1A3 activity. | ||||||