Cyp3a57 Activators
CYP3A57 is a crucial enzyme involved in drug metabolism, particularly in the liver, where it plays a vital role in the biotransformation of various xenobiotics. The gene encoding CYP3A57 is predicted to enable functions such as caffeine oxidase activity, iron ion binding activity, and monooxygenase activity, indicating its diverse role in cellular processes. Additionally, it is implicated in various diseases, including B-lymphoblastic leukemia/lymphoma, acute lymphoblastic leukemia, chronic myeloid leukemia, essential hypertension, and familial Mediterranean fever. The activation of CYP3A57 involves intricate molecular mechanisms influenced by specific chemicals. Rifampicin, for instance, activates CYP3A57 by binding to the pregnane X receptor (PXR), initiating a cascade that enhances the transcription and expression of the enzyme. Similarly, phenobarbital interacts with the constitutive androstane receptor (CAR), leading to increased levels of CYP3A57. Environmental pollutants like PBDE-47 and tetrachlorodibenzodioxin (TCDD) activate the enzyme through the aryl hydrocarbon receptor (AhR) pathway.
Other chemicals, such as 6-phenylhexan-3-one and omeprazole, directly stimulate CYP3A57 or modulate the nuclear receptor PXR, respectively, leading to enhanced enzymatic activity. Notably, quercetin acts indirectly by inhibiting CYP3A4, relieving its suppression on CYP3A57 and promoting increased gene expression. This diversity in activation mechanisms showcases the adaptability of CYP3A57 to respond to various chemical signals in the cellular environment. Understanding the complex regulatory network that governs CYP3A57 activation is crucial for deciphering its role in drug metabolism and disease pathogenesis. The identified chemicals provide valuable insights into the specific pathways and receptors involved in the activation of CYP3A57, paving the way for further research.
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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 | |
Induces CYP3A57 by activating the pregnane X receptor (PXR), a nuclear receptor. The binding of rifampicin to PXR leads to increased transcription of CYP3A57, enhancing its enzymatic activity and promoting drug metabolism in the liver. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $91.00 $139.00 $374.00 | 36 | |
Functions as a potent activator of CYP3A57 by activating the glucocorticoid receptor (GR). Upon binding, GR translocates into the nucleus and interacts with glucocorticoid response elements in the CYP3A57 promoter, leading to increased expression and enzyme activity. | ||||||
Efavirenz | 154598-52-4 | sc-207612 | 10 mg | $171.00 | 3 | |
Induces CYP3A57 expression through activation of the aryl hydrocarbon receptor (AhR) pathway. Binding of efavirenz to AhR triggers a cascade of events, including nuclear translocation and interaction with AhR response elements in the CYP3A57 gene, ultimately enhancing enzyme levels. | ||||||
BDE No 47 solution | 5436-43-1 | sc-233922 | 1 ml | $306.00 | ||
An environmental pollutant, BDE-47, activates CYP3A57 through the aryl hydrocarbon receptor (AhR) pathway. AhR activation leads to the transcriptional upregulation of CYP3A57, resulting in increased enzymatic activity and enhanced metabolism of xenobiotics. | ||||||
Omeprazole | 73590-58-6 | sc-202265 | 50 mg | $67.00 | 4 | |
Functions as a CYP3A57 activator by modulating the activity of the nuclear receptor PXR. Omeprazole induces PXR-dependent transcription of CYP3A57, leading to increased synthesis of the enzyme and subsequent enhancement of its catalytic activity in drug metabolism. | ||||||
1,4-Bis(2-methylstyryl)benzene | 13280-61-0 | sc-213523 sc-213523A | 5 g 25 g | $45.00 $170.00 | ||
Induces CYP3A57 through the activation of the nuclear receptor PXR. The binding of 1,4-Bis(2-methylstyryl)benzene to PXR triggers the upregulation of CYP3A57 gene expression, resulting in increased enzyme levels and enhanced metabolic activity in the biotransformation of xenobiotics. | ||||||
Fipronil | 120068-37-3 | sc-201546 sc-201546A | 100 mg 1 g | $62.00 $228.00 | ||
Activates CYP3A57 by modulating the constitutive androstane receptor (CAR). Fipronil-induced CAR activation leads to the enhanced transcription of CYP3A57, increasing enzyme levels and promoting the metabolism of various drugs and foreign compounds in the liver. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $110.00 $250.00 $936.00 $50.00 | 33 | |
Acts as an indirect CYP3A57 activator by inhibiting the enzyme CYP3A4, a known repressor of CYP3A57. Quercetin-mediated inhibition of CYP3A4 relieves the suppression on CYP3A57, allowing for increased expression and activity, ultimately promoting enhanced drug metabolism. | ||||||
Naringenin | 480-41-1 | sc-219338 | 25 g | $245.00 | 11 | |
Functions as a CYP3A57 activator by modulating the activity of the pregnane X receptor (PXR). Naringenin induces PXR-dependent transcription of CYP3A57, leading to increased synthesis of the enzyme and subsequent enhancement of its catalytic activity in drug metabolism. | ||||||