Cyp3a59 Activators
CYP3A59, a versatile enzyme predicted to enable caffeine oxidase activity, iron ion binding activity, and monooxygenase activity, plays a crucial role in oxidative demethylation and steroid metabolic processes. Its predicted cytoplasmic localization underscores its involvement in cellular metabolism. The human ortholog(s) of CYP3A59 are implicated in diverse diseases, including B-lymphoblastic leukemia/lymphoma, acute lymphoblastic leukemia, chronic myeloid leukemia, essential hypertension, and familial Mediterranean fever. Activation of CYP3A59 involves intricate molecular mechanisms influenced by specific chemicals. Cobalt chloride, for instance, mimics hypoxia conditions, stabilizing HIF-1α and promoting its translocation into the nucleus. This induces the expression of CYP3A59, regulated by HIF-1α binding to hypoxia response elements in its promoter, leading to increased enzymatic activity. Similarly, rifabutin activates CYP3A59 through the pregnane X receptor (PXR) pathway, showcasing the significance of PXR-mediated signaling in the regulation of CYP3A59 expression.
Dexamethasone functions as a potent activator by activating the glucocorticoid receptor (GR), which binds to response elements in the CYP3A59 promoter. Benzo[a]pyrene activates CYP3A59 through the aryl hydrocarbon receptor (AhR) pathway, illustrating the impact of AhR-mediated signaling on the enzyme. Metyrapone, by inhibiting cortisol synthesis, activates CYP3A59 through enhanced glucocorticoid receptor (GR) activation. Triclosan and amodiaquine activate CYP3A59 by modulating the constitutive androstane receptor (CAR) and nuclear receptor PXR, respectively. Quinidine activates the enzyme by modulating PXR, while diclofenac activates CYP3A59 through the aryl hydrocarbon receptor (AhR) pathway. β-Naphthoflavone induces CYP3A59 via AhR, and phenytoin acts as a direct activator by interacting with CAR. Bisphenol A activates CYP3A59 through the AhR pathway, emphasizing the diverse pathways involved in the enzyme's regulation. Understanding the complex regulatory network governing CYP3A59 activation is crucial for deciphering its role in cellular processes and disease pathogenesis. The identified chemicals provide valuable insights into the specific pathways and receptors influencing CYP3A59, paving the way for further research into its functional significance and potential implications in cellular homeostasis.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Cobalt(II) chloride | 7646-79-9 | sc-252623 sc-252623A | 5 g 100 g | $63.00 $173.00 | 7 | |
Activates CYP3A59 by mimicking hypoxia conditions. Cobalt chloride stabilizes HIF-1α, promoting its translocation into the nucleus. This induces the expression of CYP3A59, which is regulated by HIF-1α binding to hypoxia response elements in its promoter, leading to increased enzymatic activity. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $76.00 $82.00 $367.00 | 36 | |
Functions as a potent activator of CYP3A59 by activating the glucocorticoid receptor (GR). Upon binding, GR translocates into the nucleus and interacts with glucocorticoid response elements in the CYP3A59 promoter, leading to increased expression and enzyme activity. | ||||||
Benzo[a]pyrene | 50-32-8 | sc-257130 | 1 g | $439.00 | 4 | |
Activates CYP3A59 through the aryl hydrocarbon receptor (AhR) pathway. Benzo[a]pyrene binds to AhR, initiating its translocation into the nucleus and interaction with AhR response elements in the CYP3A59 promoter. This results in the upregulation of CYP3A59 gene expression and increased enzyme activity. | ||||||
Metyrapone | 54-36-4 | sc-200597 sc-200597A sc-200597B | 200 mg 500 mg 1 g | $25.00 $56.00 $86.00 | 4 | |
Functions as a CYP3A59 activator by inhibiting cortisol synthesis, leading to increased activation of the glucocorticoid receptor (GR). The activated GR then binds to glucocorticoid response elements in the CYP3A59 promoter, enhancing gene expression and subsequent enzymatic activity. | ||||||
Triclosan | 3380-34-5 | sc-220326 sc-220326A | 10 g 100 g | $138.00 $400.00 | ||
Activates CYP3A59 by modulating the constitutive androstane receptor (CAR). Triclosan-induced CAR activation leads to increased transcription of CYP3A59, elevating enzyme levels and promoting the metabolism of xenobiotics in the liver. | ||||||
Amodiaquine | 86-42-0 | sc-207282 | 10 mg | $342.00 | 1 | |
Induces CYP3A59 through the activation of the nuclear receptor PXR. Amodiaquine binding to PXR triggers a cascade of events, including nuclear translocation and interaction with PXR response elements in the CYP3A59 promoter, leading to increased expression and enzymatic activity. | ||||||
Quinidine | 56-54-2 | sc-212614 | 10 g | $102.00 | 3 | |
Functions as a CYP3A59 activator by modulating the activity of the pregnane X receptor (PXR). Quinidine induces PXR-dependent transcription of CYP3A59, leading to increased synthesis of the enzyme and subsequent enhancement of its catalytic activity in drug metabolism. | ||||||
Diclofenac acid | 15307-86-5 | sc-357332 sc-357332A | 5 g 25 g | $107.00 $292.00 | 5 | |
Activates CYP3A59 by modulating the aryl hydrocarbon receptor (AhR) pathway. Diclofenac binds to AhR, leading to its nuclear translocation and interaction with AhR response elements in the CYP3A59 promoter. This results in the upregulation of CYP3A59 gene expression and increased enzyme activity. | ||||||
β-Naphthoflavone | 6051-87-2 | sc-205597 sc-205597A sc-205597B sc-205597C | 1 g 5 g 25 g 100 g | $32.00 $126.00 $587.00 $1615.00 | 2 | |
Induces CYP3A59 through activation of the aryl hydrocarbon receptor (AhR) pathway. β-Naphthoflavone binding to AhR triggers the upregulation of CYP3A59 gene expression, leading to increased enzyme levels and enhanced metabolic activity in the biotransformation of xenobiotics. | ||||||
5,5-Diphenyl Hydantoin | 57-41-0 | sc-210385 | 5 g | $70.00 | ||
Acts as a direct activator of CYP3A59 by interacting with the constitutive androstane receptor (CAR). The binding of phenytoin to CAR triggers its translocation into the nucleus, leading to increased transcription of CYP3A59 and subsequent enhancement of enzyme levels and activity. | ||||||