Tumor necrosis factor alpha increases P-glycoprotein expression in a BME-UV in vitro model of mammary epithelial cells. (1/31)

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Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants. (2/31)

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Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic. (3/31)

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In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5alpha-reductase inhibitor finasteride and the effects of coadministered ketoconazole. (4/31)

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Effects of strong CYP2D6 and 3A4 inhibitors, paroxetine and ketoconazole, on the pharmacokinetics and cardiovascular safety of tamsulosin. (5/31)

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Overexpression of CYP3A4, but not of CYP2D6, promotes hypoxic response and cell growth of Hep3B cells. (6/31)

Cytochrome P450s (P450s) contribute to carcinogenesis by activating procarcinogens and also metabolize anti-cancer drugs. The activity and protein levels of P450s are important in cancer risk and in cancer therapy. In this study, we found that overexpression of CYP3A4 induced growth of a human hepatoma cell line, Hep3B. Overexpression of CYP2D6, by comparison, decreased cell growth. An inhibitor of CYP3A4, ketoconazole, significantly suppressed the growth of Hep3B cells overexpressing CYP3A4, but an inhibitor of CYP2D6, quinidine, did not restore Hep3B cell growth to baseline levels. Overexpression of CYP3A4 increased the production of reactive oxygen species, but this was not the cause of the CYP3A4-induced growth. Previously, we showed that CYP3A4 can produce epoxyeicosatrienoic acids (EETs) from arachidonic acid. The CYP3A4-enhanced cell growth was attenuated by a putative EET receptor antagonist, 14,15-EEZE. CYP3A4 promoted progression of the cell cycle from the G1 to the S phase. CYP3A4 also induced a hypoxic response of Hep3B cells, detected as enhanced erythropoietin gene expression (a typical hypoxic response). The cell growth promoted by CYP3A4 was inhibited by PI3K inhibitor LY294002. These results suggest that CYP3A4 plays an important role in tumor progression, independent of the activation of carcinogens and metabolism of anti-cancer drugs.  (+info)

Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14alpha-demethylase (CYP51) from Leishmania infantum. (7/31)

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Effectiveness of chronic treatment with ketoconazole in a patient with diabetic Cushing's disease resistant to surgery. (8/31)

Without treatment, Cushing's disease has significant morbidity and mortality. Where a surgical approach may not be feasible, or is refused by the patient, medical therapy becomes the only option. In this case report, we discuss the effects of two years of ketoconazole treatment on diabetes regulation and insulin resistance in a patient reluctant to agree to surgery. A 62 year-old female patient with uncontrolled type 2 diabetes mellitus was investigated. Cushing's disease was confirmed by the results of high urine free cortisol level and dexamethasone suppression tests. We discuss the effects of two years of 600 mg/day ketoconazole treatment on diabetes regulation and insulin resistance in a patient with Cushing's disease reluctant to agree to surgery. This case report illustrates the beneficial long-term effects of 24 months of ketoconazole treatment on the clinical and laboratory findings and also on steroid and glucose metabolism.  (+info)