نتایج جستجو برای: فنوتیپ cyp3a
تعداد نتایج: 2450 فیلتر نتایج به سال:
سابقه و هدف: آنزیم سیتوکروم پی 3a از مهمترین آنزیمهای کبدی- روده ای است که بیش از 50 درصد داروهای موجود در بازار نیز عمدتاً به وسیله آن متابولیزه و از بدن حذف می شوند. فعالیت متابولیکی این آنزیم به فاکتورهای متعددی بستگی دارد. از آنجائیکه تا کنون مطالعه ای سیستماتیک از فعالیت آنزیم سیتوکروم پی 3aدر جمعیت ایرانی انجام نگرفته، این مطالعه به منظور بررسی فعالیت داخل بدنی آنزیم فوق با کمک میدازولام (...
Mechanism-based inactivation (MBI) can mediate adverse reactions and hepatotoxicity from drugs, which is a result of their conversion into highly reactive metabolites catalyzed by enzymes such as cytochrome P450 3A (CYP3A). In the present research, we optimized key interaction domain fluorophore with target protein to develop two-photon fluorescent probe for CYP3A that involved in metabolism mo...
سابقه و هدف: آنزیم سیتوکروم پی 3A از مهمترین آنزیمهای کبدی- روده ای است که بیش از 50 درصد داروهای موجود در بازار نیز عمدتاً به وسیله آن متابولیزه و از بدن حذف می شوند. فعالیت متابولیکی این آنزیم به فاکتورهای متعددی بستگی دارد. از آنجائیکه تا کنون مطالعه ای سیستماتیک از فعالیت آنزیم سیتوکروم پی 3Aدر جمعیت ایرانی انجام نگرفته، این مطالعه به منظور بررسی فعالیت داخل بدنی آنزیم فوق با کمک میدازولام ...
Human CYP3A is the most abundant P450 isozyme present in the human liver and small intestine, and metabolizes around 50% of medical drugs on the market. The human CYP3A subfamily comprises four members (CYP3A4, CYP3A5, CYP3A7, CYP3A43) encoded on human chromosome 7. However, transgenic mouse lines carrying the entire human CYP3A cluster have not been constructed because of limitations in conven...
Cytochrome P450 3A (CYP3A) enzymes constitute an important detoxification system that contributes to primary metabolism of more than half of all prescribed medications. To investigate the physiological and pharmacological roles of CYP3A, we generated Cyp3a-knockout (Cyp3a-/-) mice lacking all functional Cyp3a genes. Cyp3a-/- mice were viable, fertile, and without marked physiological abnormalit...
We investigated the interactions of the anticancer drug vinorelbine with drug efflux transporters and cytochrome P450 3A drug-metabolizing enzymes. Vinorelbine was transported by human multidrug-resistance associated protein (MRP) 2, and Mrp2 knockout mice displayed increased vinorelbine plasma exposure after oral administration, suggesting that Mrp2 limits the intestinal uptake of vinorelbine....
We determined whether the drug efflux protein P-glycoprotein (Pgp) could influence the extent of CYP3A-mediated metabolism of erythromycin, a widely used model substrate for CYP3A. We compared CYP3A metabolism of erythromycin (a Pgp substrate) using the erythromycin breath test in mice proficient and deficient of mdr1 drug transporters. We first injected mdr1(+/+) mice with [(14)C]N-methyl eryt...
We characterize a novel microsome system that forms high-molecular-mass (HMM) CYP3A, CYP2E1, and ubiquitin conjugates, but does not alter CYP4A or most other microsomal proteins. The formation of the HMM bands was observed in hepatic microsomes isolated from rats treated 1 week or more with high doses (50 mg/kg/day) of nicardipine, clotrimazole, or pregnenolone 16alpha-carbonitrile, but not mic...
We evaluated the distribution pattern of a specific xenobiotic metabolizing enzyme, cytochrome P450 3A (CYP3A) in the common brushtail possum (Trichosurus vulpecula). Western blot studies using CYP3A antibodies were used to compare CYP3A levels in the intestine, liver, kidney, brain, testes and adrenal gland in possums fed diets with and without a mixture of terpenes. Possums appear to produce ...
CYP3A4, the most abundant cytochrome P450 enzyme in the human liver and small intestine, is responsible for the metabolism of about 50% of all marketed drugs. Numerous pathophysiological factors, such as diabetes and obesity, were shown to affect CYP3A activity. Evidences suggest that drug disposition is altered in type 1 (T1D) and type 2 diabetes (T2D). The objective was to evaluate the effect...
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