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Validated All-in-One™ qPCR Primer for CYP3A4(NM_017460.5) Search again
Product ID:
HQP055335
(click here to view gene annotation page)
Powered by BiozSpecies:
Human
Symbol:
Alias:
CP33, CP34, CYP3A, CYP3A3, CYPIIIA3, CYPIIIA4, HLP, NF-25, P450C3, P450PCN1, VDDR3
Gene Description:
cytochrome P450 family 3 subfamily A member 4
Target Gene Accession:
NM_017460.5(click here to view gene page)
Estimated Delivery:
Approximately 1-3 weeks, but may vary. Please email sales@genecopoeia.com or call 301-762-0888 to confirm ETA.
Important Note:
By default, qPCR primer pairs are designed to measure the expression level of the splice variant (accession number) you selected for this gene WITHOUT consideration of other possible variants of this gene. If this gene has multiple variants, and you would like to measure the expression levels of one particular variant, multiple variants, or all variants, please contact us for a custom service project at inquiry@genecopoeia.com.
Validated result:
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| A | B |
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Each All-in-One™ qPCR Primer is experimentally validated to yield a single dissociation curve peak and to generate a single amplification of the correct size for the targeted gene. A cDNA Pool, containing reverse transcript products of 8 different human tissue total RNA(Liver, Testis,Muscle,Thyroid,Brain,Spleen,Stomach,Small Intestine)),was used as the qPCR validation template. qPCR was performed using 0.2 µM primer with 2XAll-in-One™ qPCR Mix (Catalog#: QP001,QP002,QP004,QP005). Reactions were incubated for 10min. at 95°C, followed by 40 cycles of 95°C for 10 sec.; 60°C, 20 sec. and 72°C, 15sec. using Bio-Rad iQ5™ Instrument. At the end of the last cycle, temperature was increased from 72 to 95°C to produce a melting curve. Panel A: Validated Result for Amplification Curve; Panel B: Validated Result for Melting Curve. |
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Summary
This gene, CYP3A4, encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
Gene References into function
- There is a correlation between the CYP3A4*1B allele and early menarche, but this difference disappears when corrected for ethnicity and birth year.
- Comparative aflatoxin B(1) activation and cytotoxicity in human bronchial cells expressing cytochromes P450 1A2 and 3A4.
- Anti-cytochrome P450 autoantibodies, identified on the basis of their specific binding in immunoblots, are significantly increased among children on immunosuppressive drugs and in some cases are associated with drug toxicity and organ rejection.
- population screen on a panel of 101 human DNA samples of the 5' proximal regulatory region of the CYP3A4 gene using non-radioactive single strand conformation polymorphism (SSCP)
- presence of the ER6 motif of CYP3A4 mediates the high expression of CYP3A7 in subjects carrying CYP3A7*1C allele
- expression in hepatocytes by vitamin D receptor pathway
- xenobiotic inhibition of CYP3A4 promotor activity- role of the steroid and xenobiotic receptor
- An association uncorrected for stratification was observed between CYP3A4-V and prostate cancer in African Americans (P=0.007).
- Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor.
- Polymorphism has no functional significance and is not associated with risk of breast or ovarian cancer.
- change in vitamin D receptor-mediated mRNA induction in Caco-2 cells by altering cellular phosphorylation state
- Efavirenz is an inducer of liver CYP3A4 but did not appear to induce intestinal CYP3A4
- CYP3A4 is the only P450 of those tested that converts tamoxifen to alpha-hydroxytamoxifen and the only one that results in appreciable levels of irreversible binding of tamoxifen to DNA.
- description of CYP3A4 binding sites for diazepam and kinetic studies
- CYP3A4 expression in the endometrium of premenopausal women is comparable between the secretory and proliferative phases.
- Different alterations of cytochrome P450 3A4 isoform and its gene expression in livers of patients with chronic liver diseases. CYP3A4 isoenzyme and its activity declined among patients with hepatic cirrhosis.
- High activity CYP3A4, but not CYP3A5, which primarily metabolizes testosterone, showed a striking association with the onset of puberty.
- C/EBP alpha and HNF-3 gamma cooperatively regulate CYP3A4 expression in hepatic cells by a mechanism that probably involves chromatin remodeling.
- Down-regulation of cytochrome P450 CYP3A4 is associated with breast cancer CYP3A4
- "... enzymatic activity of CYP3A4 contributes to many adverse drug-drug interactions." "...results suggest that human CYP3A4 promoter functions in transgenic mice and this in vivo model can be useful to study transcriptional regulation of this gene"
- Incubation of racemic and nonracemic methadone with CYP3A4 revealed no stereoselectivity for the transformation to EDDP, whereas no EDDP formation was observed with CYP1A2.
- A stereoselectivity in the formation of 2'-hydroxymethaqualone and 2-hydroxymethaqualone from methaqualone was observed in urine and also in vitro using human liver microsomes and preparations containing the cytochrome P450 enzyme (CYP) CYP3A4 only.
- The CYP3A4*1B allele is associated with small cell lung cancers
- increased expression of CYP3A4 is associated with breast tumour
- inherited mutations in the CYP3A4 gene proximal promoter region could cause significant up-regulation of in vitro transcriptional activation by CYP3A4 xenobiotic inducers
- role in detoxification of lithocholic acid
- The catalytic activity of testosterone 6 beta-hydroxylation, membrane binding, and membrane insertion of CYP3A4 increase as a function of anionic phospholipid concentration.
- A novel enhancer of the CYP3A4 gene is identified, referred to as CLEM4, that confers the constitutive activation of CYP3A4 gene in the liver.
- three crystal structures of CYP3A4: unliganded, bound to the inhibitor metyrapone, and bound to the substrate progesterone
- cyp3A4 X-ray crystallographic structure, to 2.05-A resolution
- "The available data indicate that St. John's wort is a potent inducer of CYP 3A4..." See page 262.
- cytochrome P4503A4 is 46% homologous with CYP2C5 and they are shown to have active sites which accept the same substrates
- No difference in CYP3A4 activity in kidney transplant patients taking either FK506 or Rapamyicn and healthy controls.
- This protein interacts with viral X protein in vivo by yeast two-hybrid system, and may contribute to the development of hepatocellular carcinoma.
- certain properties of CYP3A4 are masked by expression of the protein in insect cells and reinforce the concept that the enzyme possesses multiple binding domains
- P. 92:"In this study...primary human hepatocytes ... were treated with dimethylsulfoxide." "In our experiments CYP3A4 was induced in a concentration-dependent manner by DMSO."
- presence of two functional FXR recognition sites located in a 345-bp element within the 5'-flanking region of CYP3A4
- results present a new insight into the individualized CYP3A4-dependent pharmacotherapy and the importance of expression imbalance to human phenotypic diversity
- found a significant increase in the frequency of rearrangements during chemotherapy only in patients homozygous for the wild type CYP3A4*1A allele, providing a direct link between CYP3A4 genotype and susceptibility to drug genotoxicity
- CYP3A4 is both a 24- and 25-hydroxylase for vitamin D(2), 1 alpha OHD(2), and 1 alpha OHD(3).
- CYP3A4 alters UDPG glucuroyosyltransgferase regioselectivity so that the ratio of morphine activation/detoxication is increased.
- Data show that CYP3A4 can metabolise lithocholic acid into 3-dehydrolithocholic acid, a potent activator of receptors which are known to regulate the expression of CYP3A4.
- Our results demonstrate that the CYP3A5*1 allele, previously reported as a marker for CYP3A5 expression in human kidney, is associated with increased risk for BEN, while CYP3A4*1B and CYP2D6 genotypes do not significantly modify the risk for the disease.
- findings demonstrated age-related differences in the body's capacity to metabolize steroids and xenobiotic compounds and suggest an important role for SXR and its target genes, CYP3A4 and MDR1 in this process
- transcriptional activation of ZNF185 and CYP3A4 is mediated by direct association of BRG1 with their promoters and a decreased level of ZNF185 is a common feature of lung tumours
- Rrutaecarpine and limonin are mechanism-based inhibitors of CYP3A4 from liver microsomes.
- The influence of CYP3A4 inhibition on the pharmacokinetics of ARIPIPRAZOLE was not considered to be clinically significant.
- A new distal enhancer site is identified in CYP3A4 gene where C/EBPbeta-LAP (liver activating protein) binds and activates transcription, whereas the truncated form, C/EBPbeta-liver inhibitory protein, antagonizes LAP activity and causes gene repression.
- Transgenic(Tg)-CYP3A4 females were deficient in lactation, with markedly lower pup survival. Mammary glands of Tg-CYP3A4 lactating mothers had underdeveloped alveoli with low milk content.
- CYO3A4 not associated with susceptibility to tardive dyskinesia in chronic schizophrenia subjects
- the CYP3A4 gene have no contribution to the early onset of puberty in Chinese girls, but are related in some way with the puberty development in Chinese girls.
- genotyping tests for defective CYP3A4/CYP3A5 haplotypes will be necessary to understand the variations in the metabolism and clinical toxicity of a wide variety of clinical drugs--REVIEW
- Fast and reliable in silico methods predicting CYP inhibition from calculated molecular properties are an important tool which can be applied to assess value of inhibitors.
- Low/null activity polymorphisms of this enzyme is not with the risk of developing aplastic anemia in Caucasian patients.
- Results provide evidence for a cross-talk between CYP3A4 and aryl hydrocarbon receptor, and show that conclusions drawn from experiments carried out in cell lines may lead to erroneous in vivo predictions in man.
- CYP3A5*1/*3 polymorphisms are associated with tacrolimus pharmacokinetics and dose requirements in renal transplant recipients.
- The P450 3A4 binding process is more complex than a two-state system, and the overlap of rates of some of the events with subsequent steps is proposed to underlie the observed cooperativity
- The CYP3A4-mediated first-pass sulfoxidation of (R)- and (S)-lansoprazole were not influenced by grapefruit juice. In addition, stereoselectivity of the intestinal CYP3A4-catalysed sulfoxidation of (R)- and (S)-lansoprazole was not observed.
- NF-kappaB activation by lipopolysaccharide and tumor necrosis factor-alpha plays a pivotal role in the suppression of cyp3a4 through interactions of NF-kappaB with the PXR.retinoid X receptor (RXR) complex
- IVS10+12G>A polymorphism of CYP3A4 gene modulates platelet activation in patients treated with clopidogrel and may therefore contribute to clopidogrel response variability.
- analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5
- Inhibitory effect of tofisopam was lower than that of ketoconazole (potent CYP3A4 inhibitor) with an order of magnitude.
- The constructs, CYP2C9/BMR, CYP2C19/BMR and CYP3A4/BMR are well expressed in Escherichia coli as holo proteins.
- Crystal structures of human CYP3A4 in complex with two well characterized drugs: ketoconazole and erythromycin were reported.
- novel SNPs detected in the CYP3A4 gene suggest that the Chinese population has different patterns of allele frequency compared with other populations
- Expression of Thy1 decreased in differentiated ADSC and BMSC. Expression of albumin, CYP2E1, and CYP3A4 increased in differentiated BMSC and ADSC. Hepatic gene activation may involve increased C/EBPbeta and HNF4alpha.
- the results suggest that 2-p-toluidinylnaphthalene-6-sulfonic acid binds in the active site of CYP3A4, while the first equivalent of testosterone binds at a distant allosteric effector site.
- The effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine dose adjusted trough blood concentration during the early period after renal transplantation in Chinese patients is reported.
- Formula feeding appears to accelerate maturation of caffeine and DM metabolism by increasing the activity of CYP1A2 and CYP3A4, respectively.
- The effects of hyperforin and four oxidized analogues from H. perforatum on the activity of CYP3A4 in vitro are reported.
- This report is the first demonstration that thalassemia major is associated with an alteration of CYP2E1 and CYP3A4 activities; this could modify the sensitivity of thalassemia patients to the toxic or therapeutic effects of drugs.
- substantial similarities in expression and gene regulation between marmoset CYP3A21 and human CYP3A4
- The interactions of P450 3A4 with several structurally diverse inhibitors were investigated using both kinetic and thermodynamic approaches to resolve the steps involved in binding of these ligands
- Administration of Curcuma drugs might inhibit the catalytic activity of intestinal CYP3A4
- PXR plays a critical role in the regulation of P450 3A4 expression in osteosarcoma and that its expression and activation in these tumors may influence the effect of chemotherapeutic agents on the induction of target genes implicated in drug resistance
- there is no significant association between polymorphisms in CYP3A4, CYP3A5, MDR1, GSTM1 and GSTT1 and outcome either after treatment with induction chemotherapy or after high-dose therapy for multiple myeloma
- identification of metabolites produced by CYP3A4 biotransformation of praziquantel
- Differences exist in protein levels of certain CYPs in non-malignant esophageal tissue (e.g. CYP2C8, CYP3A4, CYP3A5, and CYP2E1) between SCC patients and healthy subjects and may contribute to the development of squamous-cell carcinoma in the esophagus.
- Valproic acid up-regulates CYP3A4 by activating CAR and/or PXR pathways and synergistically augments the effect of rifampicin in transactivation of CYP3A4.
- An inhibition assay was developed and validated for CYP3A4 in liver microsomes.
- not only the Q158K variant found in Chinese, but also in native pregnane X receptor variants in other ethnic groups (D163G, A370T, R381W, and I403V) affect CYP3A4 induction by altering steroid receptor coactivator-1 recruitment
- CYP3A4 has been demonstrated to be involved in the metabolism of voriconoazole.
- A subgroup of breast cancer patients who carry the CYP3A4*1B allele and take tamoxifen may be at increased risk of developing endometrial cancer.
- CYP3A4 plays a major role in TPA023 metabolism, and CYP3A5 may also contribute at higher concentrations of the compound.
- associations between the hepatic CYP3A4 protein expression level, as well as its enzymatic activity and genetic polymorphisms from two regions within the CYP3A gene cluster
- Determine extent of CYP3A4 inhibition by itraconazole and its metabolites.
- Significant herb-drug interactions may result from the concomitant ingestion of goldenseal and CYP3A substrates.
- There was an association between race and CYP3A4 polymorphisms with 75% of European Americans having the Wild Type compared to only 25% of African American men. There was no association between CYP3A4 classification or race and survival or progression.
- analysis of CYP3A4 activity in the presence of organic cosolvents, ionic liquids, or water-immiscible organic solvents
- Tamoxifen activated the SXR-mediated transcription through CYP3A4 and MDR1 promoters in a ligand- and receptor concentration-dependent manner.
- Transcription factor binding to a putative double E-box motif represses CYP3A4 expression in lung cells.
- mechanisms of interactions of CYP3A4 with 1-pyrenebutanol & testosterone involve an effector-induced transition that displaces a system of conformational equilibria in the enzyme toward the state(s) with decreased solvent accessibility.
- Differences in CYP3A41G genotype distribution and haplotypes of CYP3A4, CYP3A5 and CYP3A7 in 3 different Chinese ethnic groups; close linkage is demonstrated
- genotype and allele frequencies of genetic polymorphisms of CYP3A4 among Malaysian subjects
- Common polymorphisms on CYP3A4 and CYP3A5 genes do not modify the risk of developing digestive cancers in Western Europe.
- Tramadol disposition can be used as a probe to assess CYP2D6/CYP3A4 ontogeny in the first months of life.
- inhibited by Sophora flavescens
- CYP3A4*18B genotype affects cyclosporine pharmacokinetics.
- A high CYP3A4 tumoral expression could be useful to predict poor response to the standard PTCL chemotherapy.
- Except for the daily tacrolimus dose (P = 0.025) no significant differences were observed for carriers of the CYP3A4*1B variant allele.
- The recombinant fused enzymes CYP3A4-truncated (t)-P450 reductase-t-b5 (3RB) and CYP3A4-t-b5-t-P450 reductase (3BR) in yeast microsomes showed a higher specific activity in 6beta-hydroxylation of testosterone than did the reconstitution premixes.
- CYP2C19 and CYP3A4 gene polymorphisms have a role in clopidogrel responsiveness in healthy subjects
- The heterozygous CYP3A4(*)1/(*)18 does not appear to cause a significant change of midazolam disposition in vivo; however, the clinical relevance of CYP3A4(*)18/(*)18 remains to be evaluated.
- CYP3A4 enhancers co-ordinate the proximal promoter in responding similarly to the pregnane X receptor but differentially to hepatocyte nuclear factor-4alpha
- Frmation of the major vicriviroc metabolites in human liver microsomes is primarily mediated via CYP3A4. CYP2C9 and CYP3A5 play a minor rolesin the biotransformation.
- CYP3A4*1B polymorphism is not associated with prostate cancer risk
- CYP3A4 is the main CYP3A expressed in the gastrointestinal tract.
- Multivariable logistic regression analysis with adjustment for age and sex also revealed that the 13989-->G (Ile118Val) polymorphism of CYP3A4 was significantly (P=0.00002) associated with the prevalence of type 2 diabetes mellitus.
- concomitant treatment with a CYP3A4 inhibitor and a CCB increases the risk of an ADR by 53%, compared with CCB monotherapy.
- CYP3A4*1B was significantly associated with being infected with HIV (p < 0.0001) both in heterozygotes and in homozygotes for the polymorphism, but only for Ethiopians. CYP3A4*1B did not influence CD4 count or AIDS defining illnesses.
- PXR promoter and intron 1 SNPs associated with PXR target gene expression (CYP3A4)
- CYP3A4*1B variant is present in both the Tepehuano and Mestizo populations of northern Mexico at frequencies that are similar to that found in the white North American population, but different from that in African and Asian populations.
- LS180 cells may be useful to quickly investigate the CYP3A4-inducing effect of drugs.
- Frequency distribution of CYP3A4 gene polymorphism in ethnic populations and in transplant receipients is reported.
- CYP3A4 in Nanodiscs remains enzymatically active throughout the precipitation protocol as monitored by bromocriptine binding
- CYP3A4*16B was associated with decreased metabolism of irinotecan to APC cpd.
- Both mRNA levels and metabolic activity of CYP3A4 in serum-shocked HepG2 cells fluctuated rhythmically with a period length of about 24 h.
- Here are presented several in vitro methods to detect induction of CYP1A2 and CYP3A4 in fresh and cryopreserved primary human hepatocytes
- Summarized the frequently used CYP3A probe drugs, inducers and inhibitors, and evaluated their current status in drug development and research. (Review)
- The near-infrared fluorescent probe Nile Red, which has strong solvatochromic behavior, was investigated as a probe of allostery and sequential metabolism with CYP3A4.
- QSAR analysis for substrate specificity of six CYP isoforms, revealing that CYP2C9 substrates are anionic compounds, while CYP2D6 substrates are cationic, and CYP2E1 substrates are smaller compounds, while CYP3A4 substrates are larger compounds
- CYP3A4 metabolized statins had no effect on the antiplatelet activity of a loading dose of clopidogrel 600mg and did not affect clinical outcome after coronary stenting.
- miR-148a post-transcriptionally regulated human PXR, resulting in the modulation of the inducible and/or constitutive levels of CYP3A4 in human liver.
- Concomitant exposure to glucocorticoids and phthalates resulted in enhanced metabolic activity of CYP3A4 in human hepatocytes.
- metabolism of tandospirone by human liver microsomes primarily involves CYP3A4, and to a lesser extent CYP2D6
- Data concluded that CYP2C9, CYP2C19 and CYP3A4 are the primary cytochromes in the bioactivation of lynestrenol in vitro, while CYP3A4 catalyses the further metabolism of norethindrone.
- Eribulin does not appear to affect the metabolism of other therapeutic agents by CYP3A4.
- result shows, for the first time, that N-terminal truncated, catalytically active CYP3A4 is present principally in the cytoplasm of human liver cells
- CYP3A4 polymorphism is associated with lipid-lowering efficacy of atorvastatin but not of simvastatin.
- caffeine C-8-hydroxylation preferentially involves CYP1A2 and CYP3A4; 7-N-demethylation is catalyzed non-specifically, mainly by CYP1A2 and, to a smaller extent, by CYP2C8/9 and CYP3A4 (and not by CYP2E1, as suggested previously)
- Patients with CYP3A4*18B alleles may require higher doses of CsA to reach the target levels.
- in renal allograft recipients the CYP3A5*3/*1 genotype, but not polymorphisms of MDR1 or CYP3A4) is associated with a reduced susceptibility for the inhibitory effects of fluconazole on tacrolimus metabolism
- Cdk2 negatively regulates the activity of hPXR, and suggest an important role for Cdk2 in regulating hPXR activity and CYP3A4 expression in hepatocytes passing through the cell cycle
- Studies with tissue-specific CYP3A4 transgenic Cyp3a(-/-) mice revealed that not only hepatic but also intestinal expression of human CYP3A4 could reduce the hepatic expression of detoxifying systems to near wild-type levels.
- CYP2C19 and CYP3A4 can 21-hydroxylate progesterone but not 17OHP, possibly ameliorating mineralocorticoid deficiency, but not glucocorticoid deficiency.
- A genetic variation in the CYP3A4 gene--as a gain-of-function mutation in the metabolism of certain CYP3A substrates--including sex steroids, may predispose individuals to osteoporosis.
- CYP1A1 induction and CYP3A4 inhibition by the fungicide imazalil in the human intestinal Caco-2 cells-comparison with other conazole pesticides.
- both UBC7/gp78 and UbcH5a/CHIP may be involved in CYP3A4 ER-associated degradation, although their relative physiological contribution remains to be established
- Single nucleotide polymorphism in CYP3A4 gene is associated with ovarian cancer.