Ask about this productRelated genes to: CYP1A2 antibody
- Gene:
- CYP1A2 NIH gene
- Name:
- cytochrome P450 family 1 subfamily A member 2
- Previous symbol:
- -
- Synonyms:
- P3-450, CP12
- Chromosome:
- 15q24.1
- Locus Type:
- gene with protein product
- Date approved:
- 1990-04-25
- Date modifiied:
- 2019-04-23
Related products to: CYP1A2 antibody
Related articles to: CYP1A2 antibody
- INTRODUCTION : The evaluation of pharmacokinetic interactions is based on the knowledge of enzymatic metabolization by cytochrome 450 enzymes or cellular transport processes. Research on the metabolism of pipamperone, an antipsychotic of the butyrophenone family, has not yet yielded conclusive results. In the present in vitro study, human cytochrome enzymes were investigated for their possible involvement in the metabolism of pipamperone. - Source: PubMed
Publication date: 2026/08/19
Pfaff TamaraHinz BurkhardWalther Udo I - Hypoxic pregnancy promotes fetal growth restriction (FGR) and preterm birth, for which antenatal corticosteroids (ACS) are recommended to prevent respiratory distress. Adults born FGR or preterm are at greater risk of health conditions requiring medication(s), which are metabolised by hepatic cytochrome P450 (CYP) enzymes. We determined if ACS and/or hypoxic pregnancy alters fetal and adult offspring hepatic CYP activity. Ewes carrying singletons were randomly allocated to normoxic (Nx) or hypoxic (Hx; 11% O) pregnancy from 105 to 138 dGA (term = 147 dGA). Dexamethasone (Dex, 12 mg IM) or vehicle (saline IV) was administered at 115 and 116 dGA. Ewes carrying male fetuses were humanely killed at 138 ± 2 dGA, while female fetuses lambed spontaneously and were humanely killed at 9 months (9 mo). Hepatic CYP activity was quantified using functional assays, and expression of glucocorticoid signalling and CYP regulating proteins was determined via Western blot. Hx increased fetal hepatic CYP2B6 and CYP2D6 activity, expression of 11β-HSD1&2 and reduced GRα-A nuclear expression, and cytosolic GRβ:α-A ratio. Dex reduced fetal CYP3A metabolism of testosterone to metabolites 6β-OHT and 2α-OHT, and GRα-A and GRβ cytosolic expression. Fetal CYP2B6 activity positively correlated with CAR in Nx, but not Hx. In 9 mo lambs, Hx reduced CYP2C19 activity and PPARα and GRβ cytosolic expression. Dex decreased CYP1A2, CYP2B6, CYP2E1 activity, and CYP3A testosterone metabolism to 6β-OHT. HxDex increased cytosolic and nuclear GRβ:α-A. Hx and Dex differentially effect hepatic CYP activity in offspring, and changes to CYP activity may be due to a loss of regulatory control. - Source: PubMed
Publication date: 2026/08/13
Bennett Millicent G AMeakin Ashley SBotting-Lawford Kimberley JNiu YouguoFord Sage GWiese Michael DGiussani Dino AMorrison Janna L - Hepatocellular carcinoma (HCC) has a poor prognosis and limited treatment options. This study investigated the role and mechanism of Jiedu Xiaozheng Yin (JXY) in HCC using network pharmacology and in vivo/in vitro experiments. Active components of JXY and their potential therapeutic targets for HCC were identified via network pharmacology. A protein-protein interaction (PPI) network was constructed to identify core targets, and bioinformatics analysis confirmed their association with HCC. LC-MS/MS was used to isolate major components, which were then subjected to molecular docking with core targets. The effects of JXY on HCC were further validated through in vivo and in vitro experiments. Analysis of 171 core target genes was performed using PPI network screening and enrichment analysis. Quercetin was identified as the primary active component of JXY. Molecular docking confirmed its interaction with CYP1A2, which is overexpressed in HCC tissues. In vivo, JXY and quercetin significantly increased CYP1A2 and PTEN expression, while decreasing p-PI3K and p-Akt levels in HCC-bearing mice, thereby suppressing tumor growth and lung metastasis and promoting apoptosis. In vitro, both JXY and quercetin inhibited HCC cell proliferation and migration. CYP1A2 knockdown partially reversed, while its overexpression enhanced, these inhibitory effects. Quercetin, the main active component of JXY, upregulates CYP1A2 to promote PTEN expression, thereby inhibiting the PI3K/Akt signaling pathway and suppressing HCC progression. - Source: PubMed
Publication date: 2026/08/07
Zhou ZhenhuaXiao ZhenliangWen WuZhu Yongkang - Cytochrome P450 2E1 (CYP2E1) plays a pivotal role in the metabolism and detoxification of low molecular-weight xenobiotics, as well as in their bioactivation into toxic and DNA-reactive intermediates. Prominent examples include drugs and chemicals like acetaminophen and N-nitrosamines. Chlorzoxazone and 4-nitrophenol are widely used as probe substrates to assess CYP2E1 activity, however, their specificity remains controversial. This study aimed to reevaluate the selectivity of chlorzoxazone and 4-nitrophenol toward CYP2E1 using recombinant Supersomes™ expressing individual human CYP isoforms. Incubations were performed with chlorzoxazone and 4-nitrophenol at 100 and 500 µM, followed by quantification of 6-hydroxychlorzoxazone and 4-nitrocatechol via UPLC-MS/MS. Chlorzoxazone turnover was detected across nearly all major liver CYP isoforms, with CYP1A1 showing the highest contribution (39%), followed by CYP2D6 (14%), CYP1A2 (10%), and CYP2E1 (10%). Similarly, 4-nitrophenol hydroxylation was not limited to CYP2E1, with significant contributions from CYP1A2 (20%), CYP2A6 (19%), and CYP2D6 (16%), while CYP2E1 accounted for 26% of total activity. In conclusion, our results underscore the limited selectivity of chlorzoxazone and 4-nitrophenol and highlight the need for more specific substrates for accurate CYP2E1 enzyme characterization. - Source: PubMed
Publication date: 2026/08/04
Hellmann AnnaLenich Ann-KathrinRuez StephanieFahrer JörgLott JasminSchaefer Michelle - Associations between genetically predicted activity of metabolic enzymes and risks of adverse events from tyrosine kinase inhibitors (TKIs) may inform dosing to optimize treatment outcomes in patients with cancer. The goal of this study is to investigate the associations between UGT1A1, CYP3A4, and CYP1A2 activity and toxicity from nilotinib and pazopanib treatment. A retrospective pharmacogenetic association study was conducted in 117 participants of the Michigan Genomics Initiative who received pazopanib (n = 103) or nilotinib (n = 14). Clinical information, including patients' disease, treatment, and toxicity was collected via retrospective review of medical records. No associations were found between the genetically predicted activity of any of the three enzymes and the composite endpoint of severe toxicity or treatment modifications because of toxicity. In the secondary hypothesis-generating analyses, patients with reduced UGT1A1 activity had an increased incidence of increased aspartate aminotransferase/alanine aminotransferase (44 vs. 25%; P = 0.034) and hypertension (52 vs. 31%; P = 0.024). In addition, patients with increased CYP1A2 activity from carrying CYP1A2*1F had a lower incidence of severe toxicity from pazopanib (β-coefficient = -0.163, 95% confidence interval: -0.19 to -0.14, P = 0.008). Future investigations are needed to confirm these associations and determine whether personalized TKI treatment can optimize therapeutic outcomes in patients with cancer. - Source: PubMed
Publication date: 2026/07/28
Moy April TD'Angelo Lia EHertz Daniel L