Cytochrome P-450 Enzyme Inhibitors

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  Subject Areas on Research

  • 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. 
  • Aminoanthracene is a mechanism-based inactivator of CYP1A in channel catfish hepatic tissue. 
  • Burden of disease matters when it comes to systemic therapy for prostate cancer. 
  • Characterization of the effects of tebufelone on hepatic cytochromes P450 in the beagle dog. 
  • Clinical enflurane metabolism by cytochrome P450 2E1. 
  • Contribution of itraconazole metabolites to inhibition of CYP3A4 in vivo. 
  • Cytokine-mediated production of nitric oxide in isolated rat hepatocytes is dependent on cytochrome P-450III activity. 
  • Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. 
  • Effects of herbal products and their constituents on human cytochrome P450(2E1) activity. 
  • Effects of inhibition and induction of cytochrome P-450 isozymes on hyperoxic lung injury in rats. 
  • Effects of tobacco smoking and nicotine on cancer treatment. 
  • Elucidation of the functions of genes central to diterpene metabolism in tobacco trichomes using posttranscriptional gene silencing. 
  • Embryonic cardiotoxicity of weak aryl hydrocarbon receptor agonists and CYP1A inhibitor fluoranthene in the Atlantic killifish (Fundulus heteroclitus). 
  • Enantiomeric metabolic interactions and stereoselective human methadone metabolism. 
  • Human enteric microsomal CYP4F enzymes O-demethylate the antiparasitic prodrug pafuramidine. 
  • Human halothane metabolism, lipid peroxidation, and cytochromes P(450)2A6 and P(450)3A4. 
  • Human liver microsomal enflurane defluorination catalyzed by cytochrome P-450 2E1. 
  • Human reductive halothane metabolism in vitro is catalyzed by cytochrome P450 2A6 and 3A4. 
  • Identification of the enzyme responsible for oxidative halothane metabolism: implications for prevention of halothane hepatitis. 
  • In vitro hepatic metabolism explains higher clearance of voriconazole in children versus adults: role of CYP2C19 and flavin-containing monooxygenase 3. 
  • Inactivation of metabolic enzymes by photo-treatment with zinc meta N-methylpyridylporphyrin. 
  • Induction of specific cytochrome P-450 isozymes by methylenedioxyphenyl compounds and antagonism by 3-methylcholanthrene. 
  • Investigating the contribution of CYP2J2 to ritonavir metabolism in vitro and in vivo. 
  • Ketamine as a probe for medetomidine stereoisomer inhibition of human liver microsomal drug metabolism. 
  • Lack of single-dose disulfiram effects on cytochrome P-450 2C9, 2C19, 2D6, and 3A4 activities: evidence for specificity toward P-450 2E1. 
  • Liver-specific loss of beta-catenin blocks glutamine synthesis pathway activity and cytochrome p450 expression in mice. 
  • Metabolism of methadone and levo-alpha-acetylmethadol (LAAM) by human intestinal cytochrome P450 3A4 (CYP3A4): potential contribution of intestinal metabolism to presystemic clearance and bioactivation. 
  • Molecular approaches to identify novel targets for future development of antifungal agents. 
  • Protease-activated receptor 2 (PAR2) protein and transient receptor potential vanilloid 4 (TRPV4) protein coupling is required for sustained inflammatory signaling. 
  • Pruning the ricket thicket. 
  • Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. 
  • Relationship between cytochrome P450 2E1 and acetone catabolism in rats as studied with diallyl sulfide as an inhibitor. 
  • Retinoic acid-mediated gene expression in transgenic reporter zebrafish. 
  • Role of flavin-containing monooxygenase in oxidative metabolism of voriconazole by human liver microsomes. 
  • Similarities and differences in the currents activated by capsaicin, piperine, and zingerone in rat trigeminal ganglion cells. 
  • Single-dose disulfiram does not inhibit CYP2A6 activity. 
  • Single-dose disulfiram inhibition of chlorzoxazone metabolism: a clinical probe for P450 2E1. 
  • Single-dose methoxsalen effects on human cytochrome P-450 2A6 activity. 
  • Statin safety: an assessment using an administrative claims database. 
  • Stereochemical aspects of itraconazole metabolism in vitro and in vivo. 
  • Suppression of a P450 hydroxylase gene in plant trichome glands enhances natural-product-based aphid resistance. 
  • Suppression of male-specific cytochrome P450 2c and its mRNA by 3,4,5,3',4',5'-hexachlorobiphenyl in rat liver is not causally related to changes in serum testosterone. 
  • The gap junction inhibitor 2-aminoethoxy-diphenyl-borate protects against acetaminophen hepatotoxicity by inhibiting cytochrome P450 enzymes and c-jun N-terminal kinase activation.