Skip to main content
Article thumbnail
Location of Repository

Metabolism of the EGFR tyrosin kinase inhibitor gefitinib by cytochrome P450 1A1 enzyme in EGFR-wild type non small cell lung cancer cell lines

By Roberta R Alfieri, Maricla Galetti, Stefano Tramonti, Roberta Andreoli, Paola Mozzoni, Andrea Cavazzoni, Mara Bonelli, Claudia Fumarola, Silvia La Monica, Elena Galvani, Giuseppe De Palma, Antonio Mutti, Marco Mor, Marcello Tiseo, Ettore Mari, Andrea Ardizzoni and Pier Giorgio Petronini
Topics: Research
Publisher: BioMed Central
OAI identifier: oai:pubmedcentral.nih.gov:3281800
Provided by: PubMed Central
Download PDF:
Sorry, we are unable to provide the full text but you may find it at the following location(s):
  • http://www.pubmedcentral.nih.g... (external link)
  • Suggested articles

    Citations

    1. (2006). A: Exploring the relationship between expression of cytochrome P450 enzymes and gefitinib pharmacokinetics. Clin Pharmacokinet
    2. (1978). A: Possible mechanisms of emphysema in smokers. In vitro suppression of serum elastase-inhibitory capacity by fresh cigarette smoke and its prevention by antioxidants. Am Rev Respir Dis
    3. (2009). Chowbay B: Polymorphism of human cytochrome P450 enzymes and its clinical impact. Drug Metab Rev
    4. (2005). Cytochrome P450-dependent metabolism of gefitinib. Xenobiotica
    5. (2007). de Waziers I: Reverse transcriptase-PCR quantification of mRNA levels from cytochrome (CYP)1, CYP2 and CYP3 families in 22 different human tissues. Pharmacogenet Genomics
    6. (2004). Du Souich P: Effect of hypoxia on cytochrome P450 activity and expression. Curr Drug Metab
    7. (2003). EK: CYP450- and COMT-derived estradiol metabolites inhibit activity of human coronary artery SMCs. Hypertension
    8. (2006). et al: Creatine as a compatible osmolyte in muscle cells exposed to hypertonic stress.
    9. (2008). et al: Dual mechanisms of action of the 5-benzylidene-hydantoin UPR1024 on lung cancer cell lines. Mol Cancer Ther
    10. (2009). et al: Everolimus restores gefitinib sensitivity in resistant non-small cell lung cancer cell lines. Biochem Pharmacol
    11. (2010). et al: Functional characterization of gefitinib uptake in non-small cell lung cancer cell lines. Biochem Pharmacol
    12. (2010). et al: Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial.
    13. (2006). et al: Molecular predictors of outcome with gefitinib in a phase III placebo-controlled study in advanced non-small-cell lung cancer.
    14. (1997). Expression and localization of CYP3A4 and CYP3A5 in human lung.
    15. (2006). Expression of xenobiotic metabolizing enzymes in different lung compartments of smokers and nonsmokers. Environ Health Perspect
    16. (2009). Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat Rev Drug Discov
    17. (2009). Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev
    18. (1998). Guengerich FP: Selectivity of polycyclic inhibitors for human cytochrome P450s 1A1, 1A2, and 1B1. Chem Res Toxicol
    19. (2000). Induction and regulation of xenobioticmetabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line.
    20. (2008). Interstitial lung disease in Japanese patients with lung cancer: a cohort and nested case-control study. Am J Respir Crit Care Med
    21. (1991). Kawajiri K: PCR detection of an A/G polymorphism within exon 7 of the CYP1A1 gene. Nucleic Acids Res
    22. (2004). M: In vitro metabolism of gefitinib in human liver microsomes. Xenobiotica
    23. (2009). MD: Bioactivation of the epidermal growth factor receptor inhibitor gefitinib: implications for pulmonary and hepatic toxicities. Chem Res Toxicol
    24. (2008). Mechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Clin Cancer Res
    25. (2006). Membrane transporters and channels in chemoresistance and -sensitivity of tumor cells. Cancer Lett
    26. (2006). Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition. Xenobiotica
    27. (2003). Nukiwa T: Severe acute interstitial pneumonia and gefitinib. Lancet
    28. (1997). Oxidation of xenobiotics by recombinant human cytochrome P450 1B1. Drug Metab Dispos
    29. (2011). Quintas-Cardama A: Treatment of non-small-cell lung cancer with erlotinib or gefitinib.
    30. (2008). RH: CYP450 pharmacogenetics for personalizing cancer therapy. Drug Resist Updat
    31. (1994). Roots I: Polymorphisms in the human CYP1A1 gene as susceptibility factors for lung cancer: exon7 mutation (4889 A to G), and a T to C mutation in the 3’-flanking region. Clin Investig
    32. (2000). RT: Bioflavonoids: selective substrates and inhibitors for cytochrome P450 CYP1A and CYP1B1. Toxicology
    33. (2004). Sarkadi B: High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol
    34. (2007). SD: Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res
    35. (1994). SP: Simultaneous measurement of cytochrome P4501A catalytic activity and total protein concentration with a fluorescence plate reader. Anal Biochem
    36. (2009). Sutter TR: EGF receptor signaling blocks aryl hydrocarbon receptormediated transcription and cell differentiation in human epidermal keratinocytes. Proc Natl Acad Sci USA
    37. (2004). Swaisland HC: Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and man. Xenobiotica
    38. (2011). YL: CYP1A1*2A polymorphism as a predictor of clinical outcome in advanced lung cancer patients treated with EGFR-TKI and its combined effects with EGFR intron 1 (CA)n polymorphism.

    To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.