Latest Publications - selected

• Mechanism-Based Inactivation of Cytochrome P450 2B6 by Methadone Through Destruction of Prosthetic Heme. Amunugama, H., Zhang, H., and Hollenberg, P.F. Drug Metab Dispos., 2012 In press

• Formation Of The Thiol Conjugates And Active Metabolite of Clopidogrel By Human Liver Microsomes. Zhang, H., Lau, W.C., Hollenberg, P.F. Mol Pharmacol, 2012. In press

• High-Throughput Fluorescence Assay for Cytochrome P450 Mechanism-Based Inactivators. Kenaan, C., Zhang, H., and Hollenberg, P.F. Methods in Molecular Biology, 2012 (Invited). In press.

• Identification of the Residue in Human CYP3A4 that is Covalently Modified by Bergamottin and the Reactive Intermediate that Contributes to the Grapefruit Juice Effect. Lin, H.L., Kenaan, C., Hollenberg, P.F. Drug Metab Dispos., 2012 May;40(5): p.998-1006. PMID 22344702

• Thr302 is the Site for the Covalent Modification of Human Cytochrome P450 2B6 Leading to Mechanism-based Inactivation by tert-Butylphenylacetylene. Lin, H.L., Zhang, H., Pratt-Hyatt, M. J., and Hollenberg, P.F. Drug Metab Dispos. 2011 Dec;39(12): p. 2431-9. PMID 21930824

•Mechanism-Based Inactivation Of Human Cytochrome P450 2B6 By Clopidogrel: Involvement Of Both Covalent Modification Of Cysteinyl Residue 475 And Loss of Heme. Zhang, H., Amunugama, H., Ney, S., Cooper, N. and Hollenberg, P.F. Mol Pharmacol. 2011 80(5): p. 839-847. PMID 21862689

• Polymorphic Variants Of Cytochrome P450 2B6 (CYP2B6.4-CYP2B6.9) Exhibit Altered Rates Of Metabolism For Bupropion And Efavirenz: A Charge-Reversal Mutation In The K139E Variant (CYP2B6.8) Impairs Formation Of A Functional P450-Reductase Complex. Zhang, H., Chitra, S., Kenaan, C., Amunugama, H., Ballou, D.P., and Hollenberg, P.F. J Pharmacol Expt Ther. 2011 Sep;338(3):803-9. PMID 21659470

•Structural Analysis of Mammalian Cytochrome P450 2B4 Covalently Bound to the Mechanism-Based Inactivator tert-Butylphenylacetylene: Insight into Partial Enzymatic Activity. Gay, S.C., Zhang, H., Wilderman, P.R., Roberts, A.G., Liu, T., Li, S., Lin, H.L , Zhang, Q., Woods, V.L., Stout, C.D., Hollenberg, P.F., and Halpert, J.R. Biochemistry. 2011 Jun 7;50(22):4903-11 PMID 21510666

• Uncovering the Role of Hydrophobic Residues in Cytochrome P450 - Cytochrome P450 Reductase Interactions. Kenaan, C., Zhang, H., Shea, E.V., and Hollenberg, P.F. Biochemistry, 2011, 50 (19), pp 3957-3967 PMID 21462923

• Anandamide oxidation by wild type and polymorphically expressed CYP2B6 and CYP2D6. Sridar, C., Snider, NT., and Hollenberg, PF. Drug Metab Dispos. 2011 May;39(5):782-8. . PMID: 21289075

• Inactivation of Cytochrome P450 3A4 but not 3A5 by OSI-930, a Thiophene-containing Anticancer Drug. Lin, HL., Zhang, H., Medower, C., Hollenberg, P.F., and Johnson, W.W. Drug Metab Dispos. 2011 Feb. PMID: 21068193 (manuscript featured on the cover of the February 2011 issue).

• A Quantitative High-Throughput 96-well plate Fluorescence Assay for Mechanism-Based Inactivators of Cytochromes P450 Exemplified using CYP2B6. Kenaan, C., Zhang, H., and Hollenberg, P.F. Nature Protocols, 2010.Sep; 5 (10): 1652-8. PMID:20885377

• Targeting of the highly conserved threonine 302 residue of cytochromes P450 2B family during mechanism-based inactivation by aryl acetylenes.Zhang H, Lin HL, Kenaan C, Hollenberg PF. Arch Biochem Biophys. 2010 Sep 10. [Epub ahead of print]PMID: 20836985

• Mechanism-based inactivation of Human Cytochrome P450 2E1 by Diethyldithocarbamate. Pratt-Hyatt M, Lin HL, Hollenberg P. Drug Metab Dispos. 2010 Sep 8. [Epub ahead of print]PMID: 20826547

• Effects Of a Commonly Occurring Genetic Polymorphism of Human CYP3A4 (Ile118Val) On the Metabolism of Anandamide. Pratt-Hyatt M, Zhang H, Snider N, Hollenberg PF. Drug Metab Dispos. 2010 Aug 11. [Epub ahead of print]PMID: 20702771

• Covalent modification of Thr302 in cytochrome P450 2B1 by the mechanism-based inactivator 4-tert-butylphenylacetylene. Lin HL, Zhang H, Jushchyshyn M, Hollenberg PF. J Pharmacol Exp Ther. 2010 Jun;333(3):663-9. Epub 2010 Mar 3.PMID: 20200115

• Beta sheet 2-alpha helix C loop of cytochrome P450 reductase serves as a docking site for redox partners. Jang HH, Jamakhandi AP, Sullivan SZ, Yun CH, Hollenberg PF, Miller GP. Biochim Biophys Acta. 2010 Jun;1804(6):1285-93. Epub 2010 Feb 10.PMID: 20152939

• Introduction: mechanisms of metal toxicity special issue. Hollenberg PF. Chem Res Toxicol. 2010 Feb 15;23(2):292-3.

• Oxidation of the endogenous cannabinoid arachidonoyl ethanolamide by the cytochrome P450 monooxygenases: physiological and pharmacological implications. Snider NT, Walker VJ, Hollenberg PF. Pharmacol Rev. 2010 Mar;62(1):136-54. Epub 2010 Feb 4. Review.PMID: 20133390

• Cross-linking of human cytochrome P450 2B6 to NADPH-cytochrome P450 reductase: Identification of a potential site of interaction. Bumpus NN, Hollenberg PF. J Inorg Biochem. 2010 Apr;104(4):485-8. Epub 2010 Jan 4.PMID: 20096935

• Defining the structural consequences of mechanism-based inactivation of mammalian cytochrome P450 2B4 using resonance Raman spectroscopy. Mak PJ, Zhang H, Hollenberg PF, Kincaid JR. J Am Chem Soc. 2010 Feb 10;132(5):1494-5.PMID: 20078059

• Gender dimorphic formation of mouse Mallory-Denk bodies and the role of xenobiotic metabolism and oxidative stress. Hanada S, Snider NT, Brunt EM, Hollenberg PF, Omary MB. Gastroenterology. 2010 Apr;138(4):1607-17. Epub 2010 Jan 11.PMID: 20064513

• tert-Butylphenylacetylene is a potent mechanism-based inactivator of cytochrome P450 2B4: inhibition of cytochrome P450 catalysis by steric hindrance. Zhang H, Lin HL, Walker VJ, Hamdane D, Hollenberg PF. Mol Pharmacol. 2009 Nov;76(5):1011-8. Epub 2009 Aug 31.PMID: 19720728

• Mechanism-based inactivation of CYP2B1 and its F-helix mutant by two tert-butyl acetylenic compounds: covalent modification of prosthetic heme versus apoprotein. Lin HL, Zhang H, Noon KR, Hollenberg PF. J Pharmacol Exp Ther. 2009 Nov;331(2):392-403. Epub 2009 Aug 21.PMID: 19700628

• Effect of conformational dynamics on substrate recognition and specificity as probed by the introduction of a de novo disulfide bond into cytochrome P450 2B1. Zhang H, Kenaan C, Hamdane D, Hoa GH, Hollenberg PF. J Biol Chem. 2009 Sep 18;284(38):25678-86. Epub 2009 Jul 15.PMID: 19605359

• Kinetics of oxidation of benzphetamine by compounds I of cytochrome P450 2B4 and its mutants. Sheng X, Zhang H, Im SC, Horner JH, Waskell L, Hollenberg PF, Newcomb M. J Am Chem Soc. 2009 Mar 4;131(8):2971-6.PMID: 19209859

• Kinetic isotope effects in hydroxylation reactions effected by cytochrome P450 compounds I implicate multiple electrophilic oxidants for P450-catalyzed oxidations. Sheng X, Zhang H, Hollenberg PF, Newcomb M. Biochemistry. 2009 Feb 24;48(7):1620-7.PMID: 19182902

• A cytochrome P450-derived epoxygenated metabolite of anandamide is a potent cannabinoid receptor 2-selective agonist. Snider NT, Nast JA, Tesmer LA, Hollenberg PF. Mol Pharmacol. 2009 Apr;75(4):965-72. Epub 2009 Jan 26.PMID: 19171674

• Metabolic activation of mifepristone [RU486; 17beta-hydroxy-11beta-(4-dimethylaminophenyl)-17alpha-(1-propynyl)-estra-4,9-dien-3-one] by mammalian cytochromes P450 and the mechanism-based inactivation of human CYP2B6. Lin HL, Zhang H, Hollenberg PF. J Pharmacol Exp Ther. 2009 Apr;329(1):26-37. Epub 2009 Jan 23.PMID: 19168709

• Mechanistic analysis of the inactivation of cytochrome P450 2B6 by phencyclidine: effects on substrate binding, electron transfer, and uncoupling. Shebley M, Kent UM, Ballou DP, Hollenberg PF. Drug Metab Dispos. 2009 Apr;37(4):745-52. Epub 2009 Jan 14.PMID: 19144770

• Modification of serine 360 by a reactive intermediate of 17-alpha-ethynylestradiol results in mechanism-based inactivation of cytochrome P450s 2B1 and 2B6. Kent UM, Sridar C, Spahlinger G, Hollenberg PF. Chem Res Toxicol. 2008 Oct;21(10):1956-63. Epub 2008 Aug 26.PMID: 18729327

• The endocannabinoid anandamide is a substrate for the human polymorphic cytochrome P450 2D6. Snider NT, Sikora MJ, Sridar C, Feuerstein TJ, Rae JM, Hollenberg PF. J Pharmacol Exp Ther. 2008 Nov;327(2):538-45. Epub 2008 Aug 12.PMID: 18698000

• Differential inhibition of cytochromes P450 3A4 and 3A5 by the newly synthesized coumarin derivatives 7-coumarin propargyl ether and 7-(4-trifluoromethyl)coumarin propargyl ether. Sridar C, Kent UM, Noon K, McCall A, Alworth B, Foroozesh M, Hollenberg PF. Drug Metab Dispos. 2008 Nov;36(11):2234-43. Epub 2008 Jul 24.PMID: 18653744

• Investigation of the mechanisms underlying the differential effects of the K262R mutation of P450 2B6 on catalytic activity. Bumpus NN, Hollenberg PF. Mol Pharmacol. 2008 Oct;74(4):990-9. Epub 2008 Jul 11.PMID: 18621926

• Oxygen activation by cytochrome P450 monooxygenase. Hamdane D, Zhang H, Hollenberg P. Photosynth Res. 2008 Oct-Dec;98(1-3):657-66. Epub 2008 Jul 4. Review.PMID: 18600471

• Mechanism-based inactivation of human cytochromes p450s: experimental characterization, reactive intermediates, and clinical implications. Hollenberg PF, Kent UM, Bumpus NN. Chem Res Toxicol. 2008 Jan;21(1):189-205. Epub 2007 Dec 4. Review

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