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Items: 43

1.

Drug Concentration Asymmetry in Tissues and Plasma for Small Molecule-Related Therapeutic Modalities.

Zhang D, Hop CE, Patilea-Vrana G, Gampa G, Seneviratne HK, Unadkat JD, Kenny JR, Nagapudi K, Di L, Zhou L, Zak M, Wright MR, Bumpus NN, Zang R, Liu X, Lai Y, Khojasteh SC.

Drug Metab Dispos. 2019 Jul 2. pii: dmd.119.086744. doi: 10.1124/dmd.119.086744. [Epub ahead of print]

2.

Tenofovir Plasma Concentration from Preexposure Prophylaxis at the Time of Potential HIV Exposure: a Population Pharmacokinetic Modeling and Simulation Study Involving Serodiscordant Couples in East Africa.

Mallayasamy S, Chaturvedula A, Fossler MJ, Sale M, Goti V, Bumpus NN, Marzinke MA, Hendrix CW, Haberer JE; Partners Demonstration Project Team.

Antimicrob Agents Chemother. 2019 Jul 25;63(8). pii: e00446-19. doi: 10.1128/AAC.00446-19. Print 2019 Aug.

PMID:
31182536
3.

Biotransformation and bioactivation reactions - 2018 literature highlights.

Khojasteh SC, Bumpus NN, Driscoll JP, Miller GP, Mitra K, Rietjens IMCM, Zhang D.

Drug Metab Rev. 2019 May;51(2):121-161. doi: 10.1080/03602532.2019.1615937. Epub 2019 Aug 6.

PMID:
31170851
4.

Genetic variation of kinases and activation of nucleotide analog reverse transcriptase inhibitor tenofovir.

Hamlin AN, Tillotson J, Bumpus NN.

Pharmacogenomics. 2019 Jan;20(2):105-111. doi: 10.2217/pgs-2018-0140. Epub 2019 Jan 10.

PMID:
30628547
5.

Efavirenz and Efavirenz-like Compounds Activate Human, Murine, and Macaque Hepatic IRE1α-XBP1.

Heck CJS, Hamlin AN, Bumpus NN.

Mol Pharmacol. 2019 Feb;95(2):183-195. doi: 10.1124/mol.118.113647. Epub 2018 Nov 15.

PMID:
30442673
6.

Population Pharmacokinetics and Pharmacodynamics of Disulfiram on Inducing Latent HIV-1 Transcription in a Phase IIb Trial.

Lee SA, Elliott JH, McMahon J, Hartogenesis W, Bumpus NN, Lifson JD, Gorelick RJ, Bacchetti P, Deeks SG, Lewin SR, Savic RM.

Clin Pharmacol Ther. 2019 Mar;105(3):692-702. doi: 10.1002/cpt.1220. Epub 2018 Oct 9.

PMID:
30137649
7.

MALDI Mass Spectrometry Imaging Reveals Heterogeneous Distribution of Tenofovir and Tenofovir Diphosphate in Colorectal Tissue of Subjects Receiving a Tenofovir-Containing Enema.

Seneviratne HK, Hendrix CW, Fuchs EJ, Bumpus NN.

J Pharmacol Exp Ther. 2018 Oct;367(1):40-48. doi: 10.1124/jpet.118.250357. Epub 2018 Jul 23.

PMID:
30037813
8.

Discovery of genetic variants of the kinases that activate tenofovir among individuals in the United States, Thailand, and South Africa: HPTN067.

Figueroa DB, Tillotson J, Li M, Piwowar-Manning E, Hendrix CW, Holtz TH, Bokoch K, Bekker LG, van Griensven F, Mannheimer S, Hughes JP, Grant RM, Bumpus NN.

PLoS One. 2018 Apr 11;13(4):e0195764. doi: 10.1371/journal.pone.0195764. eCollection 2018.

9.

Genetic Variation of the Kinases That Phosphorylate Tenofovir and Emtricitabine in Peripheral Blood Mononuclear Cells.

Figueroa DB, Madeen EP, Tillotson J, Richardson P, Cottle L, McCauley M, Landovitz RJ, Andrade A, Hendrix CW, Mayer KH, Wilkin T, Gulick RM, Bumpus NN.

AIDS Res Hum Retroviruses. 2018 May;34(5):421-429. doi: 10.1089/AID.2017.0243. Epub 2018 Mar 20.

10.

Probing Ligand Structure-Activity Relationships in Pregnane X Receptor (PXR): Efavirenz and 8-Hydroxyefavirenz Exhibit Divergence in Activation.

Narayanan B, Lade JM, Heck CJS, Dietz KD, Wade H, Bumpus NN.

ChemMedChem. 2018 Apr 6;13(7):736-747. doi: 10.1002/cmdc.201700730. Epub 2018 Mar 2.

11.

Utility of Different Adherence Measures for PrEP: Patterns and Incremental Value.

Abaasa A, Hendrix C, Gandhi M, Anderson P, Kamali A, Kibengo F, Sanders EJ, Mutua G, Bumpus NN, Priddy F, Haberer JE.

AIDS Behav. 2018 Apr;22(4):1165-1173. doi: 10.1007/s10461-017-1951-y.

12.

Single Heteroatom Substitutions in the Efavirenz Oxazinone Ring Impact Metabolism by CYP2B6.

Cox PM, Bumpus NN.

ChemMedChem. 2016 Dec 6;11(23):2630-2637. doi: 10.1002/cmdc.201600519. Epub 2016 Nov 10.

13.

Single-Stranded Nucleic Acids Bind to the Tetramer Interface of SAMHD1 and Prevent Formation of the Catalytic Homotetramer.

Seamon KJ, Bumpus NN, Stivers JT.

Biochemistry. 2016 Nov 8;55(44):6087-6099. Epub 2016 Oct 27.

14.

Divergence of Antiangiogenic Activity and Hepatotoxicity of Different Stereoisomers of Itraconazole.

Shim JS, Li RJ, Bumpus NN, Head SA, Kumar Pasunooti K, Yang EJ, Lv J, Shi W, Liu JO.

Clin Cancer Res. 2016 Jun 1;22(11):2709-20. doi: 10.1158/1078-0432.CCR-15-1888. Epub 2016 Jan 22.

15.

Discovery of Genetic Variants of the Kinases That Activate Tenofovir in a Compartment-specific Manner.

Lade JM, To EE, Hendrix CW, Bumpus NN.

EBioMedicine. 2015 Jul 9;2(9):1145-52. doi: 10.1016/j.ebiom.2015.07.008. eCollection 2015 Sep.

16.

Dose Frequency Ranging Pharmacokinetic Study of Tenofovir-Emtricitabine After Directly Observed Dosing in Healthy Volunteers to Establish Adherence Benchmarks (HPTN 066).

Hendrix CW, Andrade A, Bumpus NN, Kashuba AD, Marzinke MA, Moore A, Anderson PL, Bushman LR, Fuchs EJ, Wiggins I, Radebaugh C, Prince HA, Bakshi RP, Wang R, Richardson P, Shieh E, McKinstry L, Li X, Donnell D, Elharrar V, Mayer KH, Patterson KB.

AIDS Res Hum Retroviruses. 2016 Jan;32(1):32-43. doi: 10.1089/AID.2015.0182. Epub 2015 Oct 15.

17.

Response to "clinical relevance of CYP3A5 genotype on maraviroc exposures".

Lu Y, Fuchs EJ, Hendrix CW, Bumpus NN.

Drug Metab Dispos. 2015 May;43(5):773. doi: 10.1124/dmd.115.064188. No abstract available.

18.

Correlation between compartmental tenofovir concentrations and an ex vivo rectal biopsy model of tissue infectibility in the RMP-02/MTN-006 phase 1 study.

Richardson-Harman N, Hendrix CW, Bumpus NN, Mauck C, Cranston RD, Yang K, Elliott J, Tanner K, McGowan I, Kashuba A, Anton PA.

PLoS One. 2014 Oct 28;9(10):e111507. doi: 10.1371/journal.pone.0111507. eCollection 2014.

19.

Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz.

Cox PM, Bumpus NN.

ACS Med Chem Lett. 2014 Sep 4;5(10):1156-1161. eCollection 2014 Oct 9.

20.

CYP3A5 genotype impacts maraviroc concentrations in healthy volunteers.

Lu Y, Fuchs EJ, Hendrix CW, Bumpus NN.

Drug Metab Dispos. 2014 Nov;42(11):1796-802. doi: 10.1124/dmd.114.060194. Epub 2014 Aug 12.

21.

Small molecule inhibition of SAMHD1 dNTPase by tetramer destabilization.

Seamon KJ, Hansen EC, Kadina AP, Kashemirov BA, McKenna CE, Bumpus NN, Stivers JT.

J Am Chem Soc. 2014 Jul 16;136(28):9822-5. doi: 10.1021/ja5035717. Epub 2014 Jul 8.

22.

HIV protective efficacy and correlates of tenofovir blood concentrations in a clinical trial of PrEP for HIV prevention.

Donnell D, Baeten JM, Bumpus NN, Brantley J, Bangsberg DR, Haberer JE, Mujugira A, Mugo N, Ndase P, Hendrix C, Celum C.

J Acquir Immune Defic Syndr. 2014 Jul 1;66(3):340-8. doi: 10.1097/QAI.0000000000000172.

23.

A targeted proteomics approach for profiling murine cytochrome P450 expression.

Hersman EM, Bumpus NN.

J Pharmacol Exp Ther. 2014 May;349(2):221-8. doi: 10.1124/jpet.113.212456. Epub 2014 Mar 4.

24.

A pilot study assessing the safety and latency-reversing activity of disulfiram in HIV-1-infected adults on antiretroviral therapy.

Spivak AM, Andrade A, Eisele E, Hoh R, Bacchetti P, Bumpus NN, Emad F, Buckheit R 3rd, McCance-Katz EF, Lai J, Kennedy M, Chander G, Siliciano RF, Siliciano JD, Deeks SG.

Clin Infect Dis. 2014 Mar;58(6):883-90. doi: 10.1093/cid/cit813. Epub 2013 Dec 12.

25.
26.

Dissimilarities in the metabolism of antiretroviral drugs used in HIV pre-exposure prophylaxis in colon and vagina tissues.

To EE, Hendrix CW, Bumpus NN.

Biochem Pharmacol. 2013 Oct 1;86(7):979-90. doi: 10.1016/j.bcp.2013.08.013. Epub 2013 Aug 18.

27.

Human biotransformation of the nonnucleoside reverse transcriptase inhibitor rilpivirine and a cross-species metabolism comparison.

Lade JM, Avery LB, Bumpus NN.

Antimicrob Agents Chemother. 2013 Oct;57(10):5067-79. doi: 10.1128/AAC.01401-13. Epub 2013 Aug 5.

28.

Undisclosed antiretroviral drug use in a multinational clinical trial (HIV Prevention Trials Network 052).

Fogel JM, Wang L, Parsons TL, Ou SS, Piwowar-Manning E, Chen Y, Mudhune VO, Hosseinipour MC, Kumwenda J, Hakim JG, Chariyalertsak S, Panchia R, Sanne I, Kumarasamy N, Grinsztejn B, Makhema J, Pilotto J, Santos BR, Mayer KH, McCauley M, Gamble T, Bumpus NN, Hendrix CW, Cohen MS, Eshleman SH.

J Infect Dis. 2013 Nov 15;208(10):1624-8. doi: 10.1093/infdis/jit390. Epub 2013 Aug 1.

29.

MTN-001: randomized pharmacokinetic cross-over study comparing tenofovir vaginal gel and oral tablets in vaginal tissue and other compartments.

Hendrix CW, Chen BA, Guddera V, Hoesley C, Justman J, Nakabiito C, Salata R, Soto-Torres L, Patterson K, Minnis AM, Gandham S, Gomez K, Richardson BA, Bumpus NN.

PLoS One. 2013;8(1):e55013. doi: 10.1371/journal.pone.0055013. Epub 2013 Jan 30.

30.

Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.

Avery LB, VanAusdall JL, Hendrix CW, Bumpus NN.

Drug Metab Dispos. 2013 Feb;41(2):422-9. doi: 10.1124/dmd.112.049601. Epub 2012 Nov 19.

31.

Dendritic spine injury induced by the 8-hydroxy metabolite of efavirenz.

Tovar-y-Romo LB, Bumpus NN, Pomerantz D, Avery LB, Sacktor N, McArthur JC, Haughey NJ.

J Pharmacol Exp Ther. 2012 Dec;343(3):696-703. doi: 10.1124/jpet.112.195701. Epub 2012 Sep 13.

32.

RMP-02/MTN-006: A phase 1 rectal safety, acceptability, pharmacokinetic, and pharmacodynamic study of tenofovir 1% gel compared with oral tenofovir disoproxil fumarate.

Anton PA, Cranston RD, Kashuba A, Hendrix CW, Bumpus NN, Richardson-Harman N, Elliott J, Janocko L, Khanukhova E, Dennis R, Cumberland WG, Ju C, Carballo-Diéguez A, Mauck C, McGowan I.

AIDS Res Hum Retroviruses. 2012 Nov;28(11):1412-21. doi: 10.1089/AID.2012.0262. Epub 2012 Oct 9.

33.

Cytochrome P450 3A5 plays a prominent role in the oxidative metabolism of the anti-human immunodeficiency virus drug maraviroc.

Lu Y, Hendrix CW, Bumpus NN.

Drug Metab Dispos. 2012 Dec;40(12):2221-30. doi: 10.1124/dmd.112.048298. Epub 2012 Aug 24.

34.

Antiretroviral prophylaxis for HIV prevention in heterosexual men and women.

Baeten JM, Donnell D, Ndase P, Mugo NR, Campbell JD, Wangisi J, Tappero JW, Bukusi EA, Cohen CR, Katabira E, Ronald A, Tumwesigye E, Were E, Fife KH, Kiarie J, Farquhar C, John-Stewart G, Kakia A, Odoyo J, Mucunguzi A, Nakku-Joloba E, Twesigye R, Ngure K, Apaka C, Tamooh H, Gabona F, Mujugira A, Panteleeff D, Thomas KK, Kidoguchi L, Krows M, Revall J, Morrison S, Haugen H, Emmanuel-Ogier M, Ondrejcek L, Coombs RW, Frenkel L, Hendrix C, Bumpus NN, Bangsberg D, Haberer JE, Stevens WS, Lingappa JR, Celum C; Partners PrEP Study Team.

N Engl J Med. 2012 Aug 2;367(5):399-410. doi: 10.1056/NEJMoa1108524. Epub 2012 Jul 11.

35.
36.

Efavirenz and 8-hydroxyefavirenz induce cell death via a JNK- and BimEL-dependent mechanism in primary human hepatocytes.

Bumpus NN.

Toxicol Appl Pharmacol. 2011 Dec 1;257(2):227-34. doi: 10.1016/j.taap.2011.09.008. Epub 2011 Sep 19.

PMID:
21958719
38.

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. doi: 10.1016/j.jinorgbio.2009.12.017. Epub 2010 Jan 4.

39.

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. doi: 10.1124/mol.108.048637. Epub 2008 Jul 11.

40.

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.

PMID:
18052110
41.

Metabolism of efavirenz and 8-hydroxyefavirenz by P450 2B6 leads to inactivation by two distinct mechanisms.

Bumpus NN, Kent UM, Hollenberg PF.

J Pharmacol Exp Ther. 2006 Jul;318(1):345-51. Epub 2006 Apr 12.

PMID:
16611850
42.

The naturally occurring cytochrome P450 (P450) 2B6 K262R mutant of P450 2B6 exhibits alterations in substrate metabolism and inactivation.

Bumpus NN, Sridar C, Kent UM, Hollenberg PF.

Drug Metab Dispos. 2005 Jun;33(6):795-802. Epub 2005 Mar 15.

PMID:
15769884
43.

Metabolism of N,N',N"-triethylenethiophosphoramide by CYP2B1 and CYP2B6 results in the inactivation of both isoforms by two distinct mechanisms.

Harleton E, Webster M, Bumpus NN, Kent UM, Rae JM, Hollenberg PF.

J Pharmacol Exp Ther. 2004 Sep;310(3):1011-9. Epub 2004 Apr 30.

PMID:
15121764

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