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Items: 39

1.

Safety, pharmacokinetics, and antiretroviral activity of islatravir (ISL, MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor, following single-dose administration to treatment-naive adults infected with HIV-1: an open-label, phase 1b, consecutive-panel trial.

Schürmann D, Rudd DJ, Zhang S, De Lepeleire I, Robberechts M, Friedman E, Keicher C, Hüser A, Hofmann J, Grobler JA, Stoch SA, Iwamoto M, Matthews RP.

Lancet HIV. 2020 Jan 3. pii: S2352-3018(19)30372-8. doi: 10.1016/S2352-3018(19)30372-8. [Epub ahead of print]

PMID:
31911147
2.

Islatravir for the treatment and prevention of infection with the human immunodeficiency virus type 1.

Markowitz M, Grobler JA.

Curr Opin HIV AIDS. 2020 Jan;15(1):27-32. doi: 10.1097/COH.0000000000000599.

PMID:
31658118
3.

Title: Once-weekly Oral Dosing of MK-8591 Protects Male Rhesus Macaques from Intrarectal SHIV109CP3 Challenge.

Markowitz M, Gettie A, St Bernard L, Andrews CD, Mohri H, Horowitz A, Grasperge BF, Blanchard JL, Niu T, Sun L, Fillgrove K, Hazuda DJ, Grobler JA.

J Infect Dis. 2019 Jun 7. pii: jiz271. doi: 10.1093/infdis/jiz271. [Epub ahead of print]

PMID:
31175822
4.

Extended-Duration MK-8591-Eluting Implant as a Candidate for HIV Treatment and Prevention.

Barrett SE, Teller RS, Forster SP, Li L, Mackey MA, Skomski D, Yang Z, Fillgrove KL, Doto GJ, Wood SL, Lebron J, Grobler JA, Sanchez RI, Liu Z, Lu B, Niu T, Sun L, Gindy ME.

Antimicrob Agents Chemother. 2018 Sep 24;62(10). pii: e01058-18. doi: 10.1128/AAC.01058-18. Print 2018 Oct.

5.

Long-acting formulations for the treatment of latent tuberculous infection: opportunities and challenges.

Swindells S, Siccardi M, Barrett SE, Olsen DB, Grobler JA, Podany AT, Nuermberger E, Kim P, Barry CE, Owen A, Hazuda D, Flexner C.

Int J Tuberc Lung Dis. 2018 Feb 1;22(2):125-132. doi: 10.5588/ijtld.17.0486.

6.

Discovery of a Distinct Chemical and Mechanistic Class of Allosteric HIV-1 Integrase Inhibitors with Antiretroviral Activity.

Burlein C, Wang C, Xu M, Bhatt T, Stahlhut M, Ou Y, Adam GC, Heath J, Klein DJ, Sanders J, Narayan K, Abeywickrema P, Heo MR, Carroll SS, Grobler JA, Sharma S, Diamond TL, Converso A, Krosky DJ.

ACS Chem Biol. 2017 Nov 17;12(11):2858-2865. doi: 10.1021/acschembio.7b00550. Epub 2017 Oct 19.

PMID:
29024587
7.

MK-8591 (4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine) Exhibits Potent Activity against HIV-2 Isolates and Drug-Resistant HIV-2 Mutants in Culture.

Wu VH, Smith RA, Masoum S, Raugi DN, Ba S, Seydi M, Grobler JA, Gottlieb GS; University of Washington–Dakar HIV-2 Study Group.

Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00744-17. doi: 10.1128/AAC.00744-17. Print 2017 Aug.

8.

Characterizing Class-Specific Exposure-Viral Load Suppression Response of HIV Antiretrovirals Using A Model-Based Meta-Analysis.

Xu Y, Li YF, Zhang D, Dockendorf M, Tetteh E, Rizk ML, Grobler JA, Lai MT, Gobburu J, Ankrom W.

Clin Transl Sci. 2016 Aug;9(4):192-200. doi: 10.1111/cts.12395. Epub 2016 May 12.

9.

In vitro resistance selection with doravirine (MK-1439), a novel nonnucleoside reverse transcriptase inhibitor with distinct mutation development pathways.

Feng M, Wang D, Grobler JA, Hazuda DJ, Miller MD, Lai MT.

Antimicrob Agents Chemother. 2015 Jan;59(1):590-8. doi: 10.1128/AAC.04201-14. Epub 2014 Nov 10.

10.

Derivatives of mesoxalic acid block translocation of HIV-1 reverse transcriptase.

Bernatchez JA, Paul R, Tchesnokov EP, Ngure M, Beilhartz GL, Berghuis AM, Lavoie R, Li L, Auger A, Melnyk RA, Grobler JA, Miller MD, Hazuda DJ, Hecht SM, Götte M.

J Biol Chem. 2015 Jan 16;290(3):1474-84. doi: 10.1074/jbc.M114.614305. Epub 2014 Oct 29.

11.

Resistance to HIV integrase strand transfer inhibitors: in vitro findings and clinical consequences.

Grobler JA, Hazuda DJ.

Curr Opin Virol. 2014 Oct;8:98-103. doi: 10.1016/j.coviro.2014.07.006. Epub 2014 Aug 14. Review.

PMID:
25128610
12.

Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.

Stachel SJ, Sanders JM, Henze DA, Rudd MT, Su HP, Li Y, Nanda KK, Egbertson MS, Manley PJ, Jones KL, Brnardic EJ, Green A, Grobler JA, Hanney B, Leitl M, Lai MT, Munshi V, Murphy D, Rickert K, Riley D, Krasowska-Zoladek A, Daley C, Zuck P, Kane SA, Bilodeau MT.

J Med Chem. 2014 Jul 10;57(13):5800-16. doi: 10.1021/jm5006429. Epub 2014 Jun 19.

PMID:
24914455
13.

Antiviral activity and in vitro mutation development pathways of MK-6186, a novel nonnucleoside reverse transcriptase inhibitor.

Lu M, Felock PJ, Munshi V, Hrin RC, Wang YJ, Yan Y, Munshi S, McGaughey GB, Gomez R, Anthony NJ, Williams TM, Grobler JA, Hazuda DJ, McKenna PM, Miller MD, Lai MT.

Antimicrob Agents Chemother. 2012 Jun;56(6):3324-35. doi: 10.1128/AAC.00102-12. Epub 2012 Mar 5.

14.

Impact of primer-induced conformational dynamics of HIV-1 reverse transcriptase on polymerase translocation and inhibition.

Auger A, Beilhartz GL, Zhu S, Cauchon E, Falgueyret JP, Grobler JA, Ehteshami M, Götte M, Melnyk RA.

J Biol Chem. 2011 Aug 26;286(34):29575-83. doi: 10.1074/jbc.M111.268235. Epub 2011 Jul 7.

15.

Strategies towards improving the pharmacokinetic profile of ε-substituted lysinol-derived HIV protease inhibitors.

Rajapakse HA, Walji AM, Moore KP, Zhu H, Mitra AW, Gregro AR, Tinney E, Burlein C, Touch S, Paton BL, Carroll SS, DiStefano DJ, Lai MT, Grobler JA, Sanchez RI, Williams TM, Vacca JP, Nantermet PG.

ChemMedChem. 2011 Feb 7;6(2):253-7. doi: 10.1002/cmdc.201000395. Epub 2010 Dec 29. No abstract available.

PMID:
21275047
16.

Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.

Williams PD, Staas DD, Venkatraman S, Loughran HM, Ruzek RD, Booth TM, Lyle TA, Wai JS, Vacca JP, Feuston BP, Ecto LT, Flynn JA, DiStefano DJ, Hazuda DJ, Bahnck CM, Himmelberger AL, Dornadula G, Hrin RC, Stillmock KA, Witmer MV, Miller MD, Grobler JA.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6754-7. doi: 10.1016/j.bmcl.2010.08.135. Epub 2010 Sep 24.

PMID:
20869872
17.

Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitors.

Lai MT, Lu M, Felock PJ, Hrin RC, Wang YJ, Yan Y, Munshi S, McGaughey GB, Tynebor RM, Tucker TJ, Williams TM, Grobler JA, Hazuda DJ, McKenna PM, Miller MD.

Antimicrob Agents Chemother. 2010 Nov;54(11):4812-24. doi: 10.1128/AAC.00829-10. Epub 2010 Aug 30.

18.

Structural basis for the inhibition of RNase H activity of HIV-1 reverse transcriptase by RNase H active site-directed inhibitors.

Su HP, Yan Y, Prasad GS, Smith RF, Daniels CL, Abeywickrema PD, Reid JC, Loughran HM, Kornienko M, Sharma S, Grobler JA, Xu B, Sardana V, Allison TJ, Williams PD, Darke PL, Hazuda DJ, Munshi S.

J Virol. 2010 Aug;84(15):7625-33. doi: 10.1128/JVI.00353-10. Epub 2010 May 19.

19.

Assessment of the susceptibility of mutant HIV-1 to antiviral agents.

Wang YJ, McKenna PM, Hrin R, Felock P, Lu M, Jones KG, Coburn CA, Grobler JA, Hazuda DJ, Miller MD, Lai MT.

J Virol Methods. 2010 May;165(2):230-7. doi: 10.1016/j.jviromet.2010.02.002. Epub 2010 Feb 11.

PMID:
20153375
20.

Purification of untagged HIV-1 reverse transcriptase by affinity chromatography.

Lu M, Ngo W, Mei Y, Munshi V, Burlein C, Loughran MH, Williams PD, Hazuda DJ, Miller MD, Grobler JA, Diamond TL, Lai MT.

Protein Expr Purif. 2010 Jun;71(2):231-9. doi: 10.1016/j.pep.2010.01.001. Epub 2010 Jan 8.

PMID:
20060474
21.

Scintillation proximity assays for mechanistic and pharmacological analyses of HIV-1 integration.

Grobler JA, Stillmock KA, Hazuda DJ.

Methods. 2009 Apr;47(4):249-53. doi: 10.1016/j.ymeth.2009.03.002. Epub 2009 Mar 12.

PMID:
19285556
22.

HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.

Grobler JA, Dornadula G, Rice MR, Simcoe AL, Hazuda DJ, Miller MD.

J Biol Chem. 2007 Mar 16;282(11):8005-10. Epub 2006 Dec 15.

23.

Replication fitness and NS5B drug sensitivity of diverse hepatitis C virus isolates characterized by using a transient replication assay.

Ludmerer SW, Graham DJ, Boots E, Murray EM, Simcoe A, Markel EJ, Grobler JA, Flores OA, Olsen DB, Hazuda DJ, LaFemina RL.

Antimicrob Agents Chemother. 2005 May;49(5):2059-69.

24.

A cell-based beta-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication.

Zuck P, Murray EM, Stec E, Grobler JA, Simon AJ, Strulovici B, Inglese J, Flores OA, Ferrer M.

Anal Biochem. 2004 Nov 15;334(2):344-55.

PMID:
15494142
25.

A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic properties.

Olsen DB, Eldrup AB, Bartholomew L, Bhat B, Bosserman MR, Ceccacci A, Colwell LF, Fay JF, Flores OA, Getty KL, Grobler JA, LaFemina RL, Markel EJ, Migliaccio G, Prhavc M, Stahlhut MW, Tomassini JE, MacCoss M, Hazuda DJ, Carroll SS.

Antimicrob Agents Chemother. 2004 Oct;48(10):3944-53.

26.

Identification of a key determinant of hepatitis C virus cell culture adaptation in domain II of NS3 helicase.

Grobler JA, Markel EJ, Fay JF, Graham DJ, Simcoe AL, Ludmerer SW, Murray EM, Migliaccio G, Flores OA.

J Biol Chem. 2003 May 9;278(19):16741-6. Epub 2003 Feb 28.

27.

Persistent replication of hepatitis C virus replicons expressing the beta-lactamase reporter in subpopulations of highly permissive Huh7 cells.

Murray EM, Grobler JA, Markel EJ, Pagnoni MF, Paonessa G, Simon AJ, Flores OA.

J Virol. 2003 Mar;77(5):2928-35.

28.

Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes.

Grobler JA, Stillmock K, Hu B, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J, Wai JS, Young S, Vacca J, Hazuda DJ.

Proc Natl Acad Sci U S A. 2002 May 14;99(10):6661-6. Epub 2002 May 7.

29.

Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.

Hazuda DJ, Felock P, Witmer M, Wolfe A, Stillmock K, Grobler JA, Espeseth A, Gabryelski L, Schleif W, Blau C, Miller MD.

Science. 2000 Jan 28;287(5453):646-50.

30.

Stability, activity and flexibility in alpha-lactalbumin.

Greene LH, Grobler JA, Malinovskii VA, Tian J, Acharya KR, Brew K.

Protein Eng. 1999 Jul;12(7):581-7.

PMID:
10436084
31.
32.

Protein kinase C and phospholipase C: bilayer interactions and regulation.

Hurley JH, Grobler JA.

Curr Opin Struct Biol. 1997 Aug;7(4):557-65. Review.

PMID:
9266179
33.

Similarity between C2 domain jaws and immunoglobulin CDRs.

Grobler JA, Hurley JH.

Nat Struct Biol. 1997 Apr;4(4):261-2. No abstract available.

PMID:
9095190
34.

C2 domain conformational changes in phospholipase C-delta 1.

Grobler JA, Essen LO, Williams RL, Hurley JH.

Nat Struct Biol. 1996 Sep;3(9):788-95.

PMID:
8784353
35.
37.

Second-site suppression of regulatory phosphorylation in Escherichia coli isocitrate dehydrogenase.

Chen R, Grobler JA, Hurley JH, Dean AM.

Protein Sci. 1996 Feb;5(2):287-95.

38.
39.

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