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Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition.

Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, Brendza KM, Lutz JD, Keegan KS, Ray AS, Schultz BE, Sakowicz R, Feng JY.

Biochim Biophys Acta Gen Subj. 2020 Jan 14:129531. doi: 10.1016/j.bbagen.2020.129531. [Epub ahead of print]


Phytoextracts As Antibacterials - A Review.

Chandra G, Mukherjee D, Ray AS, Chatterjee S, Bhattacharjee I.

Curr Drug Discov Technol. 2019 Nov 5. doi: 10.2174/1570163816666191106103730. [Epub ahead of print]


Improved Diagnostic Yield and Specimen Quality with EBUS-Guided Forceps Biopsies: A Retrospective Analysis.

Ray AS, Li C, Murphy TE, Cai G, Araujo KL, Bramley K, DeBiasi EM, Pisani MA, Cortopassi IO, Puchalski JT.

Ann Thorac Surg. 2019 Oct 5. pii: S0003-4975(19)31556-5. doi: 10.1016/j.athoracsur.2019.08.106. [Epub ahead of print]


Polyphenol enriched ethanolic extract of Cajanus scarabaeoides (L.) Thouars exerts potential antifilarial activity by inducing oxidative stress and programmed cell death.

Ray AS, Joardar N, Mukherjee S, Rahaman CH, Sinha Babu SP.

PLoS One. 2018 Dec 6;13(12):e0208201. doi: 10.1371/journal.pone.0208201. eCollection 2018.


Safety and Tolerability of Vacuum Versus Manual Drainage During Thoracentesis: A Randomized Trial.

Senitko M, Ray AS, Murphy TE, Araujo KLB, Bramley K, DeBiasi EM, Pisani MA, Cameron K, Puchalski JT.

J Bronchology Interv Pulmonol. 2019 Jul;26(3):166-171. doi: 10.1097/LBR.0000000000000556.


Inhibition of Acetyl-CoA Carboxylase by Phosphorylation or the Inhibitor ND-654 Suppresses Lipogenesis and Hepatocellular Carcinoma.

Lally JSV, Ghoshal S, DePeralta DK, Moaven O, Wei L, Masia R, Erstad DJ, Fujiwara N, Leong V, Houde VP, Anagnostopoulos AE, Wang A, Broadfield LA, Ford RJ, Foster RA, Bates J, Sun H, Wang T, Liu H, Ray AS, Saha AK, Greenwood J, Bhat S, Harriman G, Miao W, Rocnik JL, Westlin WF, Muti P, Tsakiridis T, Harwood HJ Jr, Kapeller R, Hoshida Y, Tanabe KK, Steinberg GR, Fuchs BC.

Cell Metab. 2019 Jan 8;29(1):174-182.e5. doi: 10.1016/j.cmet.2018.08.020. Epub 2018 Sep 20.


Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance.

Zamek-Gliszczynski MJ, Taub ME, Chothe PP, Chu X, Giacomini KM, Kim RB, Ray AS, Stocker SL, Unadkat JD, Wittwer MB, Xia C, Yee SW, Zhang L, Zhang Y; International Transporter Consortium.

Clin Pharmacol Ther. 2018 Nov;104(5):890-899. doi: 10.1002/cpt.1112. Epub 2018 Aug 8. Review.


GS-0976 Reduces Hepatic Steatosis and Fibrosis Markers in Patients With Nonalcoholic Fatty Liver Disease.

Loomba R, Kayali Z, Noureddin M, Ruane P, Lawitz EJ, Bennett M, Wang L, Harting E, Tarrant JM, McColgan BJ, Chung C, Ray AS, Subramanian GM, Myers RP, Middleton MS, Lai M, Charlton M, Harrison SA.

Gastroenterology. 2018 Nov;155(5):1463-1473.e6. doi: 10.1053/j.gastro.2018.07.027. Epub 2018 Jul 27.


Nucleotide Prodrug Containing a Nonproteinogenic Amino Acid To Improve Oral Delivery of a Hepatitis C Virus Treatment.

Feng JY, Wang T, Park Y, Babusis D, Birkus G, Xu Y, Voitenleitner C, Fenaux M, Yang H, Eng S, Tirunagari N, Kirschberg T, Cho A, Ray AS.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00620-18. doi: 10.1128/AAC.00620-18. Print 2018 Aug.


Acetyl-CoA Carboxylase Inhibition Reverses NAFLD and Hepatic Insulin Resistance but Promotes Hypertriglyceridemia in Rodents.

Goedeke L, Bates J, Vatner DF, Perry RJ, Wang T, Ramirez R, Li L, Ellis MW, Zhang D, Wong KE, Beysen C, Cline GW, Ray AS, Shulman GI.

Hepatology. 2018 Dec;68(6):2197-2211. doi: 10.1002/hep.30097.


ITC Commentary on Metformin Clinical Drug-Drug Interaction Study Design That Enables an Efficacy- and Safety-Based Dose Adjustment Decision.

Zamek-Gliszczynski MJ, Chu X, Cook JA, Custodio JM, Galetin A, Giacomini KM, Lee CA, Paine MF, Ray AS, Ware JA, Wittwer MB, Zhang L; International Transporter Consortium.

Clin Pharmacol Ther. 2018 Nov;104(5):781-784. doi: 10.1002/cpt.1082. Epub 2018 May 15.


Acetyl-CoA Carboxylase Inhibitor GS-0976 for 12 Weeks Reduces Hepatic De Novo Lipogenesis and Steatosis in Patients With Nonalcoholic Steatohepatitis.

Lawitz EJ, Coste A, Poordad F, Alkhouri N, Loo N, McColgan BJ, Tarrant JM, Nguyen T, Han L, Chung C, Ray AS, McHutchison JG, Subramanian GM, Myers RP, Middleton MS, Sirlin C, Loomba R, Nyangau E, Fitch M, Li K, Hellerstein M.

Clin Gastroenterol Hepatol. 2018 Dec;16(12):1983-1991.e3. doi: 10.1016/j.cgh.2018.04.042. Epub 2018 Apr 26.


Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease.

Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR.

mBio. 2018 Mar 6;9(2). pii: e00221-18. doi: 10.1128/mBio.00221-18.


Sofosbuvir and Ribavirin Liver Pharmacokinetics in Patients Infected with Hepatitis C Virus.

Babusis D, Curry MP, Kirby B, Park Y, Murakami E, Wang T, Mathias A, Afdhal N, McHutchison JG, Ray AS.

Antimicrob Agents Chemother. 2018 Apr 26;62(5). pii: e02587-17. doi: 10.1128/AAC.02587-17. Print 2018 May.


Transporter Expression in Noncancerous and Cancerous Liver Tissue from Donors with Hepatocellular Carcinoma and Chronic Hepatitis C Infection Quantified by LC-MS/MS Proteomics.

Billington S, Ray AS, Salphati L, Xiao G, Chu X, Humphreys WG, Liao M, Lee CA, Mathias A, Hop CECA, Rowbottom C, Evers R, Lai Y, Kelly EJ, Prasad B, Unadkat JD.

Drug Metab Dispos. 2018 Feb;46(2):189-196. doi: 10.1124/dmd.117.077289. Epub 2017 Nov 14.


Beyond drug-drug interactions: effects of transporter inhibition on endobiotics, nutrients and toxins.

Lepist EI, Ray AS.

Expert Opin Drug Metab Toxicol. 2017 Oct;13(10):1075-1087. doi: 10.1080/17425255.2017.1372425. Epub 2017 Aug 29. Review.


Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses.

Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS.

Sci Transl Med. 2017 Jun 28;9(396). pii: eaal3653. doi: 10.1126/scitranslmed.aal3653.


Larvicidal activity of phytosteroid compounds from leaf extract of Solanum nigrum against Culex vishnui group and Anopheles subpictus.

Rawani A, Ray AS, Ghosh A, Sakar M, Chandra G.

BMC Res Notes. 2017 Mar 23;10(1):135. doi: 10.1186/s13104-017-2460-9.


Discovery of a 2'-fluoro-2'-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties.

Kirschberg TA, Metobo S, Clarke MO, Aktoudianakis V, Babusis D, Barauskas O, Birkus G, Butler T, Byun D, Chin G, Doerffler E, Edwards TE, Fenaux M, Lee R, Lew W, Mish MR, Murakami E, Park Y, Squires NH, Tirunagari N, Wang T, Whitcomb M, Xu J, Yang H, Ye H, Zhang L, Appleby TC, Feng JY, Ray AS, Cho A, Kim CU.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1840-1847. doi: 10.1016/j.bmcl.2017.02.037. Epub 2017 Feb 20.


GS-5734 and its parent nucleoside analog inhibit Filo-, Pneumo-, and Paramyxoviruses.

Lo MK, Jordan R, Arvey A, Sudhamsu J, Shrivastava-Ranjan P, Hotard AL, Flint M, McMullan LK, Siegel D, Clarke MO, Mackman RL, Hui HC, Perron M, Ray AS, Cihlar T, Nichol ST, Spiropoulou CF.

Sci Rep. 2017 Mar 6;7:43395. doi: 10.1038/srep43395.


Tenofovir alafenamide (TAF) does not deplete mitochondrial DNA in human T-cell lines at intracellular concentrations exceeding clinically relevant drug exposures.

Stray KM, Park Y, Babusis D, Callebaut C, Cihlar T, Ray AS, Perron M.

Antiviral Res. 2017 Apr;140:116-120. doi: 10.1016/j.antiviral.2017.01.014. Epub 2017 Jan 26.


Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.

Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL.

J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14.


Role of Mitochondrial Toxicity in BMS-986094-Induced Toxicity.

Feng JY, Tay CH, Ray AS.

Toxicol Sci. 2017 Jan;155(1):2. doi: 10.1093/toxsci/kfw224. Epub 2016 Nov 1. No abstract available.


Interaction of 2,4-Diaminopyrimidine-Containing Drugs Including Fedratinib and Trimethoprim with Thiamine Transporters.

Giacomini MM, Hao J, Liang X, Chandrasekhar J, Twelves J, Whitney JA, Lepist EI, Ray AS.

Drug Metab Dispos. 2017 Jan;45(1):76-85. Epub 2016 Nov 1. Erratum in: Drug Metab Dispos. 2017 Nov;45(11):1146-1147.


Transporter Expression in Liver Tissue from Subjects with Alcoholic or Hepatitis C Cirrhosis Quantified by Targeted Quantitative Proteomics.

Wang L, Collins C, Kelly EJ, Chu X, Ray AS, Salphati L, Xiao G, Lee C, Lai Y, Liao M, Mathias A, Evers R, Humphreys W, Hop CE, Kumer SC, Unadkat JD.

Drug Metab Dispos. 2016 Nov;44(11):1752-1758. Epub 2016 Aug 19.


Chemoprophylaxis With Oral Emtricitabine and Tenofovir Alafenamide Combination Protects Macaques From Rectal Simian/Human Immunodeficiency Virus Infection.

Massud I, Mitchell J, Babusis D, Deyounks F, Ray AS, Rooney JF, Heneine W, Miller MD, García-Lerma JG.

J Infect Dis. 2016 Oct 1;214(7):1058-62. doi: 10.1093/infdis/jiw312. Epub 2016 Jul 27.


Renal Transporter-Mediated Drug-Drug Interactions: Are They Clinically Relevant?

Lepist EI, Ray AS.

J Clin Pharmacol. 2016 Jul;56 Suppl 7:S73-81. doi: 10.1002/jcph.735. Review.


Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.

Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S.

Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Erratum in: ACS Chem Biol. 2016 May 20;11(5):1463.


Involvement of Drug Transporters in Organ Toxicity: The Fundamental Basis of Drug Discovery and Development.

Cheng Y, El-Kattan A, Zhang Y, Ray AS, Lai Y.

Chem Res Toxicol. 2016 Apr 18;29(4):545-63. doi: 10.1021/acs.chemrestox.5b00511. Epub 2016 Mar 8. Review.


Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus.

Ray AS, Fordyce MW, Hitchcock MJ.

Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27. Review.


Role of Mitochondrial RNA Polymerase in the Toxicity of Nucleotide Inhibitors of Hepatitis C Virus.

Feng JY, Xu Y, Barauskas O, Perry JK, Ahmadyar S, Stepan G, Yu H, Babusis D, Park Y, McCutcheon K, Perron M, Schultz BE, Sakowicz R, Ray AS.

Antimicrob Agents Chemother. 2015 Nov 23;60(2):806-17. doi: 10.1128/AAC.01922-15. Print 2016 Feb.


Metformin Is a Substrate and Inhibitor of the Human Thiamine Transporter, THTR-2 (SLC19A3).

Liang X, Chien HC, Yee SW, Giacomini MM, Chen EC, Piao M, Hao J, Twelves J, Lepist EI, Ray AS, Giacomini KM.

Mol Pharm. 2015 Dec 7;12(12):4301-10. doi: 10.1021/acs.molpharmaceut.5b00501. Epub 2015 Nov 16.


Synthesis of 1'-C-cyano pyrimidine nucleosides and characterization as HCV polymerase inhibitors.

Kirschberg TA, Mish M, Squires NH, Zonte S, Aktoudianakis E, Metobo S, Butler T, Ju X, Cho A, Ray AS, Kim CU.

Nucleosides Nucleotides Nucleic Acids. 2015;34(11):763-85. doi: 10.1080/15257770.2015.1075550. Epub 2015 Sep 23.


Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy.

Murakami E, Wang T, Park Y, Hao J, Lepist EI, Babusis D, Ray AS.

Antimicrob Agents Chemother. 2015;59(6):3563-9. doi: 10.1128/AAC.00128-15. Epub 2015 Apr 13.


Viral replication. Structural basis for RNA replication by the hepatitis C virus polymerase.

Appleby TC, Perry JK, Murakami E, Barauskas O, Feng J, Cho A, Fox D 3rd, Wetmore DR, McGrath ME, Ray AS, Sofia MJ, Swaminathan S, Edwards TE.

Science. 2015 Feb 13;347(6223):771-5. doi: 10.1126/science.1259210.


Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors.

Kirschberg TA, Mish MR, Zhang L, Squires NH, Wang KY, Cho A, Feng JY, Fenaux M, Babusis D, Park Y, Ray AS, Kim CU.

Bioorg Med Chem Lett. 2015 Mar 1;25(5):1040-3. doi: 10.1016/j.bmcl.2015.01.021. Epub 2015 Jan 17.


A pharmacogenetic candidate gene study of tenofovir-associated Fanconi syndrome.

Dahlin A, Wittwer M, de la Cruz M, Woo JM, Bam R, Scharen-Guivel V, Flaherty J, Ray AS, Cihlar T, Gupta SK, Giacomini KM.

Pharmacogenet Genomics. 2015 Feb;25(2):82-92. doi: 10.1097/FPC.0000000000000110.


Early Trophic Enteral Nutrition Is Associated With Improved Outcomes in Mechanically Ventilated Patients With Septic Shock: A Retrospective Review.

Patel JJ, Kozeniecki M, Biesboer A, Peppard W, Ray AS, Thomas S, Jacobs ER, Nanchal R, Kumar G.

J Intensive Care Med. 2016 Aug;31(7):471-7. doi: 10.1177/0885066614554887. Epub 2014 Oct 14.


Preparation and biological evaluation of 1'-cyano-2'-C-methyl pyrimidine nucleosides as HCV NS5B polymerase inhibitors.

Mish MR, Cho A, Kirschberg T, Xu J, Zonte CS, Fenaux M, Park Y, Babusis D, Feng JY, Ray AS, Kim CU.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3092-5. doi: 10.1016/j.bmcl.2014.05.015. Epub 2014 May 22.


Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat.

Lepist EI, Zhang X, Hao J, Huang J, Kosaka A, Birkus G, Murray BP, Bannister R, Cihlar T, Huang Y, Ray AS.

Kidney Int. 2014 Aug;86(2):350-7. doi: 10.1038/ki.2014.66. Epub 2014 Mar 19.


Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes.

Lepist EI, Gillies H, Smith W, Hao J, Hubert C, St Claire RL 3rd, Brouwer KR, Ray AS.

PLoS One. 2014 Jan 30;9(1):e87548. doi: 10.1371/journal.pone.0087548. eCollection 2014.


GS-9219/VDC-1101--a prodrug of the acyclic nucleotide PMEG has antitumor activity in spontaneous canine multiple myeloma.

Thamm DH, Vail DM, Kurzman ID, Babusis D, Ray AS, Sousa-Powers N, Tumas DB.

BMC Vet Res. 2014 Jan 25;10:30. doi: 10.1186/1746-6148-10-30.


Inhibition of hepatitis C virus replication by GS-6620, a potent C-nucleoside monophosphate prodrug.

Feng JY, Cheng G, Perry J, Barauskas O, Xu Y, Fenaux M, Eng S, Tirunagari N, Peng B, Yu M, Tian Y, Lee YJ, Stepan G, Lagpacan LL, Jin D, Hung M, Ku KS, Han B, Kitrinos K, Perron M, Birkus G, Wong KA, Zhong W, Kim CU, Carey A, Cho A, Ray AS.

Antimicrob Agents Chemother. 2014;58(4):1930-42. doi: 10.1128/AAC.02351-13. Epub 2014 Jan 13.


Metabolism and pharmacokinetics of the anti-hepatitis C virus nucleotide prodrug GS-6620.

Murakami E, Wang T, Babusis D, Lepist EI, Sauer D, Park Y, Vela JE, Shih R, Birkus G, Stefanidis D, Kim CU, Cho A, Ray AS.

Antimicrob Agents Chemother. 2014;58(4):1943-51. doi: 10.1128/AAC.02350-13. Epub 2014 Jan 13.


Pharmacokinetics of cobicistat boosted-elvitegravir administered in combination with rosuvastatin.

Custodio JM, Wang H, Hao J, Lepist EI, Ray AS, Andrews J, Ling KH, Cheng A, Kearney BP, Ramanathan S.

J Clin Pharmacol. 2014 Jun;54(6):649-56. doi: 10.1002/jcph.256. Epub 2014 Jan 17.


Evaluation of the effect of cobicistat on the in vitro renal transport and cytotoxicity potential of tenofovir.

Stray KM, Bam RA, Birkus G, Hao J, Lepist EI, Yant SR, Ray AS, Cihlar T.

Antimicrob Agents Chemother. 2013 Oct;57(10):4982-9. doi: 10.1128/AAC.00712-13. Epub 2013 Jul 29.


Evaluation of 2'-α-fluorine modified nucleoside phosphonates as potential inhibitors of HCV polymerase.

Parrish JP, Lee SK, Boojamra CG, Hui H, Babusis D, Brown B, Shih IH, Feng JY, Ray AS, Mackman RL.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3354-7. doi: 10.1016/j.bmcl.2013.03.095. Epub 2013 Apr 2.


Discovery of the first C-nucleoside HCV polymerase inhibitor (GS-6620) with demonstrated antiviral response in HCV infected patients.

Cho A, Zhang L, Xu J, Lee R, Butler T, Metobo S, Aktoudianakis V, Lew W, Ye H, Clarke M, Doerffler E, Byun D, Wang T, Babusis D, Carey AC, German P, Sauer D, Zhong W, Rossi S, Fenaux M, McHutchison JG, Perry J, Feng J, Ray AS, Kim CU.

J Med Chem. 2014 Mar 13;57(5):1812-25. doi: 10.1021/jm400201a. Epub 2013 May 1.


Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate.

Piao D, Basavapathruni A, Iyidogan P, Dai G, Hinz W, Ray AS, Murakami E, Feng JY, You F, Dutschman GE, Austin DJ, Parker KA, Anderson KS.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1511-8. doi: 10.1016/j.bmcl.2012.12.015. Epub 2012 Dec 20.


Sensitivity of mitochondrial transcription and resistance of RNA polymerase II dependent nuclear transcription to antiviral ribonucleosides.

Arnold JJ, Sharma SD, Feng JY, Ray AS, Smidansky ED, Kireeva ML, Cho A, Perry J, Vela JE, Park Y, Xu Y, Tian Y, Babusis D, Barauskus O, Peterson BR, Gnatt A, Kashlev M, Zhong W, Cameron CE.

PLoS Pathog. 2012;8(11):e1003030. doi: 10.1371/journal.ppat.1003030. Epub 2012 Nov 15.

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