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George Kukolj

Academic title(s): 

Head of Infectious Disease Discovery, Janssen Biopharma Inc.

George Kukolj
Contact Information
Address: 

260 East Grand Avenue,
South San Francisco, CA
USA, 94080

Phone: 
650-635-5539
Email address: 
gkukolj [at] its.jnj.com
Division: 
Adjunct Members
Location: 
USA
Graduate supervision: 

NOT ACCEPTING GRADUATE OR POST-DOCTORAL听STUDENTS

Current research: 

Research interests include chronic infectious disease/immunology spanning early pre-clinical/ basic discovery through to clinical development. Drug discovery in the fields of anti-infectives, direct acting anti-virals and viral immunology across infectious disease indications. Interests also include anti-viral drug resistance, virus and host immune-modulatory mechanisms.
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Selected publications: 
  • Ferenci P, Asselah T, Foster GR, Zeuzem S, Sarrazin C, Moreno C, Ouzan D, Maevskaya M, Calinas F, Morano LE, Crespo J, Dufour JF, Bourli猫re M, Agarwal K, Forton D, Schuchmann M, Zehnter E, Nishiguchi S, Omata M, Kukolj G, Datsenko Y, Garcia M, Scherer J, Quinson AM, Stern JO; on behalf of the STARTVerso1 study group (2015). STARTVerso1: A randomized trial of faldaprevir plus pegylated interferon/ribavirin for chronic HCV genotype-1 infection.听J Hepatol.听2015 Jan 2. pii: S0168-8278(14)00953-2. doi: 10.1016/j.jhep.2014.12.024. Epub ahead of print.
  • Beaulieu PL, Anderson PC, Bethell R, B枚s M, Bousquet Y, Brochu C, Cordingley MG, Fazal G, Garneau M, Gillard JR, Kawai S, Marquis M, McKercher G, Poupart MA, Stammers T, Thavonekham B, Wernic D, Duan J, Kukolj G. (2014). Discovery of BI 207524, an Indole Diamide NS5B Thumb Pocket 1 Inhibitor with Improved Potency for the Potential Treatment of Chronic Hepatitis C Virus Infection.听J Med Chem.听2014 Dec 11;57(23):10130-43. doi: 10.1021/jm501532z.
  • El-Far M, Pellerin C, Pilote L, Fortin J-F, Lessard IAD, Peretz Y, Wardrop E, Salois P, Bethell RC, Cordingely, MG, Kukolj G. (2014). CD160 isoforms and regulation of CD4 and CD8 T-cell responses.听J. Trans Med听2014 Sep 2;12:217. doi: 10.1186/s12967-014-0217-y.
  • Martin B, Hennecke N, Lohmann V, Kayser A, Neumann-Haefelin C, Kukolj G, B枚cher WO, Thimme R. (2014).听Restoration of HCV-specific CD8+ T-cell function by interferon-free therapy.听J Hepatol.听2014 Sep;61(3):538-43. doi: 10.1016/j.jhep.2014.05.043. Epub 2014 Jun 4.听 (Editorial comment in same issue)
  • Berger KL, Triki I, Cartier M, Marquis M, Massariol MJ, B枚cher WO, Datsenko Y, Steinmann G, Scherer J, Stern JO, Kukolj G. (2014) Baseline Hepatitis C Virus (HCV) NS3 Polymorphisms and Their Impact on Clinical Studies of the HCV NS3 Protease Inhibitor Faldaprevir.听Antimicrob Agents Chemother.听2014 Feb; 58(2):698-705. doi: 10.1128/AAC.01976-13. Epub 2013 Nov 11.
  • Laplante SR, B枚s M, Brochu C, Chabot C, Coulombe R, Gillard JR, Jakalian A, Poirier M, Rancourt J, Stammers T, Thavonekham B, Beaulieu PL, Kukolj G, Tsantrizos YS. (2014) Conformation-Based Restrictions and Scaffold Replacements in the Design of Hepatitis C Virus Polymerase Inhibitors: Discovery of Deleobuvir (BI 207127).听J Med Chem.听2014 Mar 13;57(5):1845-54. doi: 10.1021/jm4011862. Epub 2013 Nov 11.
  • Zeuzem S, Soriano V, Asselah T, Bronowicki JP, Lohse AW, M眉llhaupt B, Schuchmann M, Bourli猫re M, Buti M, Roberts SK, Gane EJ, Stern JO, Vinisko R, Kukolj G, Gallivan JP, B枚cher WO, Mensa FJ. (2013) Faldaprevir and deleobuvir for HCV genotype 1 infection.听N Engl J Med.听2013 Aug 15;369(7):630-639.
  • Berger KL, Lagac茅 L, Triki I, Cartier M, Marquis M, Lawetz C, Bethell R, Scherer J, Kukolj G. (2013) Viral resistance in hepatitis C virus genotype 1-infected patients receiving the NS3 protease inhibitor Faldaprevir (BI 201335) in a phase 1b multiple-rising-dose study.听Antimicrob Agents Chemother.听2013 Oct;57(10):4928-4936.
  • Larrey D, Lohse AW, Trepo C, Bronowicki JP, Arast茅h K, Bourli猫re M, Calleja JL, Stern JO, Nehmiz G, Abdallah N, Berger KL, Marquis M, Steffgen J, Kukolj G; BI 207127 Study Group (2013). Antiviral effect, safety, and pharmacokinetics of five-day oral administration of Deleobuvir (BI 207127), an investigational hepatitis C virus RNA polymerase inhibitor, in patients with chronic hepatitis C.听听Antimicrob Agents Chemother.听2013 Oct;57(10):4727-4735.
  • Sulkowski, M.S., Asselah,T., Lalezari,J., Ferenci,P., Fainboim,H., Leggett,B., Bessone,F., Mauss,S., Heo,J., Datsenko,Y., Stern,J.O., Kukolj,G., Scherer,J., Nehmiz,G., Steinmann,G.G., Bocher,W.O. (2013) Faldaprevir combined with peginterferon alfa-2a and ribavirin in treatment-naive patients with chronic genotype-1 HCV: SILEN-C1 trial.听Hepatology听2013 Jun;57(6):2143-2154.
  • O'Meara, J. A., Lemke,C.T., Godbout,C., Kukolj,G., Lagace,L., Moreau,B., Thibeault,D., White,P.W., Llinas-Brunet,M. (2013) Molecular Mechanism by Which a Potent Hepatitis C Virus NS3-NS4A Protease Inhibitor Overcomes Emergence of Resistance.听J.Biol.Chem.听2013 Feb;288 (8) : 5673-5781.
  • Vaillancourt, F.H., Brault, M., Pilote, L., Uyttersprot, N., Gaillard, E.T., Stoltz, J.H., Knight, B.L., Pantages, L., McFarland, M., Breitfelder, S., Chiu, T.T., Mahrouche, L., Faucher, A.M., Cartier, M., Cordingley, M.G., Bethell, R.C., Jiang, H., White, P.W., Kukolj, G. (2012) Evaluation of phosphatidylinositol-4-kinase III伪 as a hepatitis C virus drug target.听J Virol.听2012 Nov;86(21):11595-11607.
  • Larrey, D., Lohse, A.W., de Ledinghen, V., Trepo, C., Gerlach, T., Zarski, J,P., Tran, A., Mathurin, P., Thimme, R., Arast茅h, K., Trautwein, C., Cerny, A., Dikopoulos, N., Schuchmann, M., Heim, M.H., Gerken, G., Stern, J.O., Wu, K., Abdallah, N., Girlich, B., Scherer, J., Berger, F., Marquis, M., Kukolj, G., B枚cher, W.O., Steffgen, J. (2012) Rapid and strong antiviral activity of the non-nucleosidic NS5B polymerase inhibitor BI 207127 in combination with peginterferon alfa 2a and ribavirin.听J Hepatol.听2012 Jul;57(1):39-46.
  • Lagac茅, L., White, P.W., Bousquet, C., Dansereau, N., D么, F., Llinas-Brunet, M., Marquis, M., Massariol, M.J., Maurice, R., Spickler, C., Thibeault, D., Triki, I., Zhao, S., Kukolj, G.. (2012) In vitro resistance profile of the HCV NS3 protease inhibitor BI 201335.听Antimicrob Agents Chemother.听2011 Oct 24. [Epub ahead of print] Antimicrob Agents Chemother. 2012 Jan;56(1):569-72.
  • Zeuzem, S., Asselah, T., Angus, P., Zarski, J.P., Larrey, D., M眉llhaupt, B., Gane, E., Schuchmann, M., Lohse, A., Pol, S., Bronowicki, J.P., Roberts, S., Arasteh, K., Zoulim, F., Heim, M., Stern, J.O., Kukolj, G., Nehmiz, G., Haefner, C., Boecher, W.O. (2011) Efficacy of the Protease Inhibitor BI 201335, Polymerase Inhibitor BI 207127, and Ribavirin in Patients With Chronic HCV Infection.听Gastroenterology.听2011 Dec;141(6):2047-55
  • Manns, M.P, Bourli猫re, M., Benhamou, Y., Pol, S., Bonacini, M., Trepo, C., Wright, D., Berg, T., Calleja, J.L., White, P.W., Stern, J.O., Steinmann, G., Yong, C.L., Kukolj, G., Scherer, J., Boecher, W.O. (2011) Potency, safety, and pharmacokinetics of the NS3/4A protease inhibitor BI201335 in patients with chronic HCV genotype-1 infection.听J Hepatol.听2011 Jun;54(6):1114-22.
  • White, P.W., Llin脿s-Brunet, M., Amad, M., Bethell, R.C., Bolger, G., Cordingley, M,G,, Duan, J., Garneau, M., Lagac茅, L., Thibeault, D., Kukolj, G. (2010) Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.听Antimicrob Agents Chemother.听2010 Nov;54(11):4611-8.
  • Bethell, R., Kukolj, G. and White, P.W. (2009)听Inhibition of the replicative cycle of hepatitis C virus.听Nature Reviews Microbiology听Vol. 7 (6): Poster
  • Vaillancourt, F.H., Pilote, L., Cartier, M., Lippens, J., Liuzzi, M., Bethell, R.C., Cordingley, M.G., Kukolj, G. (2009) Identification of a lipid kinase as a host factor involved in hepatitis C virus RNA replication.听Virology听387(1):5-10.
  • Erhardt, A., Deterding, K., Benhamou, Y., Reiser, M., Forns, X., Pol, S., Calleja, J.L., Ross, S., Spangenberg, H.C., Garcia-Samaniego, J., Fuchs, M., Enr铆quez, J., Wiegand, J., Stern, J.,O. Wu, K., Kukolj, G., Marquis, M., Beaulieu, P.L., Nehmiz, G., Steffgen, J. BILB 1941 Study Group. (2009) Safety, pharmacokinetics and antiviral effect of BILB 1941, a novel hepatitis C virus RNA polymerase inhibitor, after 5 days oral treatment.听Antivir Ther.听14(1):23-32.
  • Kukolj, G., McGibbon, G.A., McKercher, G., Marquis, M., Lef猫bvre, S.,听 Thauvette, L., Gauthier, J.,听 Goulet, S., Poupart, M.-A. and Beaulieu, P.L. (2005) Binding-site characterization and resistance to a class of non-nucleoside inhibitors of the HCV NS5B polymerase.听听J Biol Chem.听280(47):39260-39267. doi:10.1074/jbc.M506407200
  • Ali, S. and Kukolj, G. (2005) Interferon Regulatory Factor-3 independent double-stranded RNA induced inhibition of Hepatitis C Virus replicons in Human Embryonic Kidney 293 cells.听J Virol.听79 (5):3174-3178.
  • Beaulieu P.L., Bos M., Bousquet Y., Fazal G., Gauthier J., Gillard J., Goulet S., Marquis, M., Pellerin, C., Poupart M.A., Valois S., Kukolj G. (2004) Non-nulceoside benzimidazole-based allosteric inhibitors of the hepatitis C virus polymerase: Inhibition of subgenomic HCV RNA replication in Huh-7 cells.听J Med Chem.听47(27):6884-6892.
  • LaPlante S.R., Jakalian A., Aubry N., Bousquet Y., Ferland J.M., Gillard J., Lefebvre S., Poirier M., Tsantrizos Y.S., Kukolj G., Beaulieu P.L. (2004) Binding mode determination of benzimidazole inhibitors of the hepatitis C virus RNA polymerase by a structure and dynamics strategy.听Angew Chem Int Ed Engl.听43(33):4306-11.
  • McKercher, G., Beaulieu P.L., Lamarre, D., LaPlante, S., Lefebvre, S., Pellerin, C., Thauvette,听 L., Kukolj, G. (2004) Specific inhibitors of HCV polymerase identified using an NS5B with lower affinity for template/primer substrate.听Nucleic Acids Res.听32: 422-31.
  • Ali, S., Pellerin, C., Lamarre, D., and Kukolj, G. (2004) Hepatitis C Virus Subgenomic Replicons in the Human Embryonic Kidney 293 Cell Line.听听J. Virology.听78: 491-501.
  • Lamarre D., Anderson P.C., Bailey M., Beaulieu P., Bolger G., Bonneau P., Bos M., Cameron D.R., Cartier M., Cordingley M.G., Faucher A.M., Goudreau N., Kawai S.H., Kukolj G., Lagac茅 L., LaPlante S.R., Narjes H., Poupart M.A., Rancourt J., Sentjens R.E., St. George R., Simoneau B., Steinmann G., Thibeault D., Tsantrizos Y.S., Weldon S.M., Yong C.L., Llinas-Brunet M. (2003) An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus.听Nature.听426:186-189
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