Development and evaluation of a FACS-based medium-throughput assay for HCV entry inhibitors

Journal of Biomolecular Screening

Volumn 14, Issue 6, 2009, Pages 620-626

  Ziegler, Sigrid ^a   Kronenberger, Bernd ^b   Albrecht, Beatrice A M ^a   Kaul, Artur ^c   Gamer, Anna Lena ^c   Klein, Christian D ^a   Hartmann, Rolf W ^a,c  

^a SAARLAND UNIVERSITY   (Germany)

^b Medizinische Klinik I   (Germany)

^c UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

CD81 LEL; HCV entry inhibitors; HCV E2 protein; Protein protein interaction inhibitors

Indexed keywords

ANTIVIRUS AGENT; CANNABIGEROL; CD81 ANTIGEN; EPIGALLOCATECHIN; GLYCOPROTEIN E2; LIGAND; LUCIFERASE; NORDIHYDROGUAIARETIC ACID; OUABAIN; SALICYLIC ACID BENZYL ESTER; TAMOXIFEN; TERFENADINE; XANTHOHUMOL;

ARTICLE; BINDING SITE; DRUG DETERMINATION; DRUG EFFICACY; DRUG POTENCY; EVALUATION; FLOW CYTOMETRY; FLUORESCENCE ACTIVATED CELL SORTING; HEPATITIS C VIRUS; HIGH THROUGHPUT SCREENING; HOST CELL; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; REPORTER GENE; VIRUS GENOME;

ANTIBODIES; ANTIVIRAL AGENTS; BIOLOGICAL ASSAY; CELL LINE, TUMOR; FLOW CYTOMETRY; FLUORESCENCE; HEPACIVIRUS; HUMANS; PHYCOERYTHRIN; STAINING AND LABELING; TEMPERATURE; TIME FACTORS; VIRUS INTERNALIZATION;

HEPATITIS C VIRUS;

EID: 67651024151     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057109337161     Document Type: Article

References (29)

1. World Health Organization: Initiative for vaccine research (IVR). http://www.who.int/vaccine-research/diseases/viral-cancers/en/index2.html. 2006.
2. Sy T., Jamal MM: Epidemiology of hepatitis C virus (HCV) infection. Int J Med Sci 2006 ; 3 (2). 41-46.
3. Centers for Disease Control and Prevention: Viral hepatitis. http://www.cdc.gov/ncidod/diseases/hepatitis/c/fact.htm. 2005.
4. McHutchison JG, Gordon SC, Schiff ER, Shiffman ML, Lee WM, Rustgi VK, et al. Interferon alfa-2b alone or in combination with ribavirin as initial treatment for chronic hepatitis C. Hepatitis Interventional Therapy Group. N Engl J Med 1998 ; 339 (21). 1485-1492.
5. Hadziyannis SJ, Sette H. Jr., Morgan TR, Balan V., Diago M., Marcellin P., et al. Peginterferon-alpha2a and ribavirin combination therapy in chronic hepatitis C: a randomized study of treatment duration and ribavirin dose. Ann Intern Med 2004 ; 140 (5). 346-355.
6. Chen SH, Tan SL: Discovery of small-molecule inhibitors of HCV NS3-4A protease as potential therapeutic agents against HCV infection. Curr Med Chem 2005 ; 12 (20). 2317-2342.
7. Goudreau N., Llinas-Brunet M.: The therapeutic potential of NS3 protease inhibitors in HCV infection. Expert Opin Investig Drugs 2005 ; 14 (9). 1129-1144.
8. Kwong AD, Kim JL, Rao G., Lipovsek D., Raybuck SA: Hepatitis C virus NS3/4A protease. Antiviral Res 1999 ; 41 (1). 67-84.
9. Chen RY, Kilby JM, Saag MS: Enfuvirtide. Expert Opin Investig Drugs 2002 ; 11 (12). 1837-1843.
10. Bartosch B., Vitelli A., Granier C., Goujon C., Dubuisson J., Pascale S., et al. Cell entry of hepatitis C virus requires a set of co-receptors that include the CD81 tetraspanin and the SR-B1 scavenger receptor. J Biol Chem 2003 ; 278 (43). 41624-41630.
11. Bartosch B., Dubuisson J., Cosset FL: Infectious hepatitis C virus pseudo-particles containing functional E1-E2 envelope protein complexes. J Exp Med 2003 ; 197 (5). 633-642.
12. Drummer HE, Maerz A., Poumbourios P.: Cell surface expression of functional hepatitis C virus E1 and E2 glycoproteins. FEBS Lett 2003 ; 546 (2-3). 385-390.
13. Drummer HE, Wilson KA, Poumbourios P.: Identification of the hepatitis C virus E2 glycoprotein binding site on the large extracellular loop of CD81. J Virol 2002 ; 76 (21). 11143-11147.
14. Higginbottom A., Quinn ER, Kuo CC, Flint M., Wilson LH, Bianchi E., et al. Identification of amino acid residues in CD81 critical for interaction with hepatitis C virus envelope glycoprotein E2. J Virol 2000 ; 74 (8). 3642-3649.
15. Patel AH, Wood J., Penin F., Dubuisson J., McKeating JA: Construction and characterization of chimeric hepatitis C virus E2 glycoproteins: analysis of regions critical for glycoprotein aggregation and CD81 binding. J Gen Virol 2000 ; 81 (pt 12). 2873-2883.
16. Pileri P., Uematsu Y., Campagnoli S., Galli G., Falugi F., Petracca R., et al. Binding of hepatitis C virus to CD81. Science 1998 ; 282 (5390). 938-941.
17. Levy S., Todd SC, Maecker HT: CD81 (TAPA-1): a molecule involved in signal transduction and cell adhesion in the immune system. Annu Rev Immunol 1998 ; 16: 89-109.
18. Pawlotsky JM: Hepatitis C virus genetic variability: pathogenic and clinical implications. Clin Liver Dis 2003 ; 7 (1). 45-66.
19. Rosa D., Campagnoli S., Moretto C., Guenzi E., Cousens L., Chin M., et al. A quantitative test to estimate neutralizing antibodies to the hepatitis C virus: cytofluorimetric assessment of envelope glycoprotein 2 binding to target cells. Proc Natl Acad Sci U S A 1996 ; 93 (5). 1759-1763.
20. Blight KJ, McKeating JA, Rice CM: Highly permissive cell lines for subgenomic and genomic hepatitis C virus RNA replication. J Virol 2002 ; 76 (24). 13001-13014.
21. Koutsoudakis G., Kaul A., Steinmann E., Kallis S., Lohmann V., Pietschmann T., et al. Characterization of the early steps of hepatitis C virus infection by using luciferase reporter viruses. J Virol 2006 ; 80 (11). 5308-5320.
22. Kato T., Date T., Miyamoto M., Furusaka A., Tokushige K., Mizokami M., et al. Efficient replication of the genotype 2a hepatitis C virus subgenomic replicon. Gastroenterology 2003 ; 125 (6). 1808-1817.
23. Kaul A., Woerz I., Meuleman P., Leroux-Roels G., Bartenschlager R.: Cell culture adaptation of hepatitis C virus and in vivo viability of an adapted variant. J Virol 2007 ; 81 (23). 13168-13179. (Pubitemid 350156954)
24. Pietschmann T., Lohmann V., Kaul A., Krieger N., Rinck G., Rutter G., et al. Persistent and transient replication of full-length hepatitis C virus genomes in cell culture. J Virol 2002 ; 76 (8). 4008-4021.
25. Neugebauer A., Hartmann RW, Klein CD: Prediction of protein-protein interaction inhibitors by chemoinformatics and machine learning methods. J Med Chem 2007 ; 50 (19). 4665-4668.
26. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999 ; 4 (2). 67-73.
27. Holzer M., Ziegler S., Albrecht B., Kronenberger B., Kaul A., Bartenschlager R., et al. Identification of terfenadine as an inhibitor of human CD81-receptor HCV-E2 interaction: synthesis and structure optimization. Molecules 2008 ; 13 (5). 1081-1110.
28. Hao W., Duggal R.: High-throughput screening of HCV RNA replication inhibitors by means of a reporter replicon system. Methods Mol Biol 2009 ; 510: 243-250.
29. Cai L., Gochin M.: A novel fluorescence intensity screening assay identifies new low-molecular-weight inhibitors of the gp41 coiled-coil domain of human immunodeficiency virus type 1. Antimicrob Agents Chemother 2007 ; 51 (7). 2388-2395.