Use of parallel validation high-throughput screens to reduce false positives and identify novel dengue NS2B-NS3 protease inhibitors

Antiviral Research

Volumn 93, Issue 2, 2012, Pages 245-252

  Tomlinson, Suzanne M ^a   Watowich, Stanley J ^a  

^a University of Texas Medical Branch School of Medicine   (United States)

Author keywords

Dengue virus; High throughput screen; Inhibitors; NS2B NS3; Protease; West Nile virus

Indexed keywords

ALEXIDINE; ANTIINFECTIVE AGENT; ANTIVIRUS AGENT; DENGUE VIRUS 2 NS2B NS3 PROTEASE INHIBITOR; IVERMECTIN; METHYLBENZETHONIUMCHLORIDE; SELAMECTIN; TRYPSIN; TYROTHRICIN; UNCLASSIFIED DRUG; VIRUS ENZYME;

ARTICLE; ASIAN; CONTROLLED STUDY; DENGUE VIRUS; DENGUE VIRUS 2; DRUG IDENTIFICATION; ENZYME INHIBITION; FALSE POSITIVE RESULT; HIGH THROUGHPUT SCREENING; MOLECULAR LIBRARY; NONHUMAN; PRIORITY JOURNAL; SOLUBILITY; VALIDATION STUDY; WEST NILE FLAVIVIRUS;

DENGUE; DENGUE VIRUS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; FALSE POSITIVE REACTIONS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; KINETICS; SERINE ENDOPEPTIDASES; VIRAL NONSTRUCTURAL PROTEINS;

DENGUE VIRUS; DENGUE VIRUS TYPE 2; FLAVIVIRIDAE; WEST NILE VIRUS;

EID: 84856093723     PISSN: 01663542     EISSN: 18729096     Source Type: Journal    
DOI: 10.1016/j.antiviral.2011.12.003     Document Type: Article

References (36)

1. Alleman M., Twim-Danso N., Thylefors B. The Mectizan donation program - highlights from 2005. Filaria J. 2006, 5:1-11.
2. Alvarez M., Rodriguez-Roche R., Bernardo L., Vazquez S., Morier L., Gonzalez D., Castro O., Kouri G., Halstead S.B., Guzman M.G. Dengue hemorrhagic fever caused by sequential dengue 1-3 virus infections over a long time interval: Havana epidemic, 2001-2002. Am. J. Trop. Med. Hyg. 2006, 75:1113-1117.
3. Cahour A., Falgout B., Lai C.J. Cleavage of the dengue virus polyprotein at the NS3/NS4A and NS4B/NS5 junctions are mediated by viral protease NS2B-NS3, whereas NS4A/NS4B may be processed by a cellular protease. J. Virol. 1992, 66:1535-1542.
4. CDC Locally acquired Dengue - Key West Florida 2009-2010. MMWR Morb. Mortal Weekly Rep. 2010, 59:577-581.
5. Chambers T.J., Nestorowicz A., Amberg S.M., Rice C.M. Mutagenesis of the yellow fever virus NS2B protein: effects on proteolytic processing, NS2B-NS3 complex formation, and viral replication. J. Virol. 1993, 67:6797-6807.
6. Chanprapaph S., Saparpakorn P., Sangma C., Niyomrattanakit P., Hannongbua S., Angsuthanasombat C., Katzenmeier G. Competitive inhibition of the dengue virus NS3 serine protease by synthetic peptides representing polyprotein cleavage sites. Biochem. Biophys. Res. Commun. 2005, 330:1237-1246.
7. Erbel P., Schiering N., D'Arcy A., Renatus M., Kroemer M., Lim S.P., Yin Z., Keller T.H., Vasudevan S.G., Hommel U. Structural basis for the activation of flaviviral NS3 proteases from dengue and West Nile virus. Nat. Struct. Mol. Biol. 2006, 13:372-373.
8. Falgout B., Pethel M., Zhang Y.M., Lai C.J. Both nonstructural proteins NS2B and NS3 are required for the proteolytic processing of dengue virus nonstructural proteins. J. Virol. 1991, 65:2467-2475.
9. Fields B., Knipe D., Howley P., Chanock R., Melnick J., Monath T., Roizman B., Strauss S. Field's Virology 1996, Lippincott Williams & Wilkins, Philadelphia, Third Edition.
10. Halstead S.B. Neutralization and antibody-dependent enhancement of dengue viruses. Adv. Virus Res. 2003, 60:421-467.
11. Hanna J.N., Ritchie S.A., Richards A.R., Humphreys J.L., Montgomery B.L., Ehlers G.J., Pyke A.T., Taylor C.T. Dengue in north Queensland, 2005-2008. Commun. Dis. Intell. 2009, 33:198-203.
12. Kim D.H., Chung H.J., Bleys J., Ghohestani R.F. Is paromomycin an effective and safe treatment against cutaneous leishmaniasis? A meta-analysis of 14 randomized controlled trials. PLoS Negl. Trop. Dis. 2009, 3:e381.
13. Kuan M.M., Lin T., Chuang J.H., Wu H.S. Epidemiological trends and the effect of airport fever screening on prevention of domestic dengue fever outbreaks in Taiwan, 1998-2007. Int. J. Infect. Dis. 2010, 14:e693-697.
14. Kuzmic P. Program DYNAFIT for the analysis of enzyme kinetic data: application to HIV proteinase. Anal. Biochem. 1996, 237:260-273.
15. La Ruche G., Souares Y., Armengaud A., Peloux-Petiot F., Delaunay P., Despres P., Lenglet A., Jourdain F., Leparc-Goffart I., Charlet F., Ollier L., Mantey K., Mollet T., Fournier J.P., Torrents R., Leitmeyer K., Hilairet P., Zeller H., Van Bortel W., Dejour-Salamanca D., Grandadam M., Gastellu-Etchegorry M. First two autochthonous dengue virus infections in metropolitan France, September 2010. Euro. Surveill. 2010, 15:19676.
16. Leung D., Schroder K., White H., Fang N.X., StoermerMJ Abbenante.G., Martin J.L., Young P.R., Fairlie D.P. Activity of recombinant dengue 2 virus NS3 protease in the presence of a truncated NS2B co-factor, small peptide substrates, and inhibitors. J. Biol. Chem. 2001, 276:45762-45771.
17. Li J., Lim S.P., Beer D., Patel V., Wen D., Tumanut C., Tully D.C., Williams J.A., Jiricek J., Priestle J.P., Harris J.L., Vasudevan S.G. Functional profiling of recombinant NS3 proteases from all four serotypes of dengue virus using tetrapeptide and octapeptide substrate libraries. J. Biol. Chem. 2005, 280:28766-28774.
18. McDonnell G., Russell A.D. Antiseptics and disinfectants: activity, action, and resistance. Clin. Microbiol. Rev. 1999, 12:147-179.
19. Mogi T., Kita K. Gramicidin S and polymyxins: the revival of cationic cyclic peptide antibiotics. Cell. Mol. Life Sci. 2009, 66:3821-3826.
20. Molinari G., Soloneski S., Reigosa M.A., Larramendy M.L. In vitro genotoxic and cytotoxic effects of ivermectin and its formulation on Chinese hamster ovary (CHOK1) cells. J. Hazard. Mater. 2009, 165:1074-1082.
21. Mueller N.H., Yon C., Ganesh V.K., Padmanabhan R. Characterization of theWest Nile virus protease substrate specificity and inhibitors. Int. J. Biochem. Cell Biol. 2007, 39:606-614.
22. Ogoussan K.T., Hopkins A. Mectizan procurement and delivery for onchocerciasis mass drug administration programmes. Acta Trop. 2010, 120(Suppl 1):S173-S176.
23. Otoguro K., Liu Z.X., Fukuda K., Li Y., Iwai Y., Tanaka H., Omura S. Screening for new nematocidal substances of microbial origin by a new method using the pine wood nematode. J. Antibiot. (Tokyo) 1988, 41:573-575.
24. Pipano E. Recent developments in the control of ectoparasites and endoparasites of dogs and cats. Israel J. Veter. Med. 2002, 58:2-3.
25. Tomlinson S.M., Malmstrom R.D., Watowich S.J. New approaches to structure-based discovery of dengue protease inhibitors. Infect. Disord.: Drug Targets 2009, 9:327-343.
26. Tomlinson S.M., Malmstrom R.D., Russo A., Mueller N., Pang Y.P., Watowich S.J. Structure-based discovery of dengue virus protease inhibitors. Antiviral Res. 2009, 82:110-114.
27. Tomlinson S.M., Watowich S.J. Substrate inhibition kinetic model for West Nile virus NS2B-NS3 protease. Biochemistry 2008, 47:11763-11770.
28. Tomlinson S.M., Watowich S.J. Anthracene-based inhibitors of dengue virus NS2B-NS3 protease. Antiviral Res. 2011, 89:127-135.
29. Wagstaff K.M., Rawlinson S.M., Hearps A.C., Jans D.A. An Alpha Screen(R)-based assay for high-throughput screening for specific inhibitors of nuclear import. J. Biomol. Screen 2011, 16:192-200.
30. WHO (2010).. http://www.who.int/mediacentre/factsheets/fs117/en/.
31. Xie J., Nair A., Hermiston T.W. A comparative study examining the cytotoxicity of inducible gene expression system ligands in different cell types. Toxicol. In Vitro 2008, 22:261-266.
32. Yang C.C., Hsieh Y.C., Lee S.J., Wu S.H., Liao C.L., Tsao C.H., Chao Y.S., Chern J.H., Wu C.P., Yueh A. Novel dengue virus-specific NS2B/NS3 protease inhibitor, BP2109, discovered by a high-throughput screening assay. Antimicrob. Agents Chemother. 2011, 55:229-238.
33. Yates D.M., Wolstenholme A.J. An ivermectin-sensitive glutamate-gated chloride channel subunit from Dirofilariaimmitis. Int. J. Parasitol. 2004, 34:1075-1081.
34. Yin Z., Patel S.J., Wang W.L., Chan W.L., RangaRao K.R., Wang G., Ngew X., Patel V., Beer D., Knox J.E., Ma N.L., Ehrhardt C., Lim S.P., VasudevanSG Keller.T.H. Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors. Bioorg. Med. Chem. Lett. 2006, 16:40-43.
35. Yip K.W., Ito E., Mao X., Au P.Y., Hedley D.W., Mocanu J.D., Bastianutto C., Schimmer A., Liu F.F. Potential use of alexidinedihydrochloride as an apoptosis-promoting anticancer agent. Mol. Cancer Ther. 2006, 5:2234-2240.
36. Yusof R., Clum S., Wetzel M., Murthy H.M., Padmanabhan R. Purified NS2B/NS3 serine protease of dengue virus type 2 exhibits cofactor NS2B dependence for cleavage of substrates with dibasic amino acids in vitro. J. Biol. Chem. 2000, 275:9963-9969.