Antiviral activities of 15 dengue NS2B-NS3 protease inhibitors using a human cell-based viral quantification assay

Antiviral Research

Volumn 118, Issue , 2015, Pages 68-74

  Chu, Justin Jang Hann ^a   Lee, Regina Ching Hua ^a   Ang, Melgious Jin Yan ^b   Wang, Wei Ling ^b   Lim, Huichang Annie ^b   Wee, John Liang Kuan ^b   Joy, Joma ^b   Hill, Jeffrey ^b   Brian Chia, C S ^b  

^a NATIONAL UNIVERSITY HEALTH SYSTEM   (Singapore)

^b Agency for Science   (Singapore)

Author keywords

Antiviral; Dengue; NS2B NS3; Protease inhibitor

Indexed keywords

IVERMECTIN; NONSTRUCTURAL PROTEIN 2; NONSTRUCTURAL PROTEIN 2B; NONSTRUCTURAL PROTEIN 3; PROTEINASE INHIBITOR; SELAMECTIN; UNCLASSIFIED DRUG; ANTHRAQUINONE DERIVATIVE; ANTIVIRUS AGENT; NS2B PROTEIN, FLAVIVIRUS; NS3 PROTEIN, FLAVIVIRUS; RNA HELICASE; SERINE PROTEINASE; VIRAL PROTEIN;

ANIMAL CELL; ANTIBODY TITER; ANTIVIRAL ACTIVITY; ARTICLE; CELL MEMBRANE PERMEABILITY; CONTROLLED STUDY; DENGUE; DENGUE VIRUS 2; EMBRYO; HUMAN; HUMAN CELL; IC50; K562 CELL LINE; LIVER CELL CARCINOMA; MOLECULAR DOCKING; NONHUMAN; PRIORITY JOURNAL; PROTEINASE INHIBITION; ANTAGONISTS AND INHIBITORS; CELL SURVIVAL; DENGUE VIRUS; DRUG EFFECTS; ENZYMOLOGY; LIVER CELL; MICROBIAL SENSITIVITY TEST; PHYSIOLOGY; TUMOR CELL LINE; VIROLOGY; VIRUS LOAD;

DENGUE VIRUS; MAMMALIA;

ANTHRAQUINONES; ANTIVIRAL AGENTS; CELL LINE, TUMOR; CELL SURVIVAL; DENGUE VIRUS; HEPATOCYTES; HUMANS; MICROBIAL SENSITIVITY TESTS; PROTEASE INHIBITORS; RNA HELICASES; SERINE ENDOPEPTIDASES; VIRAL LOAD; VIRAL NONSTRUCTURAL PROTEINS;

EID: 84926221731     PISSN: 01663542     EISSN: 18729096     Source Type: Journal    
DOI: 10.1016/j.antiviral.2015.03.010     Document Type: Article

References (32)

1. C.F. Arias, F. Preugschat, and J.H. Strauss Dengue virus NS2B and NS3 form a stable complex that can cleave NS3 within the helicase domain Virology 193 1993 888 899
2. S. Chanprapaph, P. Saparpakorn, C. Sangma, P. Niyom-rattanakit, S. Hannongbua, C. Angsuthanasombat, and G. Katzenmeier Competitive inhibition of the dengue virus NS3 serine protease by synthetic peptides representing polyprotein cleavage sites Biochem. Biophys. Res. Commun. 330 2005 1237 1246
3. S. Clum, K.E. Ebner, and R. Padmanabhan Co-translational membrane insertion of the serine proteinase precursor NS2B-NS3(pro) of dengue virus type 2 is required for efficient in vitro processing and is mediated through the hydrophobic regions of NS2B J. Biol. Chem. 272 1997 30715 30723
4. L. de la Cruz, T.H. Nguyen, K. Ozawa, J. Shin, B. Graham, T. Huber, and G. Otting Binding of low molecular weight inhibitors promotes large conformational changes in the dengue virus NS2B-NS3 protease: fold analysis by pseudo-contact shifts J. Am. Chem. Soc. 133 2011 19205 19215
5. L. Di, E.H. Kerns, K. Fan, O.J. McConnell, and G.T. Carter High throughput artificial membrane permeability assay for blood-brain barrier Eur. J. Med. Chem. 38 2003 223 232
6. V.K. Ganesh, N. Muller, K. Judge, C.-H. Luan, R. Padmanabhan, and K.H.M. Murthy Identification and characterization of non-substrate based inhibitors of the essential dengue and West Nile virus proteases Bioorg. Med. Chem. 13 2005 257 264
7. D.J. Gubler Dengue and dengue hemorrhagic fever Clin. Microbiol. Rev. 11 1998 480 496
8. D. Ekonomiuk, X.-C. Su, K. Ozawa, C. Bodenreider, S.P. Lim, G. Otting, D. Huang, and A. Caflisch Flaviviral protease inhibitors identified by fragment-based library docking into a structure generated by molecular dynamics J. Med. Chem. 52 2009 4860 4868
9. T. Knehans, A. Schüller, D.N. Doan, K. Nacro, J. Hill, P. Güntert, M.S. Madhusudhan, T. Weil, and S.G. Vasudevan Structure-guided fragment-based in silico drug design of dengue protease inhibitors J. Comput. Aided Mol. Des. 25 2011 263 274
10. J. Lescar, D. Luo, T. Xu, A. Sampath, S.P. Lim, B. Canard, and S.G. Vasudevan Towards the design of antiviral inhibitors against flaviviruses: the case for the multifunctional NS3 protein from Dengue virus as a target Antiviral Res. 80 2008 94 101
11. S.P. Lim, Q.-Y. Wang, C.G. Noble, Y.-L. Chen, H. Dong, B. Zou, F. Yokokawa, S. Nilar, P. Smith, D. Beer, J. Lescar, and P.-Y. Shi Ten years of dengue drug discovery: progress and prospects Antiviral Res. 100 2013 500 519
12. N. Meanwell Synopsis of some recent tactical application of bioisosteres in drug design J. Med. Chem. 54 2011 2529 2591
13. S. Melino, and M. Paci Progress for dengue virus diseases: towards the NS2B-NS3pro inhibition for a therapeutic-based approach FEBS J. 274 2007 2986 3002
14. N.H. Mueller, N. Pattabiraman, C. Ansarah-Sobrinho, P. Viswanathan, T.C. Pierson, and R. Padmanabhan Identification and biochemical characterization of small-molecule inhibitors of West Nile virus serine protease by a high-throughput screen Antimicrob. Agents Chemother. 52 2008 3385 3393
15. C. Nitsche, C. Steuer, and C.D. Klein Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases Bioorg. Med. Chem. 19 2011 7318 7337
16. C. Nitsche, M.A.M. Behnam, C. Steuer, and C.D. Klein Retro peptide-hybrids as selective inhibitors of the Dengue virus NS2B-NS3 protease Antiviral Res. 94 2012 72 79
17. C.G. Noble, Y.L. Chen, H. Dong, F. Gu, S.P. Lim, W. Schul, Q.-Y. Wang, and P.-Y. Shi Strategies for development of dengue virus inhibitors Antiviral Res. 85 2010 450 462
18. C.G. Noble, and P.-Y. Shi Structural biology of dengue virus enzymes: towards rational design of therapeutics Antiviral Res. 96 2012 115 126
19. B. Pastorino, A. Nougairède, N. Wurtz, E. Gould, and X. de Lamballerie Role of host cell factors in flavivirus infection: implications for pathogenesis and development of antiviral drugs Antiviral Res. 87 2010 281 294
20. L. Peterlin-Mašič, and D. Kikelj Arginine mimetics Tetrahedron 57 2001 7073 7105
21. C.P. Simmons, J.J. Farrar, N.V.V. Chau, and B. Wills Current concepts: Dengue N. Engl. J. Med. 366 2012 1423 1432
22. T. Solomon, and M. Mallewa Dengue and other emerging flaviviruses J. Infect. 42 2001 104 115
23. A.J. Stevens, M.E. Gahan, S. Mahalingam, and P.A. Keller The medicinal chemistry of dengue fever J. Med. Chem. 52 2009 7911 7926
24. S.M. Tomlinson, R.D. Malmstrom, and S.J. Watowich New approaches to structure-based discovery of dengue protease inhibitors Infect. Disord. Drug Targets 9 2009 327 343
25. S.M. Tomlinson, R.D. Malmstrom, A. Russo, N. Mueller, Y.-P. Pang, and S.J. Watowich Structure-based discovery of dengue virus protease inhibitors Antiviral Res. 82 2009 110 114
26. S.M. Tomlinson, and S.J. Watowich Anthracene-based inhibitors of dengue virus NS2B-NS3 protease Antiviral Res. 89 2011 127 135
27. S.M. Tomlinson, and S.J. Watowich Use of parallel validation high-throughput screens to reduce false positives and identify novel dengue NS2B-NS3 protease inhibitors Antiviral Res. 93 2012 245 252
28. P. Vlieghe, V. Lisowski, J. Martinez, and M. Khrestchatisky Synthetic therapeutic peptides: science and market Drug Discovery Today 15 2010 40 56
29. S. Xu, H. Li, X. Shao, C. Fan, B. Ericksen, J. Liu, C. Chi, and C. Wang Critical effect of peptide cyclization on the potency of peptide inhibitors against dengue virus NS2B-NS3 protease J. Med. Chem. 55 2012 6881 6887
30. C.C. Yang, Y.C. Hsieh, S.J. Lee, S.H. Wu, C.L. Liao, C.H. Tsao, Y.S. Chao, J.H. Chern, C.P. Wu, and A. Yueh Novel dengue virus-specific NS2B/NS3 protease inhibitor, BP2109, discovered by a high-throughput screening assay Antimicrob. Agents Chemother. 55 2011 229 238
31. Z. Yin, S.J. Patel, W.-L. Wang, W.-L. Chan, K.R.R. Rao, G. Wang, X. Ngew, V. Patel, D. Beer, J.E. Knox, N.L. Ma, C. Ehrhardt, S.P. Lim, S.G. Vasudevan, and T.H. Keller Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors Bioorg. Med. Chem. Lett. 16 2006 40 43
32. R. Yusof, S. Clum, M. Wetzel, H.M.K. Murthy, and R. Padmanabhan 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. 275 2000 9963 9969