Homogeneous high-throughput screening assays for HIV-1 integrase 3′-processing and strand transfer activities

Journal of Biomolecular Screening

Volumn 10, Issue 5, 2005, Pages 456-462

  Wang, Yu ^a   Klock, Heath ^a   Yin, Hong ^a   Wolff, Karen ^a   Bieza, Kimberly ^a   Niswonger, Kirk ^a   Matzen, Jason ^a   Gunderson, Drew ^a   Hale, Joanna ^a   Lesley, Scott ^a   Kuhen, Kelli ^a   Caldwell, Jeremy ^a   Brinker, Achim ^a  

^a GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

Author keywords

3 processing; Antivirals; HIV 1; Strand transfer; TR FRET

Indexed keywords

INTEGRASE; INTEGRASE INHIBITOR;

ARTICLE; CONTROLLED STUDY; ENZYME SYNTHESIS; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH THROUGHPUT SCREENING; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; NONHUMAN; PRIORITY JOURNAL; VIRUS INHIBITION;

ANTIVIRAL AGENTS; CELL LINE; CELL LINE, TUMOR; CLONING, MOLECULAR; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, GENETIC; PHOSPHATIDYLCHOLINES; TIME FACTORS;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 24144501087     PISSN: 10870571     EISSN: None     Source Type: Journal    
DOI: 10.1177/1087057105275212     Document Type: Article

References (33)

1. Sleasman JW, Goodenow MM: 13. HIV-1 infection. J Allergy Clin Immunol 2003;111:S582-S592.
2. De Clercq E: New developments in anti-HIV chemotherapy. Biochim Biophys Acta 2002;1587:258-275.
3. Pluymers W, De Clercq E, Debyser Z: HIV-1 integration as a target for antiretroviral therapy: a review. Curr Drug Targets Infect Disord 2001;1:133-149.
4. Gupta SP, Nagappa AN: Design and development of integrase inhibitors as anti-HIV agents. Curr Med Chem 2003;10:1779-1794.
5. Goldgur Y, Dyda F, Hickman AB, Jenkins TM, Craigie R, Davies DR: Three new structures of the core domain if HIV-1 integrase: an active site that binds magnesium. Proc Natl Acad Sci U S A 1998;95:9150-9154.
6. Hazuda DJ, Felock PJ, Hastings JC, Pramanik B, Wolfe AL: Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase. J Virol 1997;71:7005-7011.
7. Neamati N, Lin Z, Karki LG, Orr A, Cowansage K, Strumberg D, et al: Metal-dependent inhibition of HIV-1 integrase. J Med Chem 2002;45:5661-5670.
8. Hazuda DJ, Felock P, Witmer M, Wolfe A, Stillmock K, Grobler JA, et al: Inhibitors of strand transfer that prevents integration and inhibit HIV-1 replication in cells. Science 2000;287:646-650.
9. Farnet CM, Wang B, Lipford JR, Bushman FD: Differential inhibition of HIV-1 preintegration complexes and purified integrase by small molecules. Proc Natl Acad Sci U S A 1996;93:9742-9747.
10. Marchand C, Zhang X, Pais GCG, Cowansage K, Neamati N, Burke TR, et al: Structural determinants for HIV-1 integrase inhibition by β-diketo acids. J Biol Chem 2002;277:12596-12603.
11. Pais GCG, Zhang X, Marchand C, Neamati N, Cowansage K, Svarovskaia ES, et al: Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors. J Med Chem 2002;45:3184-3194.
12. Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, et al: A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc Natl Acad Sci U S A 2004;101:11233-11238.
13. Dayam R, Neamati N: Small-molecule HIV-1 integrase inhibitors: the 2001-2002 update. Curr Pharm Des 2003;9:1789-802.
14. Marchand C, Neamati N, Pommier Y: In vitro human immunodeficiency virus type 1 integrase assays. Methods Enzymol 2001;340:624-633.
15. Chow SA: In vitro assays for activities of retroviral integrase. Methods 1997;12:306-317.
16. David CA, Middleton T, Montgomery D, Lim HB, Kati W, Molla A, et al: Microarray compound screening (microARCS) to identify inhibitors of HIV integrase. J Biomol Screen 2002;7:259-266.
17. Craigie R, Mizuuchi K, Bushman FD, Engelman A: A rapid in vitro assay for HIV DNA integration. Nucleic Acids Res 1991;19:2729-2734.
18. Hansen MST, Smith GJ, Kafari T, Molteni V, Siegel JS, Bushman FD: Integration complexes derived from HIV vectors for rapid assays in vitro. Nat Biotechnol 1999;17:578-582.
19. Hwang Y, Rhodes D, Bushman F: Rapid microtiter assays for poxyvirus topoisomerase, mammalian type IB topoisomerase and HIV-1 integrase: application to inhibitor isolation. Nucleic Acids Res 2000;28:4884-4892.
20. Hazuda DJ, Hastings CJ, Wolfe AL, Emini EA: A novel assay for the DNA strand transfer reaction of HIV-1 integrase. Nucleic Acids Res 1994;22:1121-1122.
21. Goldgur Y, Craigie R, Cohen GH, Fujiwara T, Yoneshinaga T, Fujishita T, et al: Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: a platform for antiviral drug design. Proc Natl Acad Sci U S A 1999;96:13040-13043.
22. Jenkins TM, Engelman A, Ghirlando R, Craigie R: A soluble active mutant of HIV-1 integrase: involvement of both the core and carboxyl-terminal domains in multimerization. J Biol Chem 1996;271:7712-7718.
23. Lesley SA, Kuhn P, Godzik A, Deacon AM, Mathews I, Kreusch A, et al: Structural genomics of the Thermotoga maritima proteome implemented in a high-throughput structure determination pipeline. Proc Natl Acad Sci U S A 2002;99:11664-1669.
24. 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;4:67-73.
25. Douglas JL, Lin WY, Panis ML, Veres G: Efficient human immunodeficiency virus-based vector transduction of unstimulated human mobilized peripheral blood CD34+ cells in the SCID-hu Thy/Liv model of human T cell lymphopoiesis. Hum Gene Ther 2001;12:401-13.
26. Glickman JF, Wu X, Mercuri R, Illy C, Bowen BR, He Y, et al: A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors. J Biomol Screen 2002;7:3-10.
27. Pope AJ: Introduction LANCE™ vs. HTRF® technologies (or vice versa). J Biomol Screen 1999;4:301-302.
28. Mathis G: HTRF® technology. J Biomol Screen 1999;4:309-314.
29. Sinha S, Pursley MH, Grandgenett DP: Efficient concerted integration by recombinant human immunodeficiency virus type 1 integrase without cellular or viral cofactors. J Virol 2002;76:3105-3113.
30. King PJ, Lee DJ, Reinke RA, Victoria JG, Beale K, Robinson WE: Human immunodeficiency virus type-1 integrase containing a glycine to serine mutation at position 140 is attenuated for catalysis and resistant to integrase inhibitors. Virology 2003;306:147-161.
31. Marchand C, Johnson AA, Karki RG, Pais GCG, Zhang X, Cowansage K, et al: Metal-dependent inhibition of HIV-1 integrase by β-diketo acids and resistance of the soluble double-mutant (F185K/C280S)). Mol Pharmacol 2003;64:600-609.
32. Mazumder A, Wang S, Neamati N, Nicklaus M, Sunder S, Chen J, et al: Antiretroviral agents as inhibitors of both human immunodeficiency virus type I integrase and protease. J Med Chem 1996;39:2472-2481.
33. Mustata GI, Brigo A, Briggs JM: HIV-1 integrase pharmacophore model derived from diverse classes of inhibitors. Bioorg Med Chem Lett 2004;14:1447-1454.