A generally applicable, high-throughput screening-compatible assay to identify, evaluate, and optimize antimicrobial agents for drug therapy

Journal of Biomolecular Screening

Volumn 9, Issue 7, 2004, Pages 578-587

  Kleymann, Gerald ^a   Werling, Hans Otto ^a  

^a BAYER PHARMA AG   (Germany)

Author keywords

Anti infective; Antibiotic; Antifungal; Antimycotic; Antiviral; AS assay; Drug discovery; High throughput screening; HTS; Selectivity; Susceptibility; Test; Tolerability

Indexed keywords

ACICLOVIR; AMPHOTERICIN B; ANTIBIOTIC AGENT; ANTIFUNGAL AGENT; ANTIINFECTIVE AGENT; ANTIVIRUS AGENT; BAY 38 9489; BAY 57 1293; BAY T 5420; CIPROFLOXACIN; DIMETHYL SULFOXIDE; FLUORESCEIN DIACETATE; HYMECROMONE; MOXIFLOXACIN; TROVAFLOXACIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTIMICROBIAL ACTIVITY; ARTICLE; CANDIDA ALBICANS; CELL COUNT; CELL GROWTH; CELL SURVIVAL; CELL VIABILITY; CHO CELL; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DETERMINATION; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; DRUG TOLERABILITY; ESCHERICHIA COLI; HERPES SIMPLEX VIRUS 1; HIGH THROUGHPUT SCREENING; HOST CELL; HUMAN CYTOMEGALOVIRUS; IN VITRO STUDY; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PRIORITY JOURNAL; SPECTROFLUOROMETRY; STAPHYLOCOCCUS AUREUS; VARICELLA ZOSTER VIRUS; VERO CELL;

ANIMALS; ANTI-INFECTIVE AGENTS; BACTERIA; CELL SURVIVAL; CERCOPITHECUS AETHIOPS; CHO CELLS; CRICETINAE; CRICETULUS; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HELA CELLS; HUMANS; MICROSCOPY, ELECTRON, SCANNING; MOLECULAR STRUCTURE; VERO CELLS;

ANIMALIA; FUNGI; HERPES; HERPESVIRIDAE;

EID: 2942721870     PISSN: 10870571     EISSN: None     Source Type: Journal    
DOI: 10.1177/1087057104265291     Document Type: Article

References (35)

1. Mandall GL, Bennett JE, Dolin R: Principles and Practice of Infectious Diseases, 5th ed. Edinburgh: Churchill Livingstone, 2000.
2. Murray PR, Baron EJ, Jorgensen JH, Pfaller MA, Yolken RH: Manual of Clinical Microbiology, 8th ed. Washington, DC: American Society for Microbiology, 2003.
3. Atkinson T: Lifestyle drug market booming. Nat Med 2002;8:909.
4. Bertino J Jr, Fish D: The safety profile of the fluoroquinolones. Clin Ther 2000;22:798-817; discussion 797.
5. Cossart P, Boquet P, Normark S, Rappuoli R: Cellular microbiology emerging. Science 1996;271:315-316.
6. Ward GE, Carey KL, Westwood NJ: Using small molecules to study big questions in cellular microbiology. Cell Microbiol 2002;4:471-482.
7. Jorgensen JH, Turnidge JD, Washington JA: Antibacterial susceptibility tests. In Murray PR, Baron EJ, Jorgensen JH, Pfaller MA, Yolken RH (eds): Manual of Clinical Microbiology, 8th ed. Washington, DC: American Society for Microbiology, 2003.
8. Swierkosz EM, Hodinka RL: Antiviral agents and susceptibility tests In Murray PR, Baron EJ, Jorgensen JH, Pfaller MA, Yolken RH (eds): Manual of Clinical Microbiology, 8th ed. Washington, DC: American Society for Microbiology, 2003.
9. McLaren C, Ellis MN, Hunter GA: A colorimetric assay for the measurement of the sensitivity of herpes simplex viruses to antiviral agents. Antiviral Res 1983;3:223-234.
10. Gadler H: Nucleic acid hybridization for measurement of effects of antiviral compounds on human cytomegalovirus DNA replication. Antimicrob Agents Chemother 1983;24:370-374.
11. Wahren B, Harmenberg J, Sundqvist VA, Leven B, Skoldenberg B: A novel method for determining the sensitivity of herpes simplex virus to antiviral compounds. J Virol Methods 1983;6:141-149.
12. Musiani M, Zerbini M, Gentilomi G, La Placa M: Rapid quantitative assay of cytomegalovirus infectivity. J Virol Methods 1988;20:333-340.
13. Dicker IB, Blasecki JW, Seetharam S: Herpes simplex type1:lacZ recombinant viruses: II. Microtiter plate-based colorimetric assays for the discovery of new antiherpes agents and the points at which such agents disrupt the viral replication cycle. Antiviral Res 1995;28:213-224.
14. Rotman B, Papermaster BW: Membrane properties of living mammalian cells as studied by enzymatic hydrolysis of fluorogenic esters. Proc Natl Acad Sci USA 1966;55:134-141.
15. Schols D, Pauwels R, Vanlangendonck F, Balzarini J, De Clercq E: A highly reliable, sensitive, flow cytometric/fluorometric assay for the evaluation of the anti-HIV activity of antiviral compounds in MT-4 cells. J Immunol Methods 1988;114:27-32.
16. Fischer R, Kleymann G, Baumeister J, Bender W, Betz U, Eckenberg P, et al: Thiazolyl urea derivatives and their utilization as antiviral agents. EP1161423, WO0053591 (LeA 33621). European Patent Office (http:// gb.espacenet.com), 1999.
17. Kleymann G, Fischer R, Betz UA, Hendrix M, Bender W, Schneider U, et al: New helicase-primase inhibitors as drug candidates for the treatment of herpes simplex disease. Nat Med 2002;8:392-398.
18. Elion GB, Furman PA, Fyfe JA, de Miranda P, Beauchamp L, Schaeffer HJ: The selectivity of action of an antiherpetic agent, 9-(2-hydroxyethoxymethyl) guanine. Reproduced from Proc Natl Acad Sci U S A 1977;74:5716-5720; Rev Med Virol 1999;9:147-152; discussion 152-153.
19. Elion GB, Furman PA, Fyfe JA, de Miranda P, Beauchamp L, Schaeffer HJ: The selectivity of action of an antiherpetic agent, 9-(2-hydroxyethoxymethyl) guanine. Reproduced from Proc Natl Acad Sci U S A 1977;74:5716-5720; Rev Med Virol 1999;9:147-152; discussion 152-153.
20. Schaeffer HJ, Beauchamp L, de Miranda P, Elion GB, Bauer DJ, Collins P: 9-(2-hydroxyethoxymethyl) guanine activity against viruses of the herpes group. Nature 1978;272:583-585.
21. Kleymann G: Helicase primase inhibitors. Drugs Future 2003;28:257-265.
22. Kleymann G: New antiherpes drugs target viral helicase-primase enzymes. HERPES 2003;10:46-52.
23. Bedard J, May S, Barbeau D, Yuen L, Rando RF, Bowlin TL: A high throughput colorimetric cell proliferation assay for the identification of human cytomegalovirus inhibitors. Antiviral Res 1999;41:35-43.
24. Kleymann G, Werling H-O: Patent Application DE10235967 A (LeA 34690 [2000]) & WO2004015416 (LeA 36301 [2004]), European Patent Office (http://gb.espacenet.com).
25. Kleymann G: Discovery, SAR and medicinal chemistry of herpesvirus helicase primase inhibitors. Curr Med Chem Anti-Infect Agents 2004;3:69-83.
26. Schmid MB: Microbial genomics - new targets, new drugs. Expert Opin Ther Targets 2001;5:465-475.
27. Kleymann G: Novel agents and strategies to treat herpes simplex viras infections. Expert Opin Investig Drugs 2003;12:165-183.
28. National Committee for Clinical Laboratory Standards. Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria That Grow Aerobically, 5th ed. Approved standard. NCCLS Document M7-A5 (Vol. 20, No. 2), M11-A4 (Vol. 17, No. 22). Villanova, PA: Author, 1997.
29. National Committee for Clinical Laboratory Standards. Reference Method for Broth Dilution Antifungal Susceptibility Testing of Yeasts, Vol. 15, No. 10 M27-A. NCCLS. Villanova, PA: Author, 1997.
30. Espinel-Ingroff A, White T, Pfaller MA: Antifungal agents and susceptibility testing. In Murray PR, Baron EJ, Jorgensen JH, Pfaller MA, Yolken RH (eds): Manual of Clinical Microbiology, 8th ed. Washington, DC: American Society for Microbiology, 2003.
31. Rodriguez-Tudela JL, Berenguer J, Martinez-Suarez JV, Sanchez R: Comparison of a spectrophotometric microdilution method with RPMI-2% glucose with the National Committee for Clinical Laboratory Standards reference macrodilution method M27-P for in vitro susceptibility testing of amphotericin B, flueytosine, and fluconazole against Candida albicans. Antimicrob Agents Chemother 1996;40:1998-2003.
32. O'Brien JJ, Campoli-Richards DM: Acyclovir: an updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1989;37:233-309.
33. Whitley RJ, Gnann JW Jr: Acyclovir: a decade later. N Engl J Med 1992;327:782-789. Erratum in N Engl J Med 1993;328:671. N Engl J Med 1997;337:1703.
34. Whitley RJ, Gnann JW Jr: Acyclovir: a decade later. N Engl J Med 1992;327:782-789. Erratum in N Engl J Med 1993;328:671. N Engl J Med 1997;337:1703.
35. Whitley RJ, Gnann JW Jr: Acyclovir: a decade later. N Engl J Med 1992;327:782-789. Erratum in N Engl J Med 1993;328:671. N Engl J Med 1997;337:1703.