High-throughput screening: The hits and leads of drug discovery-An overview

Journal of Applied Pharmaceutical Science

Volumn 1, Issue 1, 2011, Pages 2-10

  Martis, E A ^a   Radhakrishnan, R ^a   Badve, R R ^a  

^a Vivekanand Education Society's College of Pharmacy   (India)

Author keywords

Automation and robotics; Errors; High throughput screening (HTS); Miniaturization; Profiling; Z factor

Indexed keywords

EID: 84856289656     PISSN: None     EISSN: 22313354     Source Type: Journal    
DOI: None     Document Type: Article

References (58)

1. Abraham VC, Taylor DL, Haskins JR. High-content screening applied to large-scale cell biology. Trends in Biotechnology. 2004; 2(1):15-22.
2. Abriola L, Chin M, Fuerst P, et al. Digital imaging as a detection method for a fluorescent protease assay in 96-well and miniaturized assay plate formats. J Biomol Screening 1999; 4(4):121-7
3. Allegra CJ, Kovacs JA, Drake JC, et al. Potent in vitro and in vivo antitoxoplasma activity of the lipid-soluble antifolate trimetrexate. The Journal Clinical Investigation 1987; 79(2): 478-82.
4. Armstrong JW. HTS and robotics implementation: a critique of robotics equipment and strategies. Thousand Oaks, CA HTS Consulting Ltd. 1997.
5. Asmild M, Oswald N, Krzywkowski FM, et al. Upscaling and automation of electro-physiology: toward high throughput screening in ion channel drug discovery. Receptor and Channels 2003; 9: 49-58.
6. Bader GD, Hogue CW. An automated method for finding molecular complexes in large protein interaction networks. BMC Bioinformatics 2003; 4:2.
7. Beasley JR, Dunn DA, Walker TL, et al. Evaluation of compound interference in immobilized metal ion affinity-based fluorescence polarization detection with a four million member compound collection. Assay and Drug Devevelopment Technologies 2003; 1(3): 455-59.
8. Bosworth N, Towers P. Scintillation proximity assay. Nature 1989; 341(6238):167-68.
9. Brown RK, Proulx A. Accelerating the discovery process with automation and robotics: a sure bet or a risky venture? In: Devlin JP editor. High throughput screening. The discovery of bioactive substances. New York: Dekker 1997; p. 509-23.
10. Burbaum J. Miniaturization technologies in HTS: how fast, how small, how soon? Drug Discov Today 1998;3(7):313-22
11. Comley J, Binnie A, Bonk C, Houston J. A 384-HTS for human Factor VIIa: comparison with 96- and 864-well formats. J Biomol Screening 1997; 2(3):171-78.
12. Curtis JH, Robert WR, Heidi RB, et al. New inhibitors of ABCG2 identified by high-throughput screening. Molecular Cancer Therapeutics 2007; 6 (12): 3271-78.
13. Divers M. What is the future of high throughput screening? J Biomol Screening 1999; 4(4):177-8
14. Duane B, Nathaniel H, G. Sitta S, et al. Basic Considerations in Designing High-Throughput Screening Assays. In: Ramakrishna S, Prabhavathi BF, editors. Handbook of Drug Screening. New York: MARCEL DEKKER, INC: 2001; 14: p. 5-30.
15. Dupriez VJ, Maes K, Le-Poul E, Burgeon E, Detheux M. Aequorin-based functional assays for G-protein-coupled receptors, ion channels, and tyrosine kinase receptors. Receptors and Channels 2002; 8:319-30.
16. Gerhard HV, editor. Drug Discovery and Evaluation: Pharmacological Assays. 3rd ed. New York: Springer 2008.
17. Giulliano KA, DeBiasio RL, Dunlay RT, et al. Highcontent screening: A new approach to easing key bottlenecks in the drug discovery process. J Biomol Screen 1997; 2(4): 249-59.
18. Graziani F, Aldegheri L, Terstappen G. High throughput scintillation proximity assay for the identification of FKBP-12 ligands. J Biomol Screening 1999; 4(1); 3-7.
19. Green LS, Bell C, Janjic N. Aptamers as reagents for high-throughput screening. Biotechniques 2001; 30(5):1094-100.
20. Hemmila I., Mukkala VM, Latva M, Kiilhoma P. Diand tetracarboxylate derivatives of pyridines, bipyridines and terpyridines as luminogenic reagents for time-resolved fluorometric determination of terbium and dysprosium. J. Biochem. Biophys. Methods 1993; 26: 283-90.
21. Jason WA. A review of high-throughput screening approaches for drug discovery. Application Note.1999 Available from: http://www.combichemistry.com/articles/htscreening.pdf
22. Ji-Hu Z, Tangming C, Son HN, Keven RO. A High-Throughput homogeneous assay for Reverse Transcriptase using generic reagents and Time-Resolved Fluorescence detection. Analytical biochemistry 2000; 281(2): 182-86.
23. Ji-Hu Z, Thomas DYC, Kevin RO. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J Biomol screening 1999; 4 (2): 67-73.
24. Jin Z, Yong-Hong W, Ju C, et al. Penicillin G acylase purification with the aid of high-throughput screening approach. Journal of the Chinese Institute of Chemical Engineers 2008; 39(3): 195-02.
25. John GH, Martyn NB. HIGH-THROUGHPUT SCREENING FOR LEAD DISCOVERY. In: Donald JA, editor. BURGER'S MEDICINAL CHEMISTRY AND DRUG DISCOVERY. Vol 2: Drug Discovery and Drug Development. 6th ed. Wiley-Interscience: p. 38-55.
26. Kolb A, Kaplita P, Hayes D, et al. Tyrosine kinase assays adapted to homogeneous time-resolved fluorescence. Drug Discov Today 1998; 3(7): 333-42.
27. Kolb A, Neumann K. Beyond the 96-well microplate: instruments and assay methods for the 384-well format. J Biomol Screening 1997; 2(2):103-09.
28. Landia TA et al. HTS in the new millennium- the role of pharmacology and flexibility. Journal of Pharmacological and Toxicological methods 2000; 44(1): 270-89.
29. Lenz GR, Nash HM, Jindal S. Chemical ligands, genomics and drug discovery. Drug Discovery. Today 2000; 5(4):145-156
30. Liang M, Qiuyao J, Joseph AK. Development of a Yeast Assay for Rapid Screening of Inhibitors of Human-Derived Pneumocystis carinii Dihydrofolate Reductase. Antimicrobial agents and chemotheraphy 2002; 46(9): 3101-03.
31. Lightbody B, Alderman EM. Robotics development simplified. New Drugs 2001; 1: 30-32.
32. Maffia A, Kariv I, Oldenburg K. Miniaturization of a mammalian cell-based assay: luciferase reporter gene readout in a microliter 1536-well plate. J Biomol Screening 1999;4(3):137-42
33. Major J. What is the future of high throughput screening? Biomol Screening. 1999; 4(3):119.
34. Manly SP. In vitro biochemical screening. J Biomol Screen 1997; 2(4):197-99.
35. Mere L, Bennett T, Coassin P, et al. Miniaturized FRET assays and microfluidics: key components for ultra-highthroughput screening. Drug Discov Today 1999; 4(8): 363-69.
36. Moore K, Turconi S, Miles W, et al. A homogenous 384-well high-throughput screen for novel tumor necrosis factor receptor: ligand interactions using time resolved energy transfer. J Biomol Screening. 1999; 4(4):205-14.
37. Oldenburg K, Zhang J, Chen T, et al. Assay miniaturization for ultra-high throughput screening of combinatorial and discrete compound libraries: a 9600-well (0.2 microliter) assay system. J Biomol Screening 1998; 3(1):55-62
38. Parandoosh Z. Cell-based assays. J Biomol Screen 1997; 2(4): 201-02.
39. Richard YK, Amanda P.C. To, Louisa W.Y., et al. Characterization of SARS-CoV main protease and identification of biologically active small molecule inhibitors using a continuous fluorescence-based assay. FEBS Letters 2004; 576(3):325-30.
40. Roberts C.K. Applications of NMR in drug discovery. Drug Discov. Today 2000; 5(6): 230-40.
41. Robey RW, Steadman K, Polgar O, et al. Pheophorbide A is a specific probe for ABCG2 function and inhibition. Cancer Research 2004; 64(4):1242-46.
42. Rotstein DM, Gabriel SD, Makra F, Filonova L, et al. Spiropiperidine CCR5 antagonists. Bioorganic and Medicinal Chemistry Letters 2009; 19(18): 5401-06
43. Serb A, Schiopu C, Flangea C, et al. High-throughput analysis of gangliosides in defined regions of fetal brain by fully automated chip-based nanoelectrospray ionization multi-stage mass spectrometry. European Journal of Mass Spectrometry 2009; 15(4): 541-53.
44. Stahl W. What is the future of high throughput screening? J Biomol Screening. 1999; 4(3):117-8
45. Stenroos K, Hurskainen P. Homogeneous time-resolved IL-2-IL-2R alpha assay using fluorescence resonance energy transfer. Cytokine 1998; 10(7): 495-99.
46. Steven AS. High-throughput and ultra-high-throughput screening: solution- and cell-based approaches. Current Opinion in Biotechnology 2000; 11(1): 47-53.
47. Stoekli K, Haag H. High-Throughput Screening. In: Rang H. editor. Drug Discovery and Development Technology in transition. New York: CHURCHILL LIVINGSTONE 2005; p.129.
48. Stryer L. Fluorescence energy transfer as a spectroscopic ruler. Annual Review of biochemistry 1978; 47:819-46.
49. Suang R, Hideo N, Tsuneo Y. PCR-linked in vitro expression: a novel system for high-throughput construction and screening of protein libraries. FEBS Letters 2003; 540(1-3):147-50.
50. Vidalain PO, Boxem M, Ge H, Li S, Vidal M. Increasing specificity in High-Throughput yeast two-hybrid experiments. Methods 2004; 32(4): 363-70.
51. Walsh J. High throughput, mechanism-based screening techniques for discovering novel agrochemicals. J Biomol Screening 1998; 3(3):175-81
52. Wolcke J, Ullmann D. Miniaturized HTS technologies - uHTS. Drug Discov Today 2001; 6(12): 637-46.
53. World Health Organization (WHO). Available from: www.who.int/csr/sars/en/
54. Young K. Yeast two-hybrid: so many interactions, (in) so little time. Biology of Reproduction 1998; 58 (2): 302-11
55. Allegra CJ, Kovacs JA, Drake JC, et al. Activity of antifolates against Pneumocystis carinii dihydrofolate reductase and identification of a potent new agent. The Journal Experimental. Medicine 1987; 165(3): 926-31.
56. Douglas RH. Combinatorial chemistry In: Block JH, Beale JM, editors. Wilson and Gisvold's textbook of ORGANIC MEDICINAL AND PHARMACEUTICAL CHEMISTRY. 11th Baltimore: Lippincott Williams and Wilkins; 2004. p. 53-4.
57. Drews J. Drug Discovery: a historical perspective. Science 2000; 287(5460):1960-64.
58. Ronald EW, Prasarn M. Pharmacokinetic theory of cassette dosing in drug discovery screening. Drug Metabolism and Disposition 2001; 29 (7): 957-66.