Robotic alliance of miniaturized synthesis and screening: A case study for the identification of histone deacetylase inhibitors

Engineering in Life Sciences

Volumn 13, Issue 4, 2013, Pages 344-351

  Groß, G Alexander ^a   Singh, Sukhdeep ^a   Schlingloff, Gregor ^a   Schwienhorst, Andreas ^b   Riester, Daniel ^b   Wegener, Dennis ^b   Wurziger, Hanns ^c   Schober, Andreas ^a  

^a ILMENAU UNIVERSITY OF TECHNOLOGY   (Germany)

^b UNIVERSITY OF GÖTTINGEN   (Germany)

^c MERCK KGAA   (Germany)

Author keywords

Automation; Combinatorial chemistry; High throughput screening (HTS); Microreactor array; Miniaturization

Indexed keywords

COMBINATORIAL CHEMISTRY; HIGH-THROUGHPUT SCREENING; HISTONE DEACETYLASE INHIBITOR; HISTONE DEACETYLASES; MICRO-REACTOR; MINIATURIZATION; MODERN DRUG DEVELOPMENT; SOLID PHASE SYNTHESIS;

AUTOMATION; BIOASSAY; BIOCHIPS;

ROBOTICS;

HISTONE DEACETYLASE; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID; NST 08; NST 41; NST 43; NST 47; NST 51; NST 66; NST 72; UNCLASSIFIED DRUG;

ARRAY; AUTOMATION; DEGRADATION; DRUG DEVELOPMENT; ENZYME ACTIVITY; FLUORESCENCE; INDUSTRIAL PRACTICE; INHIBITOR; PHARMACEUTICAL INDUSTRY; ROBOTICS; TECHNOLOGICAL DEVELOPMENT;

ANIMAL TISSUE; ARTICLE; DRUG MANUFACTURE; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; NONHUMAN; RAT; ROBOTICS;

EID: 84880037944     PISSN: 16180240     EISSN: 16182863     Source Type: Journal    
DOI: 10.1002/elsc.201200090     Document Type: Article

References (25)

1. Dittrich, P. S., Manz, A., Lab-on-a-chip: Microfluidics in drug discovery. Nat. Rev. Drug Discov. 2006, 5, 210-218.
2. Hong, J., Edel, J. B., deMello, A. J., Micro- and nanofluidic systems for high-throughput biological screening. Drug Discov. Today 2009, 14, 134-146.
3. Whitesides, G. M., The origins and the future of microfluidics. Nature 2006, 442, 368-373.
4. Koppitz, M., Eis, K., Automated medicinal chemistry. Drug Discov. Today 2006, 11, 561-568.
5. Gebinoga, M., Gross, G. A., Albrecht, A., Luebeck, T. et al., "Syn&Sort": A chip-based tool for combinatorial synthesis. QSAR Comb. Sci. 2006, 25, 1063-1068.
6. Mayer, G., Wohlfahrt, K., Schober, A., Köhler, J. M., in Microsystem Technology: A Powerful Tool for Biomolecular Studies (Biomethods) Köhler, J. M., Mejavaia, T., Saluz, H. P. (Eds.), Birkhäuser Verlag 1999, pp. 75-128.
7. Gordon, E. M., Barrett, R. W., Dower, W. J., Fodor, S. P. A. et al., Application of combinatorial technologies to drug discovery. 2. combinatorial organic-synthesis, library screening strategies, and future-directions. J. Med. Chem. 1994, 37, 1385-1401.
8. Houghten, R. A., Pinilla, C., Blondelle, S. E., Appel, J. R. et al., Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery. Nature 1991, 354, 84-86.
9. Gross, G. A., Mayer, G., Albert, J., Riester, D. et al., Spatially encoded single-bead Biginelli synthesis in a microstructured silicon array. Angew. Chem. Int. Ed. 2006, 45, 3102-3106.
10. Kozikowski, B. A., Burt, T. M., Tirey, D. A., Williams, L. E. et al., The effect of room-temperature storage on the stability of compounds in DMSO. J. Biomol. Screen. 2003, 8, 205-209.
11. Kozikowski, B. A., Burt, T. M., Tirey, D. A., Williams, L. E. et al., The effect of freeze/thaw cycles on the stability of compounds in DMSO. J. Biomol. Screen. 2003, 8, 210-215.
12. Hildmann, C., Riester, D., Schwienhorst, A., Histone deacetylases-an important class of cellular regulators with a variety of functions. Appl. Microbiol. Biotechnol. 2007, 75, 487-497.
13. Gross, G. A., Wurziger, H., Schlingloff, G., Schober, A., Microreactor array assembly, designed for diversity oriented synthesis using a multiple core structure library on solid support. QSAR Comb. Sci. 2006, 25, 1055-1062.
14. Schober, A., Schlingloff, G., Gross, A., Henkel, T. et al., Miniaturisation of synthesis and screening in nanotiterplates: the concept of NanoSynTest (TM). Microsyst. Technol. 2004, 10, 281-292.
15. Gross, G. A., Deppe, H., Tomandel, D., Wurziger, H. et al., Pipetting device with evaporation protection plate. US Patent Application 20030075557 A1.
16. Wegener, D., Wirsching, F., Riester, D., Schwienhorst, A., A fluorogenic histone deacetylase assay well suited for high-throughput activity screening. Chem. Biol. 2003, 10, 61-68.
17. Wegener, D., Hildmann, C., Riester, D., Schwienhorst, A., Improved fluorogenic histone deacetylase assay for high-throughput-screening applications. Anal. Biochem. 2003, 321, 202-208.
18. Riester, D., Wegener, D., Hildmann, C., Schwienhorst, A., Members of the histone deacetylase superfamily differ in substrate specificity towards small synthetic substrates. Biochem. Biophys. Res. Commun. 2004, 324, 1116-1123.
19. Gregoretti, I. V., Lee, Y. M., Goodson, H. V., Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis. J. Mol. Biol. 2004, 338, 17-31.
20. Nielsen, T. K., Hildmann, C., Dickmanns, A., Schwienhorst, A. et al., Crystal structure of a bacterial class 2 histone deacetylase homologue. J. Mol. Biol. 2005, 354, 107-120.
21. Hildmann, C., Ninkovic, M., Dietrich, R., Wegener, D. et al., A new amidohydrolase from Bordetella or Alcaligenes strain FB188 with similarities to histone deacetylases. J. Bacteriol. 2004, 186, 2328-2339.
22. Eigen, M., Gardiner, W., Evolutionary molecular engineering based on RNA repication. Pure Appl. Chem. 1984, 56, 967-978.
23. Eigen, M., The physics of molecular evolution. Chemi. Scr. 1986, 26B, 13-26.
24. Gebinoga, M., Katzmann, J., Fernekorn, U., Hampl, J. et al., Multiphoton structuring of native polymers: a case study for structuring natural proteins. Eng. Life Sci. 2013, DOI: 10.1002/elsc.201200152.
25. Schober, A., Fernekorn, U., Singh, S., Schlingloff, G. et al., Mimicking the biological world: methods for the 3D structuring of artificial cellular environments. Eng. Life Sci. 2013, DOI: 10.1002/elsc.201200088.