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Logo of arthresbiomed central web sitesearch.manuscript submission.see also journal with issn 1478-6354registration.reference to the article.journal front page.
 
Arthritis Res. 2001; 3(Suppl A): L005.
Published online Jan 26, 2001. doi:  10.1186/ar153
PMCID: PMC3273231
The integration of functional genomics, combinatorial chemistry and nanotechnology into a miniaturized drug discovery process
M Auer1
1Novartis Forschungsinstitut GmbH, Dermatology, Fluorescence based HTS-Technology Program, Vienna, Austria
Supplement
21st European Workshop for Rheumatology Research
Conference
21st European Workshop for Rheumatology Research
1-4 March 2001
Vienna, Austria
Received January 15, 2001
Future concepts in miniaturized HTScreening technologies will concentrate on making optimal use of the two emerging technologies, combinatorial chemistry and functional genomics. To effectively exploit compounds from highly-parallel combinatorial synthesis and the high number of new target proteins from functional genomics, Novartis and Evotec BioSystems developed the CONA-BSP (confocal nanoscanning - bead scanning picking technology) as a novel high throughput - low hit-rate HTS process. In combination with the Novartis proprietary AIDA-Technology, quantitative on-bead confocal fluorescence screening can be combined with off-bead confirmation via a series of fluorescence techniques such as fluorescence anisotropy, or rotational correlation time applied to equilibrium binding studies.
Single molecule fluorescence spectroscopy and confocal nanoscanning/AIDA technology provide an optimal combination for a miniaturized automated uHTS process with high mechanistic resolution in functional and coupled assay systems.
  • Fluorescence correlation spectroscopy: Lead discovery by miniaturized HTS.
  • Auer M, Moore Keith J, Meyer-Almes F-J, Guenther R, Pope AJ, Stoeckli KA. Drug Discovery Today, 1998. pp. 457–465. [Cross Ref]
  • Auer M, Gstach H. Fluorescent dyes (AIDA) for solid phase and solution phase screening. United States Patent, WO 00/37448.
  • Meyer-Almes FJ, Auer M. Enzyme inhibition assays with fluorescence correlation spectroscopy: A new algorithm for the derivation of kcat/Km and Ki values at substrate concentrations lower than the Michaelis Menten constant. Biochemistry. 2000;39(43):13261–13268. doi: 10.1021/bi000057y. [PubMed] [Cross Ref]
  • The integration of single molecule detection technologies into miniaturized drug screening: Current status and future perspectives.
  • Bühler C, Stöckli K, Auer M. Review in press: Fluorescence Spectroscopy: Valeur/Brochon, Trends in Fluorescence Spectroscopy (Springer Verlag, 2001)
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