21st European Workshop for Rheumatology Research
- Meeting abstract
The integration of functional genomics, combinatorial chemistry and nanotechnology into a miniaturized drug discovery process
Arthritis Research & Therapy volume 3, Article number: L005 (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.
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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. 10.1021/bi000057y.
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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Auer, M. The integration of functional genomics, combinatorial chemistry and nanotechnology into a miniaturized drug discovery process. Arthritis Res Ther 3, L005 (2001). https://doi.org/10.1186/ar153
- Correlation Time
- Functional Genomic
- Discovery Process
- Fluorescence Anisotropy
- Fluorescence Technique