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Natural product lead discovery at the microgram scale - an integrated approach

Description: Das Projekt "Natural product lead discovery at the microgram scale - an integrated approach" wird vom Umweltbundesamt gefördert und von Universität Basel, Department Pharmazeutische Biologie durchgeführt. Natural products remain an important source for drugs and a source of inspiration for medicinal chemists for the design of synthetic drugs and probes for the study of biological functions. The contribution of academic laboratories in natural products discovery has been substantial. The limiting factor of pharmaceutical natural product research has been with the tedious process of purification and identification of the lead molecules from the highly complex crude extract. Recent technological advances enable now a miniaturization of the screening and discovery process for natural product leads. The proposal here is for the purchase of a 500 MHz NMR spectrometer specifically equipped for the measurement of mass limited samples. It includes a recently commercialized 1 mm probe and autosampler and is capable of recording 1D and 2D NMR spectra with microgram (20-100 myg) amounts of natural products and synthetic drug-like molecules. The spectrometer is configured to fit into the technology platforms and the workflows of the Drug Screening Group of the Swiss Tropical Institute and the Institute of Pharmaceutical Biology. The instrument shall be used for various interdisciplinary projects of the two principal applicants and for a consortium which is being established. The major use will be for HPLC-based lead discovery in the area of Alzheimer's disease, Malaria, and neglected tropical diseases. The instrument will also be employed for metabolic fingerprinting of selected plants and phytomedicines. A third application will be in the analysis of compound libraries from external sources which are screened by the applicants in the context of the principal projects. An NMR instrument with this configuration is currently not in operation at a Swiss university. It is the missing link in a technology platform established at the laboratories of the two applicants. This platform should enable a paradigm shift in the way how natural product leads are identified, namely by miniaturizing the entire process of screening, separation and lead identification to the microgram level. A significant gain in efficiency of the discovery process and, thus, in research productivity, both qualitative and quantitative, is anticipated. The equipment will also be of interest to all those scientists in the biomedical sciences who need structural information from mass limited samples such as, for example drug metabolites.

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SupportProgram

Origin: /Bund/UBA/UFORDAT

Tags: Biopharmazeutikum ? Basel ? Arzneimittel ? Skigebiet ? Blei ? Malaria ? Schweiz ? Biologie ? Stoffwechselprodukt ? Tropenkrankheit ? Studie ? Technik ? Reinigung ? Reinigungsverfahren ? Messung ? Bedarf ? Forschung ? Forschungseinrichtung ? Krankheit ? Naturprodukt ? Produktivität ? Spektrum ? Planung ? VERARBEITEN ? AUSGEWAEHLT ? VERBINDUNG ? VORSCHLAEGE ? VORSCHLAG ? WICHTIG ? WISSENSCHAFT ? Werkzeug ? AUSRUESTUNG ? Antragsteller ? BEISPIEL ? BEITRAG ? BETRAG ? Bahnsteig ? EINGESCHRAENKT ? EINSATZ ? EINSCHRAENKENDER FAKTOR ? EXTERN ? FAEHIG ? FORTSCHRITTLICH ? FUNKTION ? GEBRAUCHT ? GEMISCHT ? GRUPPE ? KAUF ? NEU ? PROBE ? PROJEKT ? Siebung ? TECHNOLOGISCH ? AKADEMISCH ?

License: cc-by-nc-nd/4.0

Language: Deutsch

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Time ranges: 2007-06-01 - 2008-05-31

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