Fluorine nmr spectroscopy for biochemical screening

Details Fluorine nmr spectroscopy for biochemical screening Fluorine nmr spectroscopy for biochemical screening

C - Chemistry, Metallurgy

12

Q

C12Q 1/00 (2006.01) C12Q 1/37 (2006.01) C12Q 1/42 (2006.01) C12Q 1/48 (2006.01)

Patent

CA 2531339

High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.

Le procédé de criblage à fort rendement (HTS) de grosses bibliothèques de composés est actuellement celui qui permet des découvertes conduisant à des médicaments, et il est maintenant bien accepté que pour un essai de fonctionnalités la qualité l'emporte sur la quantité. La méthode biochimique RMN originellement proposée par Percival et Withers (Biochemistry, 1992, 31, 498-505) est étendue au criblage des Ser/Thr kinases. Ladite méthode, qui requiert la présence sur le substrat d'un fragment de CF¿3? (ou de CF), utilise la spectroscopie ?19¿F RMN pour détecter les substrats de départ, et enzymatiquement modifiés. Les expériences peuvent se faire en temps réel ou en dans le cadre d'un essai en fin de réaction, en utilisant des concentrations de protéines et de substrats comparables à celles utilisées dans les autres techniques HTS. L'invention présente une application de cette technique à la phosphorylation d'un substrat, utilisant la Ser/Thr kinase AKT1.

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