Screen employing fluorescence anisotropy to identify...

C - Chemistry – Metallurgy – 12 – Q

Patent

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C12Q 1/68 (2006.01)

Patent

CA 2282418

The present invention provides methods for screening for bioactive compounds, in particular those that bind to RNA sequences involved in the pathogenesis of disease or in regulation of a physiological function. The methods involve assessing the stability and/or the conformation of an RNA target in the presence and absence of test ligands, and identifying as a ligand any test ligand that causes a measurable change in target RNA stability and/or conformation. In a preferred embodiment, the effect of a ligand on target RNA stability and/or conformation is assessed by measuring the fluorescence polarization of a fluorescently labeled probe.

La présente invention concerne des méthodes de sélection de composés bioactifs, notamment ceux se liant à des séquences d'ARN intervenant dans la pathogenèse d'une affection ou dans la régulation d'une fonction physiologique. Les méthodes consistent à évaluer la stabilité et/ou la conformation d'un ARN cible en présence et en l'absence de ligands d'essai, et à identifier comme ligand tout ligand d'essai provoquant une modification mesurable dans la stabilité et/ou la conformation d'un ARN cible. Dans un mode de réalisation préféré, l'effet d'un ligand sur la stabilité et/ou la conformation d'un ARN cible est évalué par mesure de la polarisation de fluorescence d'une sonde marquée avec des éléments fluorescents.

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