A fluorescence-based screening method for identifying ligands

G - Physics – 01 – N

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G01N 33/53 (2006.01) C12Q 1/68 (2006.01) G01N 33/58 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2236339

A novel method for screening chemical compounds for potential pharmaceutical effectiveness is provided. The disclosed method identifies possible therapeutic test ligands by placing them in the presence of target proteins and determining the ability of test ligands to prevent the partial unfolding of the target protein by measuring the fluorescence emission of a conformation- sensitive probe. This differs significantly from known methods of novel pharmaceutical testing in that the biochemical function of the target protein need not be known and the existence of any known ligands of the target protein is unnecessary.

L'invention concerne un nouveau procédé d'évaluation de l'efficacité pharmaceutique de composés chimiques. Le procédé décrit permet d'identifier des ligands ayant une valeur thérapeutique en les mettant en présence de protéines cibles et en déterminant leur capacité à empêcher le dépliement partiel de la protéine cible, ceci en mesurant l'émission de la fluorescence d'une sonde sensible à la conformation. Ce procédé diffère sensiblement des procédés connus d'évaluation de nouveaux composés pharmaceutiques en ce que la fonction biochimique de la protéine cible n'a pas besoin d'être connue et en ce que l'existence de ligands connus de la protéine cible n'est pas une nécessité.

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