Method for evaluating drug candidates

G - Physics – 01 – N

Patent

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G01N 33/53 (2006.01) G01N 33/543 (2006.01)

Patent

CA 2616418

Two-dimensional and/or three-dimensional polymeric or extended solid arrays comprising a polydiacetylene backbone, are used to evaluate the organic/water partition coefficient and/or oral absorptivity and/or ability of a compound to diffuse into cell membranes and/or transcellular permeability properties of a compound and/or the ionization state of a compound and/or the volume of distribution of a compound and/or the distribution of a compound into different tissues and/or the partitioning of a compound into cell organelles by monitoring the change in the fluorescence or phosphorescence upon exposure to the compound and optionally comparing it to a known change in fluorescence or phosphorescence, respectively. The method can also be used to evaluate the ability of a compound to bind to a protein.

L'invention porte sur des matrices bidimensionnelles ou tridimensionnelles polymères ou étendues, solides, comprenant une chaîne principale de polydiacétylène, permettant d'évaluer le coefficient de répartition matières organiques/eau et/ou l'absorptivité orale et/ou la capacité de diffusion dans les membranes cellulaires et/ou les propriétés de perméabilité transcellulaire d'un composé et/ou le niveau d'ionisation d'un composé et/ou le volume de distribution d'un composé et/ou la distribution d'un composé dans différents tissus et/ou la division d'un composé en organites cellulaires, par mesure du changement de fluorescence ou de phosphorescence lors de l'exposition des matrices au composé, et éventuellement par comparaison de cette mesure à une modification connue de la fluorescence ou de la phosphorescence. Ce procédé peut également servir à évaluer la capacité de liaison d'un composé avec une protéine.

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