Quenched dendrimeric dyes for bright detection

C - Chemistry – Metallurgy – 09 – B

Patent

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Details

C09B 11/22 (2006.01) C09B 11/02 (2006.01) C09B 23/06 (2006.01) C09B 23/08 (2006.01) C12Q 1/04 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2752854

The present invention presents designs for high extinction quenched "dyedrons" that can be activated by conver-sion of a single acceptor/quencher in the molecular assembly to a fluorescent state. The quencher is activated by noncovalent binding to a unique complementary expressible fluorogen activating peptide (FAP). In this way, the quencher serves as the homo-geneous switch, receiving energy efficiently from each of the donor molecules of the dendronic antenna, and releasing it as fluo-rescence only when activated by binding. The sum of the extinction of the multiple dyes on the antenna will provide dramatic en-hancements in the effective brightness of the probe in standard imaging systems. This approach provides a set of probes with ex-ceptional brightness, specifically targeted to an expressed tag that activates the fluorescence of the dyedron.

La présente invention porte sur des conceptions de colorants dendrimères (« dyedrons ») désactivés à extinction élevée qui peuvent être activés par la conversion d'un accepteur/désactivateur unique dans l'assemblage moléculaire, en un état fluorescent. Le désactivateur est activé par une liaison non covalente à un peptide d'activation de fluorogène pouvant être exprimé complémentaire unique (FAP). De cette façon, le désactivateur sert de commutateur homogène, recevant de l'énergie efficacement à partir de chacune des molécules donneuses de l'antenne dendronique, et la libérant sous forme de fluorescence uniquement lorsqu'il est activé par liaison. La somme de l'extinction des multiples colorants sur l'antenne fournira des améliorations remarquables dans la brillance efficace de la sonde dans des systèmes d'imagerie standard. Cette approche fournit un ensemble de sondes avec une brillance exceptionnelle, ciblé de façon spécifique vers un marqueur exprimé qui active la fluorescence du colorant dendrimère.

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