Intramolecularly-quenched near infrared fluorescent probes

Details Intramolecularly-quenched near infrared fluorescent probes Intramolecularly-quenched near infrared fluorescent probes

A - Human Necessities

61

K

A61K 49/00 (2006.01) A61K 41/00 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2328136

An intramolecularly-quenched, near infrared fluorescence probe that emits substantial fluorescence only after interaction with a target tissue (i.e., activation) is disclosed. The probe includes a polymeric backbone and a plurality of near infrared fluorochromes covalently linked to the backbone at fluoresence-quenching interaction-permissive positions separable by enzymatic cleavage at fluorescence activation sites. The probe optionally includes protective chains or fluorochrome spacers, or both. Also disclosed are methods of using the intramolecularly-quenched, near infrared fluorescence probes for in vivo optical imaging.

L'invention concerne une sonde fluorescente en proche infrarouge à extension intramoléculaire qui ne produit de fluorescence sensible qu'après avoir interagi avec un tissu cible, à savoir après l'activation. La sonde comprend un squelette polymère et plusieurs fluorochromes en proche infrarouge, liés par covalence au squelette dans des positions assurant l'extension de fluorescence et permettant les interactions, qui peuvent être séparées par clivage enzymatique dans les sites d'activation de la fluorescence. La sonde comprend éventuellement des chaînes protectrices ou des espaceurs fluorochromes ou les deux. L'invention concerne également des procédés d'utilisation des sondes fluorescentes en proche infrarouge à extension intramoléculaire destinées à l'imagerie optique in vivo.

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