Method to improve the tumor diagnostic efficiency of multivalent ligands by regulating the stoichiometric ratio between inner surface functionalities and ligand moieties for tumor targeting

摘要

Disclosed herein is a method of improving tumor diagnostic efficiency of multivalent ligands by regulating the stoichiometric ratio between inner surface functionalities and ligand moieties for tumor targeting, and the multivalent ligands for tumor diagnosis.

主权项

1. A method to regulate the tumor diagnostic efficiency of a multivalent ligand by regulating the stoichiometric ratio between inner surface functionalities and ligand moieties for tumor targeting, wherein the multivalent ligand comprises:
a single core consisting of a circular or spherical symmetric small molecular compound, or a radial-shaped macromolecule, wherein the core comprises terminal functional groups; said ligand moieties which are attached to a portion of the terminal functional groups of the core through a spacer; said inner surface functionalities comprising the terminal functional groups, modified terminal functional groups or the combination thereof; and one or more imaging agents which are attached to another portion of the terminal functional groups of the core; wherein the inner surface functionalities interact attractively with the surface of the tumor; and wherein the number of ligand moieties for tumor targeting accounts for 5-90% of the total number of inner surface functionalities and ligand moieties for tumor targeting.