首页> 外国专利> A 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

A 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

机译:通过调节内表面功能和配体部分之间的化学计量比来提高多价配体的肿瘤诊断效率的方法

摘要

The present invention relates to a method for improving tumor diagnostic efficiency by controlling the ratio of inner surface functionality of a multivalent ligand and a ligand moiety of a tumor target, and a multivalent ligand for diagnosing a tumor. According to the present invention, the ratio of the inner surface functionality of the multivalent ligand and the ligand moiety of the tumor target is controlled to administer the same to a living body when diagnosing the tumor. If a ligand moiety binds to a specific receptor which is expressed on a surface of tumor cells in advance, a phenomenon, in which other homogeneous receptors are gathered around the bound receptor, occurs. Other ligand moiety, which could not be bound, is bound more easily to the gathered receptors in a multivalent manner. A type of the inner surface functionality, which is appropriately selected to be closer to a cell surface due to the bound ligand moiety, interacts with the surface of the tumor cells by an attractive force, thereby significantly improving the avidity in which the ligand moiety, which could not be bound, additionally and simultaneously is bound to the gathered receptors.
机译:本发明涉及通过控制多价配体和肿瘤靶标的配体部分的内表面官能度之比来提高肿瘤诊断效率的方法,以及用于诊断肿瘤的多价配体。根据本发明,在诊断肿瘤时,控制多价配体的内表面官能度与肿瘤靶标的配体部分的比率,以将其给予活体。如果配体部分与预先在肿瘤细胞表面表达的特定受体结合,则会发生在结合的受体周围聚集其他均质受体的现象。不能结合的其他配体部分更容易以多价方式结合到收集的受体上。由于结合的配体部分A型的内表面的功能,其被适当地选择以更接近细胞表面上,通过一个有吸引力的力与肿瘤细胞的表面相互作用,从而显著改善亲合力,其中所述配体部分,不能被束缚的蛋白,另外并且同时被束缚在聚集的受体上。

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