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1. 发明申请

WO2005115457A3 COMBINED ACTIVE AND PASSIVE TARGETING OF BIOLOGICALLY ACTIVE AGENTS 审中-公开
标题翻译：生物活性剂的主动和被动目标的组合
公开(公告)号：WO2005115457A3
公开(公告)日：2009-04-09
申请号：PCT/US2005015681
申请日：2005-05-05
申请人： UNIV UTAH RES FOUND , CUCHELKAR VAIKUNTH , KOPECHOVA PAVLA , PETERSON C MATTHEW , KOPECEK JINDRICH
发明人： CUCHELKAR VAIKUNTH , KOPECHOVA PAVLA , PETERSON C MATTHEW , KOPECEK JINDRICH
IPC分类号： C07K14/00 , A61K39/40 , A61K47/48 , C07K16/00 , C07K16/30
CPC分类号： A61K41/0071 , A61K47/554 , A61K47/58 , A61K47/65 , A61K47/6869 , C07K16/3069 , C07K2319/09
摘要： Disclosed is a conjugate comprising a biologically active agent (drug) linked to a subcellular targeting moiety that targets a drug specifically to the nucleus. Targeting is achieved by attaching a steroid hormone (or an analog) to the drug. The steroid hormone attached to the drug binds its corresponding receptor; the formation of the receptor-ligand complex results in the internalization of the complex into the nucleus, thus resulting in nuclear translocation of the drug. Also disclosed is a conjugate (comprising the complex of the drug and the steroid hormone) bound to a polymer by spacers allowing for concurrent passive targeting to the tumor cell (afforded by attachment to the polymer by the EPR effect) and nuclear targeting of the conjugate (due to the presence of the steroid). Using a suitable degradable spacer allows for the release of free drug in the tumor and enhances nuclear targeting efficacy. The polymer can be further linked to a cellular targeting molecule, where the targeting molecule directs the polymer to specific cells. One may thus be able to effectively target drugs to the nucleus of tumor cells. With little or modifications, several therapeutic agents can be targeted using the invention.
摘要翻译：公开了包含与亚细胞靶向部分连接的生物活性剂（药物）的缀合物，所述亚细胞靶向部分特异性靶向细胞核。通过将类固醇激素（或类似物）连接到药物来实现靶向。附着在药物上的类固醇激素与其相应的受体结合; 受体 - 配体复合物的形成导致复合物内化到细胞核中，从而导致药物的核易位。还公开了通过间隔物与聚合物结合的缀合物（包括药物和类固醇激素的复合物），其允许同时被动靶向肿瘤细胞（通过EPR效应与聚合物连接）和缀合物的核靶向（由于存在类固醇）。使用合适的可降解间隔物可以释放肿瘤中的游离药物并增强核靶向功效。聚合物可以进一步连接到细胞靶向分子，其中靶向分子将聚合物引导到特定细胞。因此，可以有效地将药物靶向肿瘤细胞的核。通过少量或修改，可以使用本发明靶向几种治疗剂。

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