The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand-targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.
本发明涉及用于在体内向整合素阳性肿瘤细胞传递RNA干扰(RNAi)触发剂的组合物。这些组合物包括以RGD
配体为靶向的两性膜活性聚胺,其可逆修饰为酶可切割的二肽-酰胺基
苯甲酸酯掩蔽剂。修饰掩蔽了聚合物的膜活性,而可逆性提供了生理响应性。可逆修饰的聚胺(动态聚结合物或结合物)进一步共价连接到RNAi触发剂。