Compounds having affinity for integrins, the synthesis of these compounds, and the use of these compounds as ligands to facilitate the delivery of cargo molecules to cells expressing integrins are described. The described integrin targeting ligands have serum stability and affinity for αvβ3 integrin and/or αvβ5 integrin, and are suitable for conjugation to cargo molecules, such as oligonucleotide-based therapeutic agents (e.g., RNAi agents), to facilitate delivery of the cargo molecules to cells and tissues, such as tumor cells, that express integrin αvβ3, integrin αvβ5, or both integrin αvβ3 and integrin αvβ5. Compositions that include integrin targeting ligands and methods of use are also described.本發明描述對整合素具有親和力之化合物、此等化合物之合成及此等化合物作為有助於將貨物分子(cargo molecule)遞送至表現整合素之細胞的配體的用途。該等所描述之整合素靶向配體具有血清穩定性及對於αvβ3整合素及/或αvβ5整合素之親和力，且適合於結合貨物分子，諸如基於寡核苷酸之治療劑(例如RNAi試劑)，以有助於將該等貨物分子遞送至諸如腫瘤細胞之表現整合素αvβ3、整合素αvβ5或整合素αvβ3與整合素αvβ5兩者之細胞及組織。本發明亦描述包括整合素靶向配體之組合物及使用方法。
