Arrowhead Pharmaceuticals, Inc.
INTEGRIN TARGETING LIGANDS AND USES THEREOF

Abstract:

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 .alpha.v.beta.3 integrin and/or .alpha.v.beta.5 integrin, and are suitable for conjugation to cargo molecules, such as 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 .alpha.v.beta.3, integrin .alpha.v.beta.5, or both integrin .alpha.v.beta.3 and integrin .alpha.v.beta.5. Compositions that include integrin targeting ligands and methods of use are also described.