10R-RGD-siRNA

10R-RGD-siRNA is a research-stage, cell-penetrating peptide (CPP)-based siRNA delivery complex designed for the targeted treatment of triple-negative breast cancer (TNBC). The complex consists of a bifunctional peptide carrier—comprising a 10R polyarginine stretch fused to a linear RGD integrin-targeting motif—complexed with a small interfering RNA (siRNA) payload. The RGD motif targets the αvβ3 integrin receptor overexpressed on tumor cells to facilitate receptor-mediated endocytosis, while the 10R polyarginine component enables cell penetration and endosomal escape. In preclinical proof-of-concept studies, the complex was loaded with siRNA targeting Lactate Dehydrogenase C (LDHC), a metabolic enzyme highly expressed in TNBC. This formulation (10R-RGD:siLDHC) demonstrated significant LDHC knockdown, reduced TNBC cell clonogenicity, enhanced sensitivity to the PARP inhibitor olaparib, and reduced tumor growth in zebrafish xenograft models without apparent toxicity.

Other names

10R-RGD-siRNA10R-RGD:siLDHC10R-RGD:siRNA