Drug intelligence / Profile preview

RA-S-S-Cy

Development stage
Preclinical
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intravenous
01

Overview

RA-S-S-Cy is a mitochondria-targeted theranostic conjugate composed of the natural cyclopeptide RA-V (derived from *Rubia akane*) covalently linked to the near-infrared (NIR) fluorophore Cy5.5 via a glutathione (GSH)-responsive disulfide linker. Designed for the treatment and imaging of colon cancer, RA-S-S-Cy is typically delivered via a hyaluronic acid-coated liposomal system. Upon internalization into cancer cells and localization to the mitochondria, the disulfide bond is cleaved by high intracellular GSH levels, releasing the therapeutic cyclopeptide RA-V and activating the NIR fluorescence of Cy5.5 for real-time monitoring. RA-V exerts its anti-tumor activity by binding to eukaryotic translation elongation factor 1 alpha (eEF1A), thereby inhibiting protein synthesis and inducing apoptosis in cancer cells.

Other names
RA-V-disulfide-Cy5.5RA-V-disulfide-Cy-5.5RA-V-disulfide-Cy 5.5

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