DR5-B-iRGD

DR5-B-iRGD is an experimental recombinant fusion protein designed for targeted oncology, particularly pancreatic cancer. It consists of a Death Receptor 5 (DR5)-selective variant of the Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand (TRAIL), known as DR5-B, fused to the internalizing RGD (iRGD) peptide. The DR5-B component is engineered to specifically bind and activate DR5 (TNFRSF10B) to induce apoptosis in cancer cells while avoiding interaction with decoy receptors and Death Receptor 4 (DR4), thereby reducing potential systemic toxicity. The iRGD peptide (sequence: CRGDKGPDC) enhances the protein's therapeutic index by facilitating tumor-specific homing through binding to αvβ3 and αvβ5 integrins on tumor endothelium, followed by a proteolytic cleavage that allows it to interact with neuropilin-1 (NRP-1) to trigger deep tissue penetration and cell internalization. In preclinical research, DR5-B-iRGD has been utilized as a functionalizing agent in nanocarriers, such as amphiphilic poly(N-vinylpyrrolidone) biocomposites, to deliver synergistic combinations with agents like bortezomib.

Other names

DR5-selective TRAIL-iRGD fusion proteinDR-5-selective TRAIL-iRGD fusion proteinDR 5-selective TRAIL-iRGD fusion proteinDR5-B-iRGD fusion proteinDR-5-B-iRGD fusion proteinDR 5-B-iRGD fusion protein