Modulating Protein-Protein Interactions

Protein-protein interactions (PPIs) play an important role in almost all vital processes involved in many diseases, especially cancer. Peptides are perfect candidates that modulate PPIs as they can closely mimic principle features of protein. However, the intrinsic drawbacks of peptides, including poor stability and member impenetrability, severely limit the development of peptide-derived therapeutics. Nanotechnology offers a feasible route for anti-cancer peptide delivery, but much remains to be done, especially with respect to the pressing need for a simple method for efficient delivery of peptides into sites of interest towards potent and safe therapy. Herein, we report a one-step method to conjugate lanthanide-doped nanoparticles with p53-activating peptide (PMI: TSFAEYWALLSP), Bcl2-blocking peptide (BIM: IWIAQELRRIGDEFNAYYARR) and CD13-binding peptide (iNGR: CRNGRGPDC) by mercaptogenic self-assembly. The resultant LDN-iNGRPMI-BIM nanoparticles can tumor-specifically accumulate at interest sites, and potently induce apoptosis of cancer cells