Combination of PET and CXCR4-Targeted Peptide Molecule Agents for Noninvasive Tumor Monitoring

Precision medicine is emphasizing not only at individual but also at disease molecule level in modern medicine. Therefore, target-specific molecular agents are crucial for precise diagnosis and treatment. We developed a peptide agent that binds a critical chemokine receptor-CXCR4 and could be used to detect tumor status. Confocal images showed binding of the peptide agent to human osteosarcoma cells. Clinical gold-standard molecular imaging agent PET showed tumors had high glucose metabolism, CT showed that these xenograft tumors were calcified and displayed hypervascularity. Peptide imaging demonstrated that these tumors were CXCR4 positive. However, Western blot protein analysis revealed a discordance between the tumor and the CXCR4 targeted agent, suggesting that small changes in peptide sequences have profound effect on binding to their targets. We also demonstrated the molecular screening by modifying the peptide sequence and thereby altering the binding properties of the agent. In conclusion, this study demonstrates that small molecule peptide agents can be used as an additional diagnostic tool for precision medicine.