The use of monolabeled tumor-targeting peptides for molecular imaging is widespread. However, it is often desirable to use the same compound for different clinical applications, e.g., combined pre- and intraoperative tumor detection. On the basis of their detection sensitivity, the combination of radioactivity and fluorescence is probably the most valuable in multimodal molecular imaging. In this review, we compare multimodal peptide derivatives and discuss the influence of the diagnostic labels on receptor affinity and biodistribution. On the basis of the described constructs, we propose improvements for the design of future multimodal tumor-targeting peptide derivatives.
The antagonistic Ac-TZ14011 peptide, which binds the CXCR4 receptor, has been labeled with a multifunctional single-attachment-point, MSAP, reagent to obtain a peptide derivative for multimodal imaging. The imaging label contained a DTPA chelate and a fluorescent dye with Cy5.5 spectral properties. Flow cytometry and confocal microscopy showed specific receptor binding of the multimodal peptide, regardless of the presence of indium in the chelate.
The interaction between the chemokine receptor 4 (CXCR4) and stromal cell-derived factor-1 (SDF-1, also known as CXCL12) is a natural regulatory process in the human body. However, CXCR4 over-expression is also found in diseases such as cancer, where it plays a role in, among others, the metastatic spread. For this reason it is an interesting biomarker for the field of diagnostic oncology, and therefore, it is gaining increasing interest for applications in molecular imaging. Especially ''small-molecule'' imaging agents based on T140, FC131 and AMD3100 have been extensively studied. SDF-1, antibodies, pepducins and bioluminescence have also been used to visualize CXCR4. In this critical review reported CXCR4 targeting imaging agents are described based on their affinity, specificity and biodistribution. The level wherein CXCR4 is up-regulated in cancer patients and its relation to the different cell lines and animal models used to evaluate the efficacy of the imaging agents is also discussed (221 references).
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