Novel Peptide-Based PET Probe for Non-invasive Imaging of C-X-C Chemokine Receptor Type 4 (CXCR4) in Tumors

<p>These are RAW data datasets of the following final paper</p> <p>Trotta, A.M., Aurilio, M., D&#39;Alterio, C., Ieran&ograve;, C., Di Martino, D., Barbieri, A., Luciano, A., Gaballo, P., Santagata, S., Portella, L., Tomassi, S., Marinelli, L., Sementa, D., Novellino, E., Lastoria, S., Scala, S., Schottelius, M., Di Maro, S.</p> <p>Novel Peptide-Based PET Probe for Non-invasive Imaging of C-X-C Chemokine Receptor Type 4 (CXCR4) in Tumors, (2021) Journal of Medicinal Chemistry, 64 (6), pp. 3449-3461. ISSN 00222623</p> <p>https://doi.org/10.1021/acs.jmedchem.1c00066</p> <p>Abstract</p> <p>The recently reported CXCR4 antagonist 3 (Ac-Arg-Ala-[DCys-Arg-2Nal-His-Pen]-CO2H) was investigated as a molecular scaffold for a CXCR4-targeted positron emission tomography (PET) tracer. Toward this end, 3 was functionalized with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and 1,4,7-triazacyclononanetriacetic acid (NOTA). On the basis of convincing affinity data, both tracers, [68Ga]NOTA analogue ([68Ga]-5) and [68Ga]DOTA analogue ([68Ga]-4), were evaluated for PET imaging in &ldquo;in vivo&rdquo; models of CHO-hCXCR4 and Daudi lymphoma cells. PET imaging and biodistribution studies revealed higher CXCR4-specific tumor uptake and high tumor/background ratios for the [68Ga]NOTA analogue ([68Ga]-5) than for the [68Ga]DOTA analogue ([68Ga]-4) in both in vivo models. Moreover, [68Ga]-4 and [68Ga]-5 displayed rapid clearance and very low levels of accumulation in all nontarget tissues but the kidney. Although the high tumor/background ratios observed in the mouse xenograft model could partially derive from the hCXCR4 selectivity of [68Ga]-5, our results encourage its translation into a clinical context as a novel peptide-based tracer for imaging of CXCR4-overexpressing tumors.</p> <p>&nbsp;</p> <p>&nbsp;</p>