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• W1997987445 abstract "Melanoma is a malignant tumor derived from epidermal melanocytes, and it is known for its aggressiveness, therapeutic resistance, and predisposition for late metastasis. Very late antigen-4 (VLA-4; also called integrin α₄β₁) is a transmembrane noncovalent heterodimer overexpressed in melanoma tumors that plays an important role in tumor growth, angiogenesis, and metastasis by promoting adhesion and migration of cancer cells. In this study, we evaluated 2 conjugates of a high-affinity VLA-4 peptidomimetic ligand, LLP2A, for PET/CT imaging in a subcutaneous and metastatic melanoma tumor. <b>Methods:</b> LLP2A was conjugated to 1,4,8,11-tetraazacyclotetradecane-1-(methane phosphonic acid)-8-(methane carboxylic acid) (CB-TE1A1P) and 2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid (NODAGA) chelators for ⁶⁸Ga and ⁶⁴Cu labeling. The conjugates were synthesized by solid-phase peptide synthesis, purified by reversed-phase high-performance liquid chromatography, and verified by liquid chromatography mass spectrometry. Saturation and competitive binding assays with B16F10 melanoma cells determined the affinity of the compounds for VLA-4. The biodistributions of the LLP2A conjugates were evaluated in murine B16F10 subcutaneous tumor–bearing C57BL/6 mice. Melanoma metastasis was induced by intracardiac injection of B16F10 cells. PET/CT imaging was performed at 2, 4, and 24 h after injection for the ⁶⁴Cu tracers and 1 h after injection for the ⁶⁸Ga tracer. <b>Results:</b>⁶⁴Cu-labeled CB-TE1A1P-PEG₄-LLP2A and NODAGA-PEG₄-LLP2A showed high affinity to VLA-4, with a comparable dissociation constant (0.28 vs. 0.23 nM) and receptor concentration (296 vs. 243 fmol/mg). The tumor uptake at 2 h after injection was comparable for the 2 probes, but ⁶⁴Cu-CB-TE1A1P-PEG₄-LLP2A trended toward higher uptake than ⁶⁴Cu-NODAGA-PEG₄-LLP2A (16.9 ± 2.2 vs. 13.4 ± 1.7 percentage injected dose per gram, <i>P</i> = 0.07). Tumor-to-muscle and tumor-to-blood ratios from biodistribution and PET/CT images were significantly higher for ⁶⁴Cu-CB-TE1A1P-PEG₄-LLP2A than ⁶⁴Cu-NODAGA-PEG₄-LLP2A (all <i>P</i> values < 0.05). PET/CT imaging of metastatic melanoma with ⁶⁸Ga-NODAGA-PEG₄-LLP2A and ⁶⁴Cu-NODAGA-PEG₄-LLP2A showed high uptake of the probes at the site of metastasis, correlating with the bioluminescence imaging of the tumor. <b>Conclusion:</b> These data demonstrate that ⁶⁴Cu-labeled CB-TE1A1P/NODAGA LLP2A conjugates and ⁶⁸Ga-labeled NODAGA-LLP2A are excellent imaging agents for melanoma and potentially other VLA-4–positive tumors. ⁶⁴Cu-CB-TE1A1P-PEG₄-LLP2A had the most optimal tumor–to–nontarget tissue ratios for translation into humans as a PET imaging agent for melanoma." @default.
• W1997987445 created "2016-06-24" @default.
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• W1997987445 date "2014-09-25" @default.
• W1997987445 modified "2023-10-17" @default.
• W1997987445 title "PET Imaging of Very Late Antigen-4 in Melanoma: Comparison of⁶⁸Ga- and⁶⁴Cu-Labeled NODAGA and CB-TE1A1P-LLP2A Conjugates" @default.
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• W1997987445 doi "https://doi.org/10.2967/jnumed.114.144881" @default.
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