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Development and Preclinical Evaluation of 68Ga-Labeled B7-H3-Specific Bicyclic Peptides as Immuno-PET Tracers for Oncology
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DOI：10.1021/acs.jmedchem.6c00961.png)
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Abstract
En 中文
B7-H3 (CD276) is an emerging target for cancer theranostics, highlighting the need for imaging probes capable of noninvasively quantifying B7-H3 expression in tumors. Here, we developed three 68Ga-labeled B7-H3-targeting bicyclic peptide tracers with different PEG linker lengths. All tracers showed high radiochemical purity (>96%), favorable in vitro stability, and rapid blood clearance. Among them, [68Ga]Ga-B7H3-FZ1 exhibited the highest affinity (KD = 83.22 nM). Micro-PET/CT imaging demonstrated that tumor uptake of [68Ga]Ga-B7H3-FZ1 correlated positively with B7-H3 expression across multiple tumor models. In H1299 tumors. B7-H3 overexpression increased uptake from 1.09 ± 0.18 to 3.50 ± 0.97%ID/g at 30 min postinjection, confirming target specificity. Biosafety studies indicated no obvious toxicity. These results support [68Ga]Ga-B7H3-FZ1 as a promising PET tracer for noninvasive B7–H3 imaging.
Keywords:
PET/CT
B7-H3
bicyclic peptide
68Ga
solid tumor
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6.8
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2.7W
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9.4W
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