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A pretargeted imaging strategy based on the HaloTag dehalogenase enzyme is described. Here, a HaloTag–Trastuzumab conjugate has been used as the primary agent targeting HER2 expression, and three new radiolabelled HaloTag ligands have been used as secondary agents, two of which offer dual-modality (SPECT/optical) imaging capability.

Graphical abstract: Development of an enzymatic pretargeting strategy for dual-modality imaging

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