Folate conjugation to HT2 enhances selective receptor-targeting efficacy in folate receptor-expressing tumors, demonstrating potential as a PET imaging agent for tumor diagnosis.
Animal data support folate receptor-targeted PET tracer development; leaves open human translation and clinical validation.
The tissue inhibitor of metalloproteinase-2 (TIMP-2) inhibits matrix metalloproteinases activity and modulates cellular proliferation and apoptosis. The human serum albumin-TIMP-2 with folic acid conjugate (termed HT2-folate) was synthesized to promote uptake through folate receptors (FRs), and a corresponding radio-labeled compound was prepared for tumor diagnosis by positron emission tomography (PET). <TEX>⁶⁸Ga</TEX>-NOTA-HT2-folate was synthesized from <TEX>⁶⁸Ga</TEX> and the NOTA chelator with HT2-folate. The fusion protein was identified using MALDI-TOF mass spectrometry. The radioligand was prepared with a high radiochemical yield. Cell-surface association of <TEX>⁶⁸Ga</TEX>-NOTA-HT2-folate significantly increased over time in FR-positive tumor cells. In animal PET and biodistribution studies, tumor uptake was very high as early as 1 h after radioligand injection. Folate conjugation enhanced the selective receptor-targeting efficacy of HT2 in FRexpressing tumors, and its radioligand will be useful as an in vitro tool and for in vivo tumor diagnosis by PET imaging.
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Kim et al. (2013) studied this question.
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