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Synthesis, Purification, and Tumor Cell Uptake of 67Ga-Deferoxamine−Folate, a Potential Radiopharmaceutical for Tumor Imaging

Wang, Susan, Lee, Robert J., Mathias, Carla J., Green, Mark A., Low, Philip S.·1996·Bioconjugate Chemistry

Abstract

The vitamin folic acid was covalently linked to the chelating agent deferoxamine (DF) via an amide bond using a simple carbodiimide coupling reaction. A mixture of two isomers, DF--folate(alpha) and DF--folate(gamma), was produced involving the alpha- and gamma-carboxyl group of folic acid, respectively. These two isomers were separated by anion-exchange chromatography using a NH4HCO3 gradient. Competitive binding studies revealed that only the DF-folate(gamma) is recognized by the folate receptor on KB cells, interacting with an affinity comparable to unconjugated folic acid. The DF--folate conjugates were radiolabeled with the gamma-emitting radionuclide 67Ga3+ and tested for uptake by cultured KB cells overexpressing the folate receptor. The cellular accumulation of 67Ga-DF-folate(gamma) tracer exhibited rapid uptake kinetics in cell culture with a t1/2 of approximately 3 min. The KB cell association of 67Ga-DF--folate(gamma) was competitively blocked by free folic acid, indicating that uptake of the 67Ga-DF--folate(gamma) was specifically mediated by the folate receptor. Since the folate receptor is overexpressed on the surfaces of many neoplastic cells, these results suggest that 67Ga-DF--folate(gamma) complex might be useful as a diagnostic agent for noninvasive imaging of folate receptor-positing tumors.

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Metadata

Authors
Wang, S., Lee, R. J., Mathias, C. J., Green, M. A., & Low, P. S.
Venue
Bioconjugate Chemistry
Published
1996-01-01
Volume
7
Issue
1
Pages
56-62
ISSN
  • 1043-1802 (ISSN-L)
  • 1520-4812
OpenAlex
W1986177211
Cited by
245
References
0
FWCI
7.60
Type
journal article
Language
en
Open access
closed

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CoChat. (2026). Citation check: Synthesis, Purification, and Tumor Cell Uptake of 67Ga-Deferoxamine−Folate, a Potential Radiopharmaceutical for Tumor Imaging. https://app.cochat.ai/papers/10.1021/bc9500709
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Wang, S., Lee, R. J., Mathias, C. J., Green, M. A., & Low, P. S. (1996). Synthesis, Purification, and Tumor Cell Uptake of 67Ga-Deferoxamine−Folate, a Potential Radiopharmaceutical for Tumor Imaging. Bioconjugate Chemistry. https://doi.org/10.1021/bc9500709

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