Synthesis of [99mTc]DTPA-folate and its evaluation as a folate-receptor-targeted radiopharmaceutical

Bioconjugate Chemistry

Volumn 11, Issue 2, 2000, Pages 253-257

  Mathias, Carla J ^a   Hubers, David ^a   Low, Philip S ^b   Green, Mark A ^a  

^a PURDUE UNIVERSITY   (United States)

^b PURDUE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORINE COMPOUNDS; QUALITY CONTROL; SODIUM COMPOUNDS; SOLUTIONS; THIN LAYER CHROMATOGRAPHY;

% REDUCTIONS; 99M-TC-DTPA; CONDITION; FOLATE RECEPTOR; FOLATES; IN-VIVO; ITS EVALUATION; PERTECHNETATE; RADIOCHEMICAL PURITY; TUMOR UPTAKE;

TUMORS;

MUS MUSCULUS;

CARRIER PROTEIN; CELL SURFACE RECEPTOR; DRUG CARRIER; FOLATE BINDING PROTEIN; FOLATE-BINDING PROTEIN; FOLIC ACID; PENTETATE TECHNETIUM TC 99M; RADIOPHARMACEUTICAL AGENT;

ANIMAL; ARTICLE; BINDING COMPETITION; CANCER TRANSPLANTATION; CELL CULTURE; CHEMISTRY; EVALUATION; HUMAN; MALE; METABOLISM; MOUSE; NUDE MOUSE; SYNTHESIS; TISSUE DISTRIBUTION; XENOGRAFT;

ANIMALS; BINDING, COMPETITIVE; CARRIER PROTEINS; DRUG CARRIERS; EVALUATION STUDIES; FOLIC ACID; HUMANS; MALE; MICE; MICE, NUDE; NEOPLASM TRANSPLANTATION; RADIOPHARMACEUTICALS; RECEPTORS, CELL SURFACE; TECHNETIUM TC 99M PENTETATE; TISSUE DISTRIBUTION; TRANSPLANTATION, HETEROLOGOUS; TUMOR CELLS, CULTURED;

EID: 0033625094     PISSN: 10431802     EISSN: None     Source Type: Journal    
DOI: 10.1021/bc9901447     Document Type: Article

References (25)

1. Anderson, R. G. W., Kamen, B. A., and Rothberg, K. G. et al. (1992) Potocytosis: Sequestration and transport of small molecules by caveolae. Science 255, 410-411.
2. Leamon, C. P., and Low, P. S. (1992) Cytotoxicity of momordin-folate conjugates in cultured human cells. J. Biol. Chem. 267, 24966-24971.
3. Leamon, C. P., and Low, P. S. (1991) Delivery of macromolecules into living cells: a method that exploits folate receptor endocytosis. Proc. Natl. Acad. Sci. U.S.A. 88, 5572-5576.
4. Leamon, C. P., and Low, P. S. (1993) Membrane folate binding proteins are responsible for the folate-protein conjugate endocytosis into cultured cells. Biochem. J. 291, 855-860.
5. 67Ga-Deferoxamine-Folate, a Potential Radiopharmaceutical for Tumor Imaging. Bioconjugate Chem. 7, 56-62.
6. Mathias, C. J., Lee, R. J., Wang, S., Waters, D. J., Low, P. S., M. A. Green. (1996) Tumor-selective radiopharmaceutical targeting via receptor-mediated endocytosis: Evaluation of a gallium-67 labeled deferoxamine-folate conjugate. J. Nucl. Med. 37, 1003-1008.
7. 67Ga-Deferoxamine-Folate to Folate-Receptor-Positive Human KB Tumor Xenografts. Nucl. Med. Biol. 26, 23-25.
8. 111In-DTPA-Folate for Use as a Tumor-Targeted Radiopharmaceutical. Bioconjugate Chem. 8, 673-679.
9. 111In-DTPA-Folate as a Potential Folate-Receptor-Targeted Radiopharmaceutical, J. Nucl. Med. 39, 1579-1585.
10. Weitman, S. D., Lark, R. H., and Coney, L. R., et al. (1992) Distribution of the folate receptor GP38 in normal and malignant cell lines and tissues. Cancer Res. 52, 3396-3401.
11. Li, P. Y., DelVecchio, S., Fonti, R., Carriero, M. V., Potena, M. I., and Botti, G., et al. (1996) Local concentration of folate binding protein GP38 in sections of human ovarian carcinoma by in vitro quantitative autoradiography. J. Nucl. Med. 37, 665-672.
12. Miotti, S., Canevari, S., and Menard, S., et al. (1987) Characterization of human ovarian carcinoma-associated antigens defined by novel monoclonal antibodies with tumor-restricted specificity. Int. J. Cancer 39, 297-303.
13. Rothenberg, S. P., and daCosta, M. (1971) Further observations on the folate-binding factor in some leukemic cells. J. Clin. Invest. 50, 719-726.
14. Campbell, I. G., Jones, T. A., and Foulkes, W. D., et al. (1991) Folate-binding protein is a marker for ovarian cancer. Cancer Res. 51, 5329-5338.
15. Garin-Chesa, P., Campbell, I., and Saigo, P. E., et al. (1993) Trophoblast and ovarian cancer antigen LK26: Sensitivity and specificity in immunopathology and molecular identification as a folate-binding protein. Am. J. Pathol. 142, 557-567.
16. Toffoli, G., Cernigoi, C., Russo, A., Gallo, A., Bagnoli, M., and Boiocchi, M. (1997) Overexpression of folate binding protein in ovarian cancers. Int. J. Cancer (Pred. Oncol.) 74, 193-198.
17. Wu, M., Gunning, W., and Ratnam, M. (1999) Expression of folate receptor type a in relation to cell type, malignancy, and differentiation in ovary, uterus, and cervix. Cancer Epidemiol. Biomarkers Prev. 8, 775-782.
18. A portion of this work was presented in abstract form: Mathias, C. J., Hubers, D., Trump, D. P., Wang, S., Luo, J., Waters, D. J., Fuchs, P. L., Low, P. S., and Green, M. A. (1997) Synthesis of Tc-99m-DTPA-Folate and Preliminary Evaluation as a Folate-Receptor-Targeted Radiopharmaceutical. J. Nucl. Med. 38, 87P.
19. Swinscow, T. D. V. (1980) Statistics at Square One, 6th ed.; British Medicial Association, London.
20. Selhub, J., and Franklin, W. A. (1984) The folate binding protein of rat kidney. J. Biol. Chem. 259, 6601-6606.
21. Selhub, J., Emmanouel, D., Stavropoulos, T., and Arnold, R. (1987) Renal folate adsorption and the kidney folate binding protein. I. Urinary Clearance studies. Am. J. Physiol. 252, F750-F756.
22. Selhub, J., Nakamura, S., and Carone, F. A. (1987) Renal folate adsorption and the kidney folate binding protein. II. Microinfusion studies. Am. J. Physiol. 252, F757-F760.
23. Williams, W. M., and Huang, K. C. (1982) Renal tubular transport of folic acid and methotrexate in the monkey. Am. J. Physiol. 272, F757-F760.
24. Birn, J., Nielsen, S., and Christensen, E. I. (1997) Internalization and apical-to-basolateral transport of folate in rat kidney proximal tubule. Am. J. Physiol. 272, F70-F78.
25. Green, M. A., Mathias, C. J., Low, P. S., Ellis, P. R., Stabin, M. G., Wendt, R. E., III, McCullough, S. P., Broussard, W. F., Gershenson, D. M., and Podoloff, D. A. (1998) Initial experience with In-111-DTPA-Folate (FolateScan) in humans: Assessment of tracer excretion kinetics and radiation dosimetry. J. Nucl. Med. 39, 191P.