SpringerProtocols: Abstract: Folate as a Targeting Device for Proteins Utilizing Folate Receptor-Mediated Endocytosis

Folate as a Targeting Device for Proteins Utilizing Folate Receptor-Mediated Endocytosis

By: Robert J. Lee², Philip S. Low³

Abstract

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Folic acid (M _r = 441, Fig. 1) is a vitamin essential for de novo nucleotide synthesis and one-carbon metabolism. The ability to acquire folate, therefore, is important to the viability of proliferating cells.

Affiliation(s): (2) Endocyte, Inc., West Lafayette, IN
(3) Department of Chemistry, Purdue University, West Lafayette, IN

Book Title: Drug Targeting: Strategies, Principles, and Applications

Series: Methods in Molecular Medicine | Volume: 25 | Pub. Date: Apr-21-2000 | Page Range: 69-75 | DOI: 10.1385/1-59259-075-6:69

Subject: Pharmacology/Toxicology

References

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8.	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. USA 88, 5572–5576.

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10.	Wang, S., Lee, R. J., Mathias, C. J., Green, M. A., and Low, P. S. (1996) Synthesis, purification, and tumor cell uptake of Gallium-67-deferoxamine-folate, a potential radiopharmaceutical for tumor imaging. Bioconj. Chem. 7, 56–62.

11.	Leamon, C. P. and Low, P. S. (1992) Cytotoxicity of momordin-folate conjugates in cultured human cells. J. Biol. Chem. 267, 24,966–24,971.

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14.	Lee, R. J. and Low, P. S. (1994) Folate-mediated tumor cell targeting of lipo-some-entrapped doxorubicin in vitro. Biochim. Biophys. Acta 1233, 134–144.

15.	Wang, S., Luo, J., Lantrip, D. A., Waters, D. J., Mathias, C. J., Green, M. A., Fuchs, P. L., and Low, P. S. (1997) Design and Synthesis of ¹1¹In-DTPA-Folate for Use as a Tumor-Targeted Radiopharmaceutical. Bioconj. Chem., submitted.

16.	Mathias, C. J., Waters, D. J., Wang, S., Low, P. S., and Green, M. A. (1997) Indium-111 labeled Indium(III)-DTPA-folate as a radiopharmaceutical for targeting tumor-associated folate receptors: the effect of tumor size on targeting selectivity and radiochemical analysis of excreted tracer, in 12th International Symposium on Radiopharmaceutical Chemistry, Uppsala, Sweden.

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20.	Lee, R. J. and Huang, L. (1996) Folate-targeted, anionic liposome-entrapped polylysine-condensed DNA for tumor cell-specific gene transfer. J. Biol. Chem. 271, 8481–8487.

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