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Journal ArticleDOI

Design and Synthesis of [111In]DTPA−Folate for Use as a Tumor-Targeted Radiopharmaceutical

TLDR
In cultured tumor cells, uptake of [111In]DTPA-folate (gamma) was found to be specific for folate receptor-bearing cells, and the kinetics of uptake were similar to those of free folate and other folate-conjugated molecules.
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This article is published in Bioconjugate Chemistry.The article was published on 1997-09-25. It has received 242 citations till now.

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Citations
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Journal ArticleDOI

Targeted drug delivery via the folate receptor.

TL;DR: Low molecular weight radiopharmaceuticals based on folate conjugates showed much more favorable pharmacokinetic properties than radiolabeled antibodies and greater tumor selectivity in folate receptor-positive animal tumor models.
Journal ArticleDOI

Discovery and Development of Folic-Acid-Based Receptor Targeting for Imaging and Therapy of Cancer and Inflammatory Diseases

TL;DR: The quest for the ideal targeted therapeutic agent was described, which began with a search for ligands that would bind selectively to pathologic cells, displaying no affinity for healthy cells, and held great promise for increasing the potency while reducing toxicity of many cancer therapies.
Journal ArticleDOI

Folate receptor‐mediated drug targeting: From therapeutics to diagnostics

TL;DR: This review will summarize the applications of folic acid as a targeting ligand and highlight the various methods being developed for delivery of therapeutic and imaging agents to FR-expressing cells.
Journal ArticleDOI

Folate-targeted therapeutic and imaging agents for cancer.

TL;DR: Folate conjugates bind to folate receptors that are overexpressed on approximately 40% of human cancers and mediate internalization of their attached drugs by receptor-mediated endocytosis, and six folate-targeted drugs are currently in human clinical trials.
References
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Journal ArticleDOI

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

TL;DR: The results suggest that 67Ga-DF--folate(gamma) complex might be useful as a diagnostic agent for noninvasive imaging of folate receptor-positing tumors.
Journal ArticleDOI

Studies of the role of a particulate folate-binding protein in the uptake of 5-methyltetrahydrofolate by cultured human KB cells.

TL;DR: The hypothesis that the membrane-associated folate-binding protein of human cells participates in the transport of folates under physiologic conditions is supported.
Journal ArticleDOI

Membrane folate-binding proteins are responsible for folate-protein conjugate endocytosis into cultured cells

TL;DR: It is concluded that a classical FBP is responsible for the uptake of folate-protein conjugates by receptor-bearing cells through FBP-mediated folate uptake.
Journal ArticleDOI

The folate-binding protein of rat kidney. Purification, properties, and cellular distribution.

TL;DR: Intense fluorescence staining for FBP was localized at the apices (brush border) of proximal tubules, and the choroid plexus, an organ previously shown to contain FBP, also exhibited intense fluorescent staining.
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