Evaluation of Riboflavin Transporters as Targets for Drug Delivery and Theranostics

Frontiers in Pharmacology
Lisa BartmannZhuojun Wu

Abstract

The retention and cellular internalization of drug delivery systems and theranostics for cancer therapy can be improved by targeting molecules. Since an increased uptake of riboflavin was reported for various cancers, riboflavin and its derivatives may be promising binding moieties to trigger internalization via the riboflavin transporters (RFVT) 1, 2, and 3. Riboflavin is a vitamin with pivotal role in energy metabolism and indispensable for cellular growth. In previous preclinical studies on mice, we showed the target-specific accumulation of riboflavin-functionalized nanocarriers in cancer cells. Although the uptake mechanism of riboflavin has been studied for over a decade, little is known about the riboflavin transporters and their expression on cancer cells, tumor stroma, and healthy tissues. Furthermore, evidence is lacking concerning the representativeness of the preclinical findings to the situation in humans. In this study, we investigated the expression pattern of riboflavin transporters in human squamous cell carcinoma (SCC), melanoma and luminal A breast cancer samples, as well as in healthy skin, breast, aorta, and kidney tissues. Low constitutive expression levels of RFVT1-3 were found on all healthy tissues, whi...Continue Reading

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Citations

Feb 6, 2020·Cancers·Milita DarguzyteFabian Kiessling
Jul 16, 2020·Naunyn-Schmiedeberg's Archives of Pharmacology·Ibrahim M AlhazzaSaleh H Alwasel
Jan 14, 2020·Molecular Metabolism·Javier Garcia-BermudezKıvanç Birsoy
Nov 23, 2021·Frontiers in Nutrition·Keri BarronNatalia Krupenko

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Methods Mentioned

BETA
pharmacotherapies
xenografts
biopsies
FCS
confocal microscopy
PCR

Software Mentioned

Graph Prism
ImageJ
ImageJ JACoP ( Co - localization Plugin
GraphPad
JACoP
IMARIS

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