Folate as a Targeting Device for Proteins Utilizing Folate Receptor-Mediated Endocytosis
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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. Fig. 1. Folic acid.Keywords:
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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. Fig. 1. Folic acid.
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The back cover picture shows a novel synthesis route of fluorescent carbon dots by using folic acid as the carbon source, and the use of these carbon dots for the microscopic imaging of cancer cells. Importantly, cancer cells over-expressing the folate receptor upon their surface could be discriminated by their more intense fluorescence signals as compared to cells not expressing the receptor. More information can be found in the full paper by R. Jelinek et al. on page 614 in Issue 7, 2016 (DOI: 10.1002/cbic.201500694).
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In this paper, we report on a potential cancer drug delivery system that utilizes the ligand targeting of the folate receptor. Our drug delivery system consists of Pluronic-P105 micelles, targeted with folic acid moieties. A melanoma folate positive (FR+) (B16-F10), and a fibroblast folate negative (FR-) (NIH-3T3) cell lines are used to compare the cellular accumulation of a chemotherapeutic drug (Doxorubicin) when the delivery is mediated by folated Pluronic P105 micelles. In order to obtain a proper comparison, we corrected for the quenching of Doxorubicin by folic acid molecules and illustrated the significant effect of quenching on the analysis of similar systems. Results show an 80% increase in the accumulation of the antineoplastic agent in the FR+ cell line, when compared to the FR- cell line, thus providing evidence that the efficacy of Pluronic micelles, as drug delivery vehicles, can be enhanced via folic acid targeting.
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ABSTRACT Whilst plant cells are apparently equipped with all the necessary molecular machinery for receptor‐mediated endocytosis, the physiological role of this process in these cells remains an enigma. In this article, we consider current opinions of endocytosis in plants and define some of the problems that have impeded progress in our under‐standing of the part played by endocytosis in the vesicle trafficking pathway.
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Cellular uptake through endocytosis is crucial for drug delivery and nanomedicine. However, the conditions under which passive endocytosis (i.e., not ATP driven) takes place are not well understood. We report MD simulations of the passive uptake of ligand-coated nanoparticles with varying size, shape, coverage, and membrane-binding strength. We find that the efficiency of passive endocytosis is higher for spherocylindrical particles than for spheres and that endocytosis is suppressed for particles with sharp edges.
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