Journal
MEDCHEMCOMM
Volume 7, Issue 8, Pages 1564-1571Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6md00260a
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Iron is essential to life and is actively absorbed by enterocytes and secreted into plasma by the iron exporter ferroportin (SLC40A1). Dysregulation of iron homeostasis is a key component of many diseases such as hemochromatosis and beta-thalassemia. Ferroportin is the only known iron exporter protein, and as such is an important therapeutic target. To-date, modulators of ferroportin activity have shown promise in pre-clinical models, with recent screening assays enabling screening in a high throughput loss of signal format. Herein, we describe the design and synthesis of a novel BODIPY-labelled minihepcidin peptide to enable the high content analysis of ferroportin (SLC40A1) pharmacology, and the high throughput screening of compounds in a gain of signal assay format.
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