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Identification of a novel BODIPY minihepcidin tool for the high content analysis of ferroportin (SLC40A1) pharmacology
Sarah. E. Skerratt,Sian Humphreys,Rita Ferreira,Csilla Jorgensen,Joe Warmus,Lei Zhao,Xiaohe Tong,Sarah A. Nickolls
MedChemComm Pub Date : 06/08/2016 00:00:00 , DOI:10.1039/C6MD00260A
Abstract

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.

Graphical abstract: Identification of a novel BODIPY minihepcidin tool for the high content analysis of ferroportin (SLC40A1) pharmacology
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