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Pharmaceuticals 2018, 11(4), 115;

The Functional Versatility of Transferrin Receptor 2 and Its Therapeutic Value

Department of Clinical and Biological Sciences, University of Torino, 10043 Orbassano, Torino, Italy
Author to whom correspondence should be addressed.
Received: 28 September 2018 / Revised: 19 October 2018 / Accepted: 21 October 2018 / Published: 23 October 2018
(This article belongs to the Special Issue Iron as Therapeutic Targets in Human Diseases)
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Iron homeostasis is a tightly regulated process in all living organisms because this metal is essential for cellular metabolism, but could be extremely toxic when present in excess. In mammals, there is a complex pathway devoted to iron regulation, whose key protein is hepcidin (Hepc), which is a powerful iron absorption inhibitor mainly produced by the liver. Transferrin receptor 2 (Tfr2) is one of the hepcidin regulators, and mutations in TFR2 gene are responsible for type 3 hereditary hemochromatosis (HFE3), a genetically heterogeneous disease characterized by systemic iron overload. It has been recently pointed out that Hepc production and iron regulation could be exerted also in tissues other than liver, and that Tfr2 has an extrahepatic role in iron metabolism as well. This review summarizes all the most recent data on Tfr2 extrahepatic role, taking into account the putative distinct roles of the two main Tfr2 isoforms, Tfr2α and Tfr2β. Representing Hepc modulation an effective approach to correct iron balance impairment in common human diseases, and with Tfr2 being one of its regulators, it would be worthwhile to envisage Tfr2 as a therapeutic target. View Full-Text
Keywords: Tfr2; iron metabolism; hepcidin; erythropoiesis; SNC Tfr2; iron metabolism; hepcidin; erythropoiesis; SNC

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Roetto, A.; Mezzanotte, M.; Pellegrino, R.M. The Functional Versatility of Transferrin Receptor 2 and Its Therapeutic Value. Pharmaceuticals 2018, 11, 115.

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