Matriptase-2: monitoring and inhibiting its proteolytic activity

Matriptase-2 (MT2) is a membrane-anchored proteolytic enzyme. It acts as the proteolytic key regulator in human iron homeostasis. A high expression level can lead to iron overload diseases, whereas mutations in the gene encoding MT2, , may result in various forms of iron deficiency anemia. Recently,...

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Bibliographic Details
Published in:Future medicinal chemistry 2018-12, Vol.10 (23), p.2745-2761
Main Authors: Gitlin-Domagalska, Agata, Mangold, Martin, D bowski, Dawid, Ptaszy ska, Natalia, gowska, Anna, Gütschow, Michael, Rolka, Krzysztof
Format: Article
Language:English
Subjects:
anemia
fluorogenic substrates
hepcidin
iron overload
matriptase-2
peptide inhibitors
serine proteases
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Summary:Matriptase-2 (MT2) is a membrane-anchored proteolytic enzyme. It acts as the proteolytic key regulator in human iron homeostasis. A high expression level can lead to iron overload diseases, whereas mutations in the gene encoding MT2, , may result in various forms of iron deficiency anemia. Recently, MT2 has been reported as a positive prognostic factor in breast and prostate cancers. However, the exact functions of MT2 in various pathophysiological conditions are still not fully understood. In this review, we describe the synthetic tools designed and synthesized to regulate or monitor MT2 proteolytic activity and present the latest knowledge about the role of MT2 in iron homeostasis and cancer.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2018-0346