Matriptase-2: monitoring and inhibiting its proteolytic activity

Author:

Gitlin-Domagalska Agata1,Mangold Martin2,Dębowski Dawid1,Ptaszyńska Natalia1,Łęgowska Anna1,Gütschow Michael2,Rolka Krzysztof1

Affiliation:

1. Department of Molecular Biochemistry, Faculty of Chemistry, University of Gdansk, ul. Wita Stwosza 63, 80-308 Gdansk, Poland

2. Pharmaceutical Institute, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany

Abstract

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, TMPRSS6, 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.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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