Matriptase-2: monitoring and inhibiting its proteolytic activity

Agata Gitlin-Domagalska , Martin Mangold , Dawid Dębowski , Natalia Ptaszyńska , Anna Łęgowska , Michael Gütschow , Krzysztof Rolka


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.
Author Agata Gitlin-Domagalska (FCh / DMB / LBCh)
Agata Gitlin-Domagalska,,
- Laboratory of Bioorganic Chemistry
, Martin Mangold
Martin Mangold,,
, Dawid Dębowski (FCh / DMB / LBCh)
Dawid Dębowski,,
- Laboratory of Bioorganic Chemistry
, Natalia Ptaszyńska (FCh / DMB / LBCh)
Natalia Ptaszyńska,,
- Laboratory of Bioorganic Chemistry
, Anna Łęgowska (FCh / DMB / LBCh)
Anna Łęgowska,,
- Laboratory of Bioorganic Chemistry
, Michael Gütschow
Michael Gütschow,,
, Krzysztof Rolka (FCh / DMB / LBCh)
Krzysztof Rolka,,
- Laboratory of Bioorganic Chemistry
Journal seriesFuture Medicinal Chemistry, ISSN 1756-8919, (A 40 pkt)
Issue year2018
Publication size in sheets0.3
Keywords in Englishanemia, fluorogenic substrates, hepcidin, iron overload, matriptase-2, peptide inhibitors, serine proteases
ASJC Classification3002 Drug Discovery; 3004 Pharmacology; 1313 Molecular Medicine
Languageen angielski
Score (nominal)40
ScoreMinisterial score = 40.0, ArticleFromJournal
Ministerial score (2013-2016) = 40.0, ArticleFromJournal
Publication indicators WoS Citations = 0; Scopus SNIP (Source Normalised Impact per Paper): 2016 = 0.763; WoS Impact Factor: 2017 = 3.969 (2) - 2017=3.973 (5)
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* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or Perish system.