Molecular mechanisms of the defective hepcidin inhibition in TMPRSS6 mutations associated with iron-refractory iron deficiency anemia

Blood. 2009 May 28;113(22):5605-8. doi: 10.1182/blood-2008-12-195594. Epub 2009 Apr 8.

Abstract

Matriptase-2 is a transmembrane serine protease that negatively regulates hepcidin expression by cleaving membrane-bound hemojuvelin. Matriptase-2 has a complex ectodomain, including a C-terminal serine protease domain and its activation requires an autocatalytic cleavage. Matriptase-2 mutations have been reported in several patients with iron-refractory iron deficiency anemia. Here we describe a patient with 2 missense mutations in the second class A low-density lipoprotein receptor (LDLRA) domain. Functional studies of these 2 mutations and of a previously reported mutation in the second C1r/C1s, urchin embryonic growth factor and bone morphogenetic protein 1 (CUB) domain were performed. Transfection of mutant cDNAs showed that membrane targeting of the 2 LDLRA mutants was impaired, with Golgi retention of the variants. The activating cleavage was absent for the LDLRA mutants and reduced for the CUB mutant. All 3 mutated proteins were still able to physically interact with hemojuvelin but only partially repressed hepcidin expression compared with wild-type matriptase-2. Our results underline the importance of LDLRA and CUB domains of matriptase-2.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anemia, Iron-Deficiency / drug therapy
  • Anemia, Iron-Deficiency / genetics*
  • Antimicrobial Cationic Peptides / antagonists & inhibitors*
  • Child
  • HeLa Cells
  • Hepcidins
  • Humans
  • Iron / therapeutic use
  • Male
  • Membrane Proteins / genetics*
  • Models, Biological
  • Mutation / physiology
  • Serine Endopeptidases / genetics*
  • Signal Transduction / genetics
  • Treatment Failure

Substances

  • Antimicrobial Cationic Peptides
  • HAMP protein, human
  • Hepcidins
  • Membrane Proteins
  • Iron
  • Serine Endopeptidases
  • TMPRSS6 protein, human