Pursuing Orally Bioavailable Hepcidin Analogues via Cyclic
N-methylation
cyclic peptides
ferroportin
hepcidin
oral bioavailability
Journal
Biomedicines
ISSN: 2227-9059
Titre abrégé: Biomedicines
Pays: Switzerland
ID NLM: 101691304
Informations de publication
Date de publication:
08 Feb 2021
08 Feb 2021
Historique:
received:
03
12
2020
revised:
20
01
2021
accepted:
02
02
2021
entrez:
11
2
2021
pubmed:
12
2
2021
medline:
12
2
2021
Statut:
epublish
Résumé
The peptide hormone hepcidin is one of the key regulators of iron absorption, plasma iron levels, and tissue iron distribution. Hepcidin functions by binding to and inducing the internalisation and subsequent lysosomal degradation of ferroportin, which reduces both iron absorption in the gut and export of iron from storage to ultimately decrease systemic iron levels. The key interaction motif in hepcidin has been localised to the highly conserved N-terminal region, comprising the first nine amino acid residues, and has led to the development of mini-hepcidin analogs that induce ferroportin internalisation and have improved drug-like properties. In this work, we have investigated the use of head-to-tail cyclisation and
Identifiants
pubmed: 33567510
pii: biomedicines9020164
doi: 10.3390/biomedicines9020164
pmc: PMC7915682
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : NIDDK NIH HHS
ID : R01 DK107309
Pays : United States
Organisme : National Health and Medical Research Council
ID : APP1006423
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