Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.4.24.B1 (
angiotensin-converting enzyme 2
)
1,025
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The apelinergic system is a mammalian peptide hormone network with key physiological roles. Apelin isoforms and analogues are believed to be promising therapeutics for cardiovascular disease. Despite extensive studies on apelin-13 degradation patterns, only one protease,
angiotensin-converting enzyme 2
(
ACE2
), had been implicated in its physiological regulation. Through use of a peptide-based fluorescent probe, we identified the metalloprotease neprilysin (
NEP
, a target for Entresto used in treatment of heart failure) as an enzyme that cleaves apelin isoforms. In vitro
NEP
proteolysis generated fragments that lacked the ability to bind to the apelin receptor, thereby making
NEP
the first protease to fully inactivate apelin. The involvement of
NEP
in the apelinergic system contributes to the understanding of its role in cardiovascular physiology.
...
PMID:The Metalloprotease Neprilysin Degrades and Inactivates Apelin Peptides. 2737 80
