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Literature summary for 3.4.24.B14 extracted from

  • Ul-Haq, Z.; Usmani, S.; Iqbal, S.; Zia, S.R.
    In silico based investigation of dynamic variations in neprilysin (NEP and NEP2) proteins for extracting the point of specificity (2016), Mol. Biosyst., 12, 1024-1036 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
fasidotrilat fasidotrilat interacts with the Arg661 of hNEP-2 with more consistent bidentate hydrogen bonding and with weaker His658 with monodentate hydrogen bonding. The extended conformation of the inhibitor in the hNEP2 pocket might be the reason for its weak interactions Homo sapiens
additional information molecular docking studies, overview. For substrate and inhibitor binding, Arg661 and Zn694 are identified as the most conserved residues Homo sapiens
N-[(2S)-3-phenyl-2-(sulfanylmethyl)propanoyl]-L-tryptophan
-
Homo sapiens
omapatrilat
-
Homo sapiens
phosphoramidon weak interactions with hNEP-2 Homo sapiens
thiorphan Arg66a acts to support the ligand binding in NEP-2 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q495T6
-
-

Source Tissue

Source Tissue Comment Organism Textmining
central nervous system
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
NEP2
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000008
-
omapatrilat pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
evolution sequence comparisons of NEP (EC 3.4.24.11) and NEP-2 Homo sapiens
metabolism neprilysin-2 (NEP2) in the central nervous system controls Alzheimer's protein (amyloid-beta) deposition, and prevents its occurrence, while in the peripheral system, its closest homologue, neutral endopeptidase neprilysin (NEP, EC 3.4.24.11), regulates hypertension and heart related diseases Homo sapiens
additional information molecular dynamics (MD) simulations of NEP-2 and modelling, overview. For substrate and inhibitor binding, Arg661 and Zn694 are identified as the most conserved residues Homo sapiens
physiological function neprilysin-2 (NEP2) in the central nervous system controls Alzheimer's protein (amyloid-beta) deposition, and prevents its occurrence Homo sapiens