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Literature summary for 3.4.24.56 extracted from

  • Deprez-Poulain, R.; Hennuyer, N.; Bosc, D.; Liang, W.G.; Enee, E.; Marechal, X.; Charton, J.; Totobenazara, J.; Berte, G.; Jahklal, J.; Verdelet, T.; Dumont, J.; Dassonneville, S.; Woitrain, E.; Gauriot, M.; Paquet, C.; Duplan, I.; Hermant, P.; Cantrelle, F.X.; Sevin, E.; Culot, M.; Landry, V.; Herl, H.e.r.l.e.
    Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice (2015), Nat. Commun., 6, 8250 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(S)-4-fluoro-N-((1-(4-(hydroxyamino)-1-(naphthalen-2-yl)-4-oxobutan-2-yl)-1H-1,2,3-triazol-4-yl)methyl)benzamide i.e. BDM44768, catalytic site inhibitor, designed by kinetic target-guided synthesis. Selectively inhibits insulin-degrading enzyme. Crystallographic and small angle X-ray scattering analyses show that it locks insulin-degrading enzyme in a closed conformation. Acute treatment of mice with BDM44768 increases insulin signalling and impairs glucose tolerance in an insulin-degrading enzyme-dependent manner. The results casts doubt on the general usefulness of the inhibition of insulin-degrading enzyme catalytic activity to treat diabetes Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
insulin + H2O Mus musculus
-
?
-
?

Organism

Organism UniProt Comment Textmining
Mus musculus Q9JHR7
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-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
insulin + H2O
-
Mus musculus ?
-
?

Synonyms

Synonyms Comment Organism
IDE
-
Mus musculus
Insulin-degrading enzyme
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Mus musculus

General Information

General Information Comment Organism
metabolism knockout and genetic studies link insulin-degrading enzyme to Alzheimer's disease and type-2 diabetes Mus musculus
physiological function the enzyme is involved in pathways that modulate short-term glucose homeostasis Mus musculus