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Literature summary for 3.4.24.56 extracted from

  • Cabrol, C.; Huzarska, M.A.; Dinolfo, C.; Rodriguez, M.C.; Reinstatler, L.; Ni, J.; Yeh, L.A.; Cuny, G.D.; Stein, R.L.; Selkoe, D.J.; Leissring, M.A.
    Small-molecule activators of insulin-degrading enzyme discovered through high-throughput compound screening (2009), PLoS ONE, 4, e5274.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
5-(4-chlorophenyl)-2-[(E)-{[(5-chloro-1,2,3-thiadiazol-4-yl)methoxy]imino}methyl]cyclohexane-1,3-dione direct stimulation of IDE, acts highly synergistically with ATP, Ia1 activates the degradation of amyloid beta by about 700% in presence other shorter substrates Homo sapiens
ATP direct stimulation of IDE, acts highly synergistically with Ia1 and Ia2. The putative ATP-binding domain is a key modulator of IDE proteolytic activity Homo sapiens
additional information synthesis and analysis of synthetic small-molecule activators, structure-activity relationships, overview Homo sapiens
N-(3-chlorophenyl)-4-[5-(furan-2-yl)-1H-pyrazol-3-yl]piperidine-1-carboxamide direct stimulation of IDE, acts highly synergistically with ATP, Ia2 activates the degradation of amyloid beta by about 400% in presence of other shorter substrates Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information amyloid beta degradation kinetics in presence or absence of activators Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
amyloid beta + H2O Homo sapiens
-
amyloid beta peptide fragments
-
?
insulin + H2O Homo sapiens
-
insulin peptide fragments
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid beta + H2O
-
Homo sapiens amyloid beta peptide fragments
-
?
insulin + H2O
-
Homo sapiens insulin peptide fragments
-
?
additional information the putative ATP-binding domain is a key modulator of IDE proteolytic activity Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
IDE
-
Homo sapiens
Insulin-degrading enzyme
-
Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

General Information

General Information Comment Organism
malfunction hypocatabolism of the amyloid beta-protein by insulin-degrading enzyme is implicated in the pathogenesis of Alzheimer's disease Homo sapiens