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Literature summary for 3.4.24.56 extracted from

  • Durham, T.B.; Toth, J.L.; Klimkowski, V.J.; Cao, J.X.; Siesky, A.M.; Alexander-Chacko, J.; Wu, G.Y.; Dixon, J.T.; McGee, J.E.; Wang, Y.; Guo, S.Y.; Cavitt, R.N.; Schindler, J.; Thibodeaux, S.J.; Calvert, N.A.; Coghlan, M.J.; Sindelar, D.K.; Christe, M.; Kiselyov, V.V.; Michael, M.D.; Sloop, K.W.
    Dual exosite-binding inhibitors of insulin-degrading enzyme challenge its role as the primary mediator of insulin clearance in vivo (2015), J. Biol. Chem., 290, 20044-20059 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens
expression in Escherichia coli Mus musculus

Crystallization (Commentary)

Crystallization (Comment) Organism
-
Homo sapiens
-
Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
methyl [(2S)-2-(5-[5-[4-([(2S)-2-[(3S)-3-amino-2-oxopiperidin-1-yl]-2-cyclohexylacetyl]amino)phenyl]pentyl]-2-fluorophenyl)-3-(quinolin-3-yl)propyl]carbamate
-
Homo sapiens
methyl [(2S)-2-[4-([5-[4-([(2S)-2-[(3S)-3-amino-2-oxopiperidin-1-yl]-2-cyclohexylacetyl]amino)phenyl]pentyl]oxy)phenyl]-3-(quinolin-3-yl)butyl]carbamate
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
insulin + H2O Homo sapiens in HEK cells the enzyme has little impact on insulin clearance ?
-
?
insulin + H2O Mus musculus the enzyme is implicated in proteolysis of insulin ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P14735
-
-
Mus musculus Q9JHR7
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens
-
Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Glucagon + H2O
-
Homo sapiens ?
-
?
insulin + H2O
-
Homo sapiens ?
-
?
insulin + H2O
-
Mus musculus ?
-
?
insulin + H2O in HEK cells the enzyme has little impact on insulin clearance Homo sapiens ?
-
?
insulin + H2O the enzyme is implicated in proteolysis of insulin Mus musculus ?
-
?

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000015
-
37°C, pH 7.5 Homo sapiens methyl [(2S)-2-[4-([5-[4-([(2S)-2-[(3S)-3-amino-2-oxopiperidin-1-yl]-2-cyclohexylacetyl]amino)phenyl]pentyl]oxy)phenyl]-3-(quinolin-3-yl)butyl]carbamate
0.000018
-
37°C, pH 7.5 Homo sapiens methyl [(2S)-2-(5-[5-[4-([(2S)-2-[(3S)-3-amino-2-oxopiperidin-1-yl]-2-cyclohexylacetyl]amino)phenyl]pentyl]-2-fluorophenyl)-3-(quinolin-3-yl)propyl]carbamate

General Information

General Information Comment Organism
physiological function the enzyme has a minimal role in insulin metabolism in vivo. It may be more important in helping regulate amylin clearance Homo sapiens
physiological function the enzyme is implicated in proteolysis of insulin Mus musculus