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Literature summary for 3.4.24.56 extracted from

  • Malito, E.; Ralat, L.A.; Manolopoulou, M.; Tsay, J.L.; Wadlington, N.L.; Tang, W.J.
    Molecular bases for the recognition of short peptide substrates and cysteine-directed modifications of human insulin-degrading enzyme (2008), Biochemistry, 47, 12822-12834.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with bradykinin, to 1.9 A resolution. Bradykinin binds to the exosite. Residue C819 is located inside the catalytic chamber pointing toward an extended hydrophobic pocket. Specific activity similar to wild-type using substrate 7-methoxycoumarin-4-ylacetyl-NPPGFSAFK-2,4-dinitrophenyl Homo sapiens

Protein Variants

Protein Variants Comment Organism
C819A thiol-directed modification of C819 likely causes local structure perturbation to reduce substrate binding and catalysis Homo sapiens
E111Q catalysitcally inactive. Mutant forms ordered crystals of considerable size at a more rapid rate than the wild type Homo sapiens
additional information construction of mutants lacking one or severall cysteine resiudes. A mutant devoid of all 13 cysteine residues is insensitive to the inhibition by S-nitrosoglutathione, hydrogen peroxide, or N-ethylmaleimide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
hydrogen peroxide
-
Homo sapiens
N-ethylmaleimide
-
Homo sapiens
S-nitrosoglutathione potent inhibition at physiologically relevant concentrations Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
4.2
-
bradykinin pH 7.3, 37°C Homo sapiens
7.3
-
kallidin pH 7.3, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-methoxycoumarin-4-ylacetyl-NPPGFSAFK-2,4-dinitrophenyl + H2O
-
Homo sapiens ?
-
?
bradykinin + H2O cleavage at Pro/Phe site Homo sapiens ?
-
?
kallidin + H2O cleavage at Pro/Phe site Homo sapiens ?
-
?