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Literature summary for 1.4.3.4 extracted from

  • McDonald, G.R.; Olivieri, A.; Ramsay, R.R.;, Holt, A.
    On the formation and nature of the imidazoline I2 binding site on human monoamine oxidase-B (2010), Pharmacol. Res., 62, 475-488.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(2-benzofuranyl)-2-imidazoline at micromolar concentrations, to a site distinct from the active site on at least two forms of the pure enzyme, probably corresponding to oxidised and reduced enzyme states Homo sapiens
2-Phenylethylamine time-dependent, slowly reversible suicide inhibition. Addition of 2-phenylethylamine (10mM) to the enzyme results in immediate bleaching of the absorbance peak at 460 nm, a consequence of rapid reduction of the flavin cofactor by 2-phenylethylamine at steady state Homo sapiens
Phenelzine concentration-dependent inhibition Homo sapiens
tranylcypromine inactivation of recombinant human MAO-B with tranylcypromine results in the formation of a high affinity I2 site on the enzyme, measured as an increase in binding of 2-(2-benzofuranyl)-2-imidazoline. Inhibition by tranylcypromine results in displacement of Q206 and closure of the I199 gate Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0109
-
benzylamine pH 7.4, 30°C, oxidative half-reaction Homo sapiens
0.0449
-
2-Phenylethylamine pH 7.4, 30°C, oxidative half-reaction Homo sapiens
0.0485
-
benzylamine pH 7.4, 30°C, reductive half-reaction Homo sapiens
0.423
-
2-Phenylethylamine pH 7.4, 30°C, reductive half-reaction Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27338
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-phenylethylamine + H2O + O2
-
Homo sapiens 2-phenylethanal + NH3 + H2O2
-
?
benzylamine + H2O + O2
-
Homo sapiens benzaldehyde + NH3 + H2O2
-
?

Synonyms

Synonyms Comment Organism
MAO-B
-
Homo sapiens
monoamine oxidase-B
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

pH Optimum

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00789
-
2-(2-benzofuranyl)-2-imidazoline pH 7.4, 30°C, reductive half-reaction Homo sapiens
0.326
-
2-(2-benzofuranyl)-2-imidazoline pH 7.4, 30°C, oxidative half-reaction Homo sapiens