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Literature summary for 1.4.3.4 extracted from

  • Upadhyay, A.K.; Edmondson, D.E.
    Development of spin-labeled pargyline analogues as specific inhibitors of human monoamine oxidases A and B (2009), Biochemistry, 48, 3928-3935.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression of MAO-A in Pichia pastoris mitochondria Homo sapiens
expression of MAO-B in Pichia pastoris mitochondria, recombinant MAO-B is situated on the cytosolic face of the outer membrane in Pichia mitochondria Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
methyl (2E,4E)-5-(1,3-benzodioxol-5-yl)penta-2,4-dienoate
-
Homo sapiens
N-(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)-2-(4-[[methyl(prop-2-yn-1-yl)amino]methyl]phenyl)acetamide i.e. ParSL-1, a TEMPO-conjugated pargyline analogue; i.e. ParSL-1, a TEMPO-conjugated pargyline analogue Homo sapiens
N-(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)-3-[[methyl(prop-2-yn-1-yl)amino]methyl]benzamide i.e. ParSL-3, a TEMPO-conjugated pargyline analogue, specifically inhibits MAO-A Homo sapiens
N-(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)-4-[[methyl(prop-2-yn-1-yl)amino]methyl]benzamide i.e. ParSL-2, a TEMPO-conjugated pargyline analogue, specifically inhibits MAO-B Homo sapiens
Pargyline construction of three TEMPO-conjugated pargyline analogues ParSL-1, ParSL-2, and ParSL-3, which differ in flexibility and substituent positions of the linkers connecting the TEMPO group to the pargyline phenyl ring. The variations in conformational flexibility and substituent position have profound effects in tuning the specificities of these analogues toward the MAO isoforms, inhibitor synthesis, overview; construction of three TEMPO-conjugated pargyline analogues ParSL-1, ParSL-2, and ParSL-3, which differ in flexibility and substituent positions of the linkers connecting the TEMPO group to the pargyline phenyl ring. The variations in conformational flexibility and substituent position have profound effects in tuning the specificities of these analogues toward the MAO isoforms, inhibitor synthesis, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrial outer membrane
-
Homo sapiens 5741
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P21397
-
-
Homo sapiens P27338
-
-

Synonyms

Synonyms Comment Organism
MAOA
-
Homo sapiens
MAOB
-
Homo sapiens
monoamine oxidase A
-
Homo sapiens
monoamine oxidase B
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics, overview Homo sapiens
0.0013
-
methyl (2E,4E)-5-(1,3-benzodioxol-5-yl)penta-2,4-dienoate inhibition of MAO-B Homo sapiens
0.015
-
N-(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)-4-[[methyl(prop-2-yn-1-yl)amino]methyl]benzamide inhibition of MAO-B Homo sapiens
0.0235
-
methyl (2E,4E)-5-(1,3-benzodioxol-5-yl)penta-2,4-dienoate inhibition of MAO-A Homo sapiens
0.268
-
N-(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)-3-[[methyl(prop-2-yn-1-yl)amino]methyl]benzamide inhibition of MAO-A Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0016
-
inhibition of MAO-B Homo sapiens methyl (2E,4E)-5-(1,3-benzodioxol-5-yl)penta-2,4-dienoate
0.0271
-
inhibition of MAO-A Homo sapiens methyl (2E,4E)-5-(1,3-benzodioxol-5-yl)penta-2,4-dienoate