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Literature summary for 1.4.3.21 extracted from

  • Nurminen, E.M.; Pihlavisto, M.; Lazar, L.; Szakonyi, Z.; Pentikaeinen, U.; Fueloep, F.; Pentikaeinen, O.T.
    Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1 (2010), J. Med. Chem., 53, 6301-6315.
    View publication on PubMed

Application

Application Comment Organism
medicine VAP-1 might be a target for anti-inflammatory drug therapy because of its role in leukocyte adhesion to endothelium Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in CHO cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1R,2S)-2-(1-methylhydrazino)-1-phenylbutan-1-ol
-
Homo sapiens
(1R,2S)-2-(1-methylhydrazino)-1-phenylpentan-1-ol
-
Homo sapiens
(1R,2S)-2-(1-methylhydrazino)-1-phenylpropan-1-ol
-
Homo sapiens
1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-(1-methylhydrazino)-ethanol
-
Homo sapiens
1-(2-(3-chlorophenyl)-2-methoxyethyl)-1-methylhydrazine
-
Homo sapiens
1-(2-chlorophenyl)-2-(1-methylhydrazino)ethanol
-
Homo sapiens
1-(2-phenylpropyl)hydrazine
-
Homo sapiens
1-(3-methoxyphenyl)-2-(1-methylhydrazino)ethanol
-
Homo sapiens
1-(4-chlorophenyl)-2-(1-methylhydrazino)ethanol
-
Homo sapiens
1-(4-fluorophenyl)-2-(1-methylhydrazino)ethanol
-
Homo sapiens
1-(4-methoxyphenyl)-2-(1-methylhydrazino)ethanol
-
Homo sapiens
1-benzyl-1-methylhydrazine
-
Homo sapiens
1-ethyl-1-(2-phenylethyl)hydrazine
-
Homo sapiens
1-ethyl-1-[2-(3,4,5-trimethoxyphenyl)ethyl]hydrazine
-
Homo sapiens
1-ethyl-1-[2-(4-methoxyphenyl)ethyl]hydrazine
-
Homo sapiens
1-isobutyl-1-(2-phenylethyl)hydrazine
-
Homo sapiens
1-isobutyl-1-[2-(4-methoxyphenyl)ethyl]hydrazine
-
Homo sapiens
1-methyl-1-(2-phenylethyl)hydrazine
-
Homo sapiens
1-methyl-1-(2-phenylpropyl)hydrazine
-
Homo sapiens
1-methyl-1-(3-phenylpropyl)hydrazine
-
Homo sapiens
1-[2-(2,3,4-trimethoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(2,5-dimethoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(2-chlorophenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(2-fluorophenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(2-methoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(3,4,5-trimethoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(3,4-dimethoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(3-chlorophenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(3-fluorophenyl)-2-methoxyethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(3-methoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(4-chlorophenyl)-2-methoxyethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(4-chlorophenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(4-fluorophenyl)-2-methoxyethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(4-fluorophenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-(4-methoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-benzyloxy-2-(4-methoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-methoxy-1-(3-tolyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-methoxy-1-(4-methoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-methoxy-2-(1-naphthyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-methoxy-2-(2,3,4-trimethoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-methoxy-2-(2-naphthyl)ethyl]-1-methylhydrazine
-
Homo sapiens
1-[2-methoxy-2-(3-methoxyphenyl)ethyl]-1-methylhydrazine
-
Homo sapiens
2,2-dimethyl-2-(1-methylhydrazino)-1-phenylethanol
-
Homo sapiens
2-(1-isobutylhydrazino)-1-phenylethanol
-
Homo sapiens
2-(1-methylhydrazino)-1-(2,3,4-trimethoxyphenyl)ethanol
-
Homo sapiens
2-(1-methylhydrazino)-1-(2-naphthyl)ethanol
-
Homo sapiens
2-(1-methylhydrazino)-1-phenylethanol
-
Homo sapiens
2-(4-methoxyphenyl)-1-(1-methylhydrazino)-2-propanol
-
Homo sapiens
2-hydrazino-1-(3-methoxyphenyl)ethanol
-
Homo sapiens
2-hydrazino-1-(4-methoxyphenyl)ethanol
-
Homo sapiens
2-hydrazino-1-phenylethanol
-
Homo sapiens
additional information synthesis and in vitro activities of a series of VAP-1 selective inhibitors, molecular dynamics simulations and docking studies, pIC50 values, overview. Movements of Met211, Ser496, and especially Leu469 can enlarge the ligand-binding pocket, allowing larger ligands than those seen in the crystal structures to bind. Three-dimensional quantitative structure-activity relationship models for VAP-1 in comparison to MAOs, overview Homo sapiens
Phenelzine
-
Homo sapiens
Semicarbazide
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Cu2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens VAP-1/SSAOs convert amines into aldehydes. SSAOs are distinct from the mammalian monoamine oxidases, MAOs, but their substrate specificities are partly overlapping ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16853
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzylamine + H2O + O2
-
Homo sapiens benzaldehyde + NH3 + H2O2
-
?
additional information VAP-1/SSAOs convert amines into aldehydes. SSAOs are distinct from the mammalian monoamine oxidases, MAOs, but their substrate specificities are partly overlapping Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
More VAP-1 belongs to the semicarbazide-sensitive amine oxidases, SSAOs Homo sapiens
semicarbazide-sensitive amine oxidase
-
Homo sapiens
SSAO
-
Homo sapiens
VAP-1
-
Homo sapiens
vascular adhesion protein-1
-
Homo sapiens

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
7.6
-
assay at Homo sapiens