BRENDA - Enzyme Database

Classical and slow-binding inhibitors of human type II arginase

Colleluori, D.M.; Ash, D.E.; Biochemistry 40, 9356-9362 (2001)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
3.5.3.1
medicine
enzyme is a target for inhibitors used in therapeutic treatment of smooth muscle disorders, such as erectile dysfunction
Homo sapiens
3.5.3.1
pharmacology
enzyme is a target for inhibitor design based on arginine analogues with uncharged, tetrahedral functional groups
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
3.5.3.1
(S)-(2-boronoethyl)-L-cysteine
boronic acid-based transition state analogue, classical competitive inhibition at pH 7.5, slow-binding inhibition at pH 9.5
Homo sapiens
3.5.3.1
2(S)-amino-6-boronohexanoic acid
boronic acid-based transition state analogue, classical competitive inhibition at pH 7.5, slow-binding inhibition at pH 9.5
Homo sapiens
3.5.3.1
agmatine
-
Homo sapiens
3.5.3.1
L-argininamide
-
Homo sapiens
3.5.3.1
L-argininic acid
-
Homo sapiens
3.5.3.1
L-canavanine
-
Homo sapiens
3.5.3.1
L-homoarginine
-
Homo sapiens
3.5.3.1
L-N5-(1-iminoethyl)-ornithine
-
Homo sapiens
3.5.3.1
L-N6-(1-iminoethyl)-lysine
-
Homo sapiens
3.5.3.1
L-thiocitrulline
-
Homo sapiens
3.5.3.1
Nomega-amino-L-arginine
-
Homo sapiens
3.5.3.1
Nomega-hydroxy-L-arginine
competitive, reaction intermediate
Homo sapiens
3.5.3.1
Nomega-hydroxy-nor-L-arginine
competitive, reaction intermediate analogue
Homo sapiens
3.5.3.1
Nomega-Nitro-L-arginine
-
Homo sapiens
3.5.3.1
S-(2-aminoethyl)isothiourea
-
Homo sapiens
3.5.3.1
S-(3-aminopropyl)isothiourea
-
Homo sapiens
3.5.3.1
S-methyl-L-thiocitrulline
-
Homo sapiens
Localization
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
3.5.3.1
mitochondrion
-
Homo sapiens
5739
-
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.3.1
L-arginine + H2O
Homo sapiens
enzyme is involved in regulation of nitric oxide biosynthesis by modulating arginine availability for nitric oxide synthase
L-ornithine + urea
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.5.3.1
Homo sapiens
-
isozyme type II
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.3.1
L-arginine + H2O
enzyme is involved in regulation of nitric oxide biosynthesis by modulating arginine availability for nitric oxide synthase
654612
Homo sapiens
L-ornithine + urea
-
-
-
?
3.5.3.1
L-arginine + H2O
reaction intermediate is Nomega-hydroxy-L-arginine
654612
Homo sapiens
L-ornithine + urea
-
-
-
?
Temperature Optimum [°C]
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
3.5.3.1
22
-
assay at room temperature
Homo sapiens
Ki Value [mM]
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
3.5.3.1
additional information
-
additional information
estimated Ki for several inhibitors, overview, inhibition kinetics
Homo sapiens
3.5.3.1
0.0000085
-
2(S)-amino-6-boronohexanoic acid
pH 9.5, 22°C
Homo sapiens
3.5.3.1
0.00003
-
(S)-(2-boronoethyl)-L-cysteine
pH 9.5, 22°C
Homo sapiens
3.5.3.1
0.000051
-
Nomega-hydroxy-nor-L-arginine
pH 7.5, 22°C
Homo sapiens
3.5.3.1
0.00025
-
2(S)-amino-6-boronohexanoic acid
pH 7.5, 22°C
Homo sapiens
3.5.3.1
0.00031
-
(S)-(2-boronoethyl)-L-cysteine
pH 7.5, 22°C
Homo sapiens
3.5.3.1
0.0016
-
Nomega-hydroxy-L-arginine
pH 7.5, 22°C
Homo sapiens
Application (protein specific)
EC Number
Application
Commentary
Organism
3.5.3.1
medicine
enzyme is a target for inhibitors used in therapeutic treatment of smooth muscle disorders, such as erectile dysfunction
Homo sapiens
3.5.3.1
pharmacology
enzyme is a target for inhibitor design based on arginine analogues with uncharged, tetrahedral functional groups
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
3.5.3.1
(S)-(2-boronoethyl)-L-cysteine
boronic acid-based transition state analogue, classical competitive inhibition at pH 7.5, slow-binding inhibition at pH 9.5
Homo sapiens
3.5.3.1
2(S)-amino-6-boronohexanoic acid
boronic acid-based transition state analogue, classical competitive inhibition at pH 7.5, slow-binding inhibition at pH 9.5
Homo sapiens
3.5.3.1
agmatine
-
Homo sapiens
3.5.3.1
L-argininamide
-
Homo sapiens
3.5.3.1
L-argininic acid
-
Homo sapiens
3.5.3.1
L-canavanine
-
Homo sapiens
3.5.3.1
L-homoarginine
-
Homo sapiens
3.5.3.1
L-N5-(1-iminoethyl)-ornithine
-
Homo sapiens
3.5.3.1
L-N6-(1-iminoethyl)-lysine
-
Homo sapiens
3.5.3.1
L-thiocitrulline
-
Homo sapiens
3.5.3.1
Nomega-amino-L-arginine
-
Homo sapiens
3.5.3.1
Nomega-hydroxy-L-arginine
competitive, reaction intermediate
Homo sapiens
3.5.3.1
Nomega-hydroxy-nor-L-arginine
competitive, reaction intermediate analogue
Homo sapiens
3.5.3.1
Nomega-Nitro-L-arginine
-
Homo sapiens
3.5.3.1
S-(2-aminoethyl)isothiourea
-
Homo sapiens
3.5.3.1
S-(3-aminopropyl)isothiourea
-
Homo sapiens
3.5.3.1
S-methyl-L-thiocitrulline
-
Homo sapiens
Ki Value [mM] (protein specific)
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
3.5.3.1
additional information
-
additional information
estimated Ki for several inhibitors, overview, inhibition kinetics
Homo sapiens
3.5.3.1
0.0000085
-
2(S)-amino-6-boronohexanoic acid
pH 9.5, 22°C
Homo sapiens
3.5.3.1
0.00003
-
(S)-(2-boronoethyl)-L-cysteine
pH 9.5, 22°C
Homo sapiens
3.5.3.1
0.000051
-
Nomega-hydroxy-nor-L-arginine
pH 7.5, 22°C
Homo sapiens
3.5.3.1
0.00025
-
2(S)-amino-6-boronohexanoic acid
pH 7.5, 22°C
Homo sapiens
3.5.3.1
0.00031
-
(S)-(2-boronoethyl)-L-cysteine
pH 7.5, 22°C
Homo sapiens
3.5.3.1
0.0016
-
Nomega-hydroxy-L-arginine
pH 7.5, 22°C
Homo sapiens
Localization (protein specific)
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
3.5.3.1
mitochondrion
-
Homo sapiens
5739
-
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.3.1
L-arginine + H2O
Homo sapiens
enzyme is involved in regulation of nitric oxide biosynthesis by modulating arginine availability for nitric oxide synthase
L-ornithine + urea
-
-
?
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.3.1
L-arginine + H2O
enzyme is involved in regulation of nitric oxide biosynthesis by modulating arginine availability for nitric oxide synthase
654612
Homo sapiens
L-ornithine + urea
-
-
-
?
3.5.3.1
L-arginine + H2O
reaction intermediate is Nomega-hydroxy-L-arginine
654612
Homo sapiens
L-ornithine + urea
-
-
-
?
Temperature Optimum [°C] (protein specific)
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
3.5.3.1
22
-
assay at room temperature
Homo sapiens