Information on EC 3.4.17.21 - Glutamate carboxypeptidase II

New: Word Map on EC 3.4.17.21
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Mark a special word or phrase in this record:
Select one or more organisms in this record:
Show additional data
Do not include text mining results
Include (text mining) results (more...)
Include results (AMENDA + additional results, but less precise; more...)


The expected taxonomic range for this enzyme is: Coelomata

EC NUMBER
COMMENTARY
3.4.17.21
-
RECOMMENDED NAME
GeneOntology No.
Glutamate carboxypeptidase II
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
release of an unsubstituted, C-terminal glutamyl residue, typically from Ac-Asp-Glu or folylpoly-gamma-glutamates
show the reaction diagram
-
-
-
-
release of an unsubstituted, C-terminal glutamyl residue, typically from Ac-Asp-Glu or folylpoly-gamma-glutamates
show the reaction diagram
active site structure, substrate binding involving Asp210, and catalytic reaction mechanism involving Glu424 and the Zn2+ ions, the substrate binding cavity involves residues Arg463, Arg534, Arg536, stabilized by Glu457, Asp465, and Ser454
-
release of an unsubstituted, C-terminal glutamyl residue, typically from Ac-Asp-Glu or folylpoly-gamma-glutamates
show the reaction diagram
substrate recognition and induced-fit substrate binding mode, active site structure, catalytic mechanism involving Glu424
-
release of an unsubstituted, C-terminal glutamyl residue, typically from Ac-Asp-Glu or folylpoly-gamma-glutamates
show the reaction diagram
T640 is involved in catalysis, the N-glycosylation status is important for actalytic activity
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
hydrolysis of peptide bond
-
-
hydrolysis of peptide bond
-
-
hydrolysis of peptide bond
-
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
Alanine, aspartate and glutamate metabolism
-
-
Metabolic pathways
-
-
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
100 kDa ileum brush border membrane protein
-
-
-
-
Acetylaspartylglutamate dipeptidase
-
-
-
-
Dipeptidase, acetylaspartylglutamate
-
-
-
-
EC 3.4.19.8
-
-
formerly
-
FGCP
-
-
-
-
FGCP
-
-
folate hydrolase 1
-
-
FOLH1
-
-
Folylpoly-gamma-glutamate carboxypeptidase
-
-
-
-
folylpoly-gamma-glutamate carboxypeptidase II
-
-
GCP II
-
-
GCP II
Mus musculus C57/Bl
-
-
-
GCPII
Q04609
-
GCPII
Q9CZR2
-
GCPIII
Q9CZR2
-
glutamate carboxypeptidase
-
-
glutamate carboxypeptidase II
-
-
glutamate carboxypeptidase II
Q04609
-
glutamate carboxypeptidase II
-
-
glutamate carboxypeptidase II
-
-
glutamate carboxypeptidase III
-
-
glutamate carboxypeptidase III
Q9CZR2
-
I100
-
-
-
-
Ileal dipeptidylpeptidase
-
-
-
-
Membrane glutamate carboxypeptidase
-
-
-
-
N-acetyl-alpha-linked acidic dipeptidase
-
-
N-acetyl-alpha-linked acidic dipeptidase I
-
-
N-acetylaspartylglutamate peptidase
-
-
N-acetylated alpha-linked acid dipeptidase
-
-
N-Acetylated alpha-linked acidic dipeptidase
-
-
-
-
N-Acetylated alpha-linked acidic dipeptidase
-
-
N-Acetylated alpha-linked acidic dipeptidase
-
-
N-Acetylated alpha-linked acidic dipeptidase
-
-
N-Acetylated-alpha-linked acidic dipeptidase
-
-
-
-
N-Acetylated-alpha-linked acidic dipeptidase
Q9CZR2
-
N-acetylated-alpha-linked acidic dipeptidase 2
Q9CZR2
-
N-acetylated-alpha-linked acidic dipeptidase II
Q9CZR2
-
N-Acetylated-alpha-linked-acidic dipeptidase
-
-
-
-
N-Acetylated-alpha-linked-acidic dipeptidase
-
-
N-acetylated-alpha-linked-acidic-dipeptidase
-
-
N-Acetylated-alpha-linked-amino dipeptidase
-
-
-
-
NAADLADase
-
-
NAADLADse
-
-
NAAG degradation enzyme
-
-
NAAG peptidase
-
-
NAAG peptidase
Q9CZR2
-
NAAG peptidase II
Q9CZR2
-
NAAG-hydrolyzing activity
-
-
NAALA dipeptidase
-
-
-
-
NAALADase
-
-
-
-
NAALADase
-
-
NAALADase
Q9CZR2
-
Naaladase I
-
-
NAALADase II
Q9CZR2
-
NLD I
-
-
PMSA
-
-
prostate specific membrane antigen
-
-
prostate specific membrane antigen
-
-
Prostate-specific membrane antigen
-
-
-
-
Prostate-specific membrane antigen
-
-
Prostate-specific membrane antigen
-
-
Prostate-specific membrane antigen homolog
-
-
-
-
prostate-specificmembrane antigen
-
-
Prostrate-specific membrane antigen
-
-
-
-
PSM
-
-
-
-
PSM antigen
-
-
-
-
PSMA
-
-
-
-
Pteroylpoly-gamma-glutamate carboxypeptidase
-
-
-
-
Rat NAAG peptidase
-
-
-
-
mGCP
-
-
-
-
additional information
-
glutamate carboxypeptidase III and glutamate carboxypeptidase II belong to the transferrin receptor/glutamate carboxypeptidase II superfamily
CAS REGISTRY NUMBER
COMMENTARY
111070-04-3
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
bifunctional enzyme
-
-
Manually annotated by BRENDA team
bifunctional enzyme, gene PMSA
-
-
Manually annotated by BRENDA team
persons of both sexes and different ages with schizophrenia
-
-
Manually annotated by BRENDA team
cynomolgus monkey
-
-
Manually annotated by BRENDA team
bifunctional enzyme, gene folh1
-
-
Manually annotated by BRENDA team
C57/Bl mice
-
-
Manually annotated by BRENDA team
gene Naalad2
SwissProt
Manually annotated by BRENDA team
Mus musculus C57/Bl
C57/Bl mice
-
-
Manually annotated by BRENDA team
female wistar rat
-
-
Manually annotated by BRENDA team
male Long-Evans rats
-
-
Manually annotated by BRENDA team
male sprague-dawley rats
-
-
Manually annotated by BRENDA team
male Wistar rats
-
-
Manually annotated by BRENDA team
stably expressed in CHO cells
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
inhibition of the GCP II-catalyzed reaction is beneficial for the treatment of degenerative diseases associated with excess glutamate. Inhibition of GCP II is neuroprotective in a variety of cell and animal models of disease involving excess glutamate. N-acetyl-aspartyl-glutamate can acts as a marker of glutamate carboxypeptidase II inhibition
malfunction
-
involvement of the endogenous NAAG-NAALADase signaling pathway in cocaine addiction. Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats via a NAAG-mGluR2/3-mediated mechanism, overview
physiological function
-
PSMA acts as a glutamate-preferring carboxypeptidase in human prostate tissue, and plays a role in folic acid utilization and metabolism
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
folyl-poly-gamma-glutamate + H2O
?
show the reaction diagram
-
cleavage of the C-terminal glutamate
-
-
?
gamma-L-Glu-L-Glu + H2O
L-Glu + L-Glu
show the reaction diagram
-
-
-
-
-
L-Asp-L-Glu + H2O
L-Asp + L-Glu
show the reaction diagram
-
-
-
-
-
L-Glu-L-Glu + H2O
L-Glu + L-Glu
show the reaction diagram
-
-
-
-
-
N-acetyl-alpha L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
enantiospecific reaction
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
enzyme inhibition reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion traumatic brain injury
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
enzyme regulation is mediated by glial glutamate and acetylcholine receptors in the nervous tissue
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG, a neurodipeptide, the enzyme acts as membrane-bound receptor being recycled through clathrin coated pits, expression regulation within cells and involvement in prostate cancer and metastasis, overview
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG, a neurodipeptide, the enzyme acts as membrane-bound receptor being recycled through clathrin coated pits, expression regulation within cells in prostate cancer and metastasis, overview
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG, a presynaptically active endogenous neuropeptide which is cleaved by the enzyme in the extracellular space
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
NAAG peptidase inhibitor reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion TBI in rats
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
supply of the primary excitatory neurotransmitter glutamate
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
supply of the primary excitatory neurotransmitter glutamate, the enzyme is involved in neurological disorders, and neuropathic and inflammatory pain
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Q9CZR2
the enzyme inactivates the neurotransmitter in the synaptic cleft
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is involved in glutamate-mediated neurodegenerative disorders, enzyme inhibition is a mechanism for reduction of excitotoxic glutamate
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is involved in suppressing prostate cancer invasiveness
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is responsible for cleavage of NAAG to yield free glutamate
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is responsible for glutamate supply, enzyme inhibition decreases the glutamate and increases the N-acetyl-alpha-L-aspartyl-L-glutamate concentration in the brain, which can be a method to treat opioid tolerance and diminish effects of morphine withdrawal, overview
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Q04609
the essential enzyme is involved in prostate cancer, stroke, amyotrophic lateral sclerosis, and neuropathic pain
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Q9CZR2
i.e. NAAG
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Q04609
i.e. NAAG, C-terminal glutamate recognition
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Mus musculus C57/Bl
-
the enzyme is responsible for glutamate supply, enzyme inhibition decreases the glutamate and increases the N-acetyl-alpha-L-aspartyl-L-glutamate concentration in the brain, which can be a method to treat opioid tolerance and diminish effects of morphine withdrawal, overview, i.e. NAAG
-
-
?
N-acetyl-Asp-Glu + H2O
N-acetyl-Asp + Glu
show the reaction diagram
-
-
-
-
?
N-acetyl-Asp-Glu + H2O
N-acetyl-Asp + Glu
show the reaction diagram
-
-
-
-
?
N-acetyl-Asp-Glu + H2O
N-acetyl-Asp + Glu
show the reaction diagram
-
the enzyme converts N-acetylaspartylglutamate from a neuroprotectant to a neurotoxin
-
-
?
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
-
-
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
P70627
-
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
-
-
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
-
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
-
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
-
-
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
N-Acetyl-L-Asp + L-Glu
show the reaction diagram
-
-
no formation of acetate
-
N-Acetyl-L-Asp-L-Glu + H2O
?
show the reaction diagram
-
functions as a cell surface peptidase, possibly hydrolzing peptides in prostatic fluid
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
?
show the reaction diagram
-
may play a role in signaling between non-myelinating Schwann cells and peripheral axons
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
?
show the reaction diagram
-
role in synaptic peptide degradation
-
-
-
N-acetyl-L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
L-glutamate + N-acetyl-L-aspartate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
L-glutamate + N-acetyl-L-aspartate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
L-glutamate + N-acetyl-L-aspartate
show the reaction diagram
-
NAALADase, a neuropeptidase that produces the neurotransmitter glutamate and N-acetyl-Laspartate throught hydrolysis of N-acetyl-L-aspartyl-L-glutamate
-
-
?
N-[4-(phenylazo)-benzoyl]-L-glutamyl-gamma-L-glutamic acid + H2O
?
show the reaction diagram
-
-
-
-
?
poly-gamma-glutamate folate + H2O
?
show the reaction diagram
-
-
-
-
?
poly-gamma-glutamate folate + H2O
?
show the reaction diagram
-
activity outside of the cell
-
-
?
poly-gamma-Glutamylfolate + H2O
L-Glu + gamma-glutamylfolate
show the reaction diagram
-
-
removes sequentially gamma-linked glutamates
-
pteroylpentaglutamate + H2O
L-Glu + pteroylglutamate
show the reaction diagram
-
-
-
-
methotrexate triglutamate + H2O
L-Glu + methotrexate
show the reaction diagram
-
-
-
-
additional information
?
-
-
hydrolysis of peptide bonds of Asp or Glu to a Glu residue with unsubstituted alpha-carboxyl group. The amide bonds to Glu from the substituted benzoate in folate and methorexate molecules are resistant to hydrolysis
-
-
-
additional information
?
-
-
enzyme inhibition depresses mossy fiber-CA3 synaptic transmission
-
-
-
additional information
?
-
-
the enzyme interacts with filamin leading to internalization of PMSA into cells in the perinuclear region, overview
-
-
-
additional information
?
-
-
bifunctional enzyme performing folate hydrolase and N-acetylated alpha-linked acidic dipeptidase, NAALADase, activities
-
-
-
additional information
?
-
-
bifunctional enzyme performing folate hydrolase and N-acetylated alpha-linked acidic dipeptidase, NAALADase, activities
-
-
-
additional information
?
-
-
intestinal absorption of polyglutamyl folates involves cleavage of the glutamate side chain by FGCP
-
-
-
additional information
?
-
-
cross-linking of cell surface PSMA with specific antibodies activates the small GTPases RAS and RAC1 and the MAPKs p38 and ERK1/2 in prostate carcinoma LNCaP cells via NF-kappaB activation, overview. Proliferation of LNCaP cells is inducible by interleukin-6, CCL5 or by cross-linking of PSMA
-
-
-
additional information
?
-
-
PSMA is highly homologous to N-acetylated alpha-linked acidic dipeptidase, NAALADase
-
-
-
additional information
?
-
-
PSMA-targeted photodynamic therapy on cytoskeletal networks in prostate cancer cells results in rapid disruption of microtubules (alpha-/beta-tubulin), microfilaments (actin), and intermediate filaments (cytokeratin 8/18) in the cytoplasm of LNCaP cells. The collapse of cytoplasmic microtubules and the later nuclear translocation of alpha-/beta-tubulin are the most dramatic alternation, overview
-
-
-
additional information
?
-
-
the S1' pocket, the pharmacophore pocket of GCPIII, is shaped by residues Phe199, Arg200, Asn247, Glu414, Gly417, Leu418, Gly508, Tyr542, Lys689 and Tyr690. The specificity of GCPIII towards the P1' glutamate (or glutamate-like moieties) is determined by a combination of ionic and polar interactionsGCPIII substrate-binding cavity structure, overview
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
N-acetyl-alpha L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
enzyme inhibition reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion traumatic brain injury
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
enzyme regulation is mediated by glial glutamate and acetylcholine receptors in the nervous tissue
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG, a neurodipeptide, the enzyme acts as membrane-bound receptor being recycled through clathrin coated pits, expression regulation within cells and involvement in prostate cancer and metastasis, overview
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG, a neurodipeptide, the enzyme acts as membrane-bound receptor being recycled through clathrin coated pits, expression regulation within cells in prostate cancer and metastasis, overview
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
i.e. NAAG, a presynaptically active endogenous neuropeptide which is cleaved by the enzyme in the extracellular space
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
NAAG peptidase inhibitor reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion TBI in rats
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
supply of the primary excitatory neurotransmitter glutamate
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
supply of the primary excitatory neurotransmitter glutamate, the enzyme is involved in neurological disorders, and neuropathic and inflammatory pain
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Q9CZR2
the enzyme inactivates the neurotransmitter in the synaptic cleft
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is involved in glutamate-mediated neurodegenerative disorders, enzyme inhibition is a mechanism for reduction of excitotoxic glutamate
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is involved in suppressing prostate cancer invasiveness
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is responsible for cleavage of NAAG to yield free glutamate
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
-
the enzyme is responsible for glutamate supply, enzyme inhibition decreases the glutamate and increases the N-acetyl-alpha-L-aspartyl-L-glutamate concentration in the brain, which can be a method to treat opioid tolerance and diminish effects of morphine withdrawal, overview
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Q04609
the essential enzyme is involved in prostate cancer, stroke, amyotrophic lateral sclerosis, and neuropathic pain
-
-
?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O
N-acetyl-alpha-L-aspartate + L-glutamate
show the reaction diagram
Mus musculus C57/Bl
-
the enzyme is responsible for glutamate supply, enzyme inhibition decreases the glutamate and increases the N-acetyl-alpha-L-aspartyl-L-glutamate concentration in the brain, which can be a method to treat opioid tolerance and diminish effects of morphine withdrawal, overview
-
-
?
N-acetyl-Asp-Glu + H2O
N-acetyl-Asp + Glu
show the reaction diagram
-
-
-
-
?
N-acetyl-Asp-Glu + H2O
N-acetyl-Asp + Glu
show the reaction diagram
-
-
-
-
?
N-acetyl-Asp-Glu + H2O
N-acetyl-Asp + Glu
show the reaction diagram
-
the enzyme converts N-acetylaspartylglutamate from a neuroprotectant to a neurotoxin
-
-
?
N-Acetyl-L-Asp-L-Glu + H2O
?
show the reaction diagram
-
functions as a cell surface peptidase, possibly hydrolzing peptides in prostatic fluid
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
?
show the reaction diagram
-
may play a role in signaling between non-myelinating Schwann cells and peripheral axons
-
-
-
N-Acetyl-L-Asp-L-Glu + H2O
?
show the reaction diagram
-
role in synaptic peptide degradation
-
-
-
N-acetyl-L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
N-acetyl-L-aspartate + L-glutamate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
L-glutamate + N-acetyl-L-aspartate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
L-glutamate + N-acetyl-L-aspartate
show the reaction diagram
-
-
-
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
L-glutamate + N-acetyl-L-aspartate
show the reaction diagram
-
NAALADase, a neuropeptidase that produces the neurotransmitter glutamate and N-acetyl-Laspartate throught hydrolysis of N-acetyl-L-aspartyl-L-glutamate
-
-
?
poly-gamma-glutamate folate + H2O
?
show the reaction diagram
-
activity outside of the cell
-
-
?
folyl-poly-gamma-glutamate + H2O
?
show the reaction diagram
-
cleavage of the C-terminal glutamate
-
-
?
additional information
?
-
-
enzyme inhibition depresses mossy fiber-CA3 synaptic transmission
-
-
-
additional information
?
-
-
the enzyme interacts with filamin leading to internalization of PMSA into cells in the perinuclear region, overview
-
-
-
additional information
?
-
-
intestinal absorption of polyglutamyl folates involves cleavage of the glutamate side chain by FGCP
-
-
-
additional information
?
-
-
cross-linking of cell surface PSMA with specific antibodies activates the small GTPases RAS and RAC1 and the MAPKs p38 and ERK1/2 in prostate carcinoma LNCaP cells via NF-kappaB activation, overview. Proliferation of LNCaP cells is inducible by interleukin-6, CCL5 or by cross-linking of PSMA
-
-
-
additional information
?
-
-
PSMA is highly homologous to N-acetylated alpha-linked acidic dipeptidase, NAALADase
-
-
-
additional information
?
-
-
PSMA-targeted photodynamic therapy on cytoskeletal networks in prostate cancer cells results in rapid disruption of microtubules (alpha-/beta-tubulin), microfilaments (actin), and intermediate filaments (cytokeratin 8/18) in the cytoplasm of LNCaP cells. The collapse of cytoplasmic microtubules and the later nuclear translocation of alpha-/beta-tubulin are the most dramatic alternation, overview
-
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Br-
-
2 mM, activation
Ca2+
-
activation
Ca2+
-
positively regulates enzyme expression
Cl-
-
2 mM, activation
Co2+
-
activation
Co2+
Q9CZR2
stimulates the metallopeptidase
F-
-
100 mM, 20% of the activity compared to Cl-
I-
-
2 mM, activation
K+
-
extracellularly applied K+ increases the enzyme activity in vivo in glial cells and the ventral nerve cord
Mg2+
-
activation
NO3-
-
2 mM , activation
Sr2+
-
activation
Zn2+
-
metalloproteinase, 1 mM ZnCl2 increases activity 2-3fold
Zn2+
-
interacts with the glutamate recognition site
Zn2+
-
zinc-metalloenzyme, 2 Zn2+ bound per active site
Zn2+
-
involved in substrate binding
Zn2+
Q9CZR2
stimulates the metallopeptidase
Zn2+
-
zinc-metallopeptidase
Zn2+
-
the enzyme contains a binuclear Zn2+ binding site, involved in the reaction mechanism
Zn2+
-
zinc-metallopeptidase
Zn2+
-
zinc-metallopeptidase
Zn2+
-
zinc-metallopeptidase
Zn2+
-
-
Zn2+
-
binding structure of Zn2+ ions in the bimetallic active site, overview
Mn2+
-
activation
additional information
-
GCPIII and GCPII are metalloenzymes
additional information
-
PSMA is a type II transmembrane metallopeptidase
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2S)-2-([hydroxy[2-(4-hydroxyphenyl)ethoxy]phosphoryl]methyl)pentanedioic acid
-
-
(2S)-2-([[2-(4-fluorophenyl)ethoxy](hydroxy)phosphoryl]methyl)pentanedioic acid
-
-
(2S)-2-([[2-(4-[[N-(tert-butoxycarbonyl)glycyl]amino]phenyl)ethoxy](hydroxy)phosphoryl]methyl)pentanedioic acid
-
-
(2S)-2-[([[(1S)-1,3-dicarboxypropyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]carbonyl)amino]pentanedioic acid
-
the inhibitor has the ability to reduce the perception of inflammatory pain
(2S)-2-[([[(1S)-1-carboxy-2-phenylethyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(1S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(1S)-1-carboxy-3-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]-4-(2H-tetrazol-5-yl)butanoic acid
-
-
(2S)-2-[([[(1S)-3-carboxy-1-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(S)-carboxy(4-hydroxyphenyl)methyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[[(2-[4-[(tert-butoxycarbonyl)amino]phenyl]ethoxy)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S)-2-[[([(1S)-1-carboxy-3-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl]amino)carbonyl]amino]pentanedioic acid
-
-
(2S)-2-[[([(1S)-3-carboxy-1-[2-(2-cyanoethyl)-2H-tetrazol-5-yl]propyl]amino)carbonyl]amino]pentanedioic acid
-
-
(2S)-2-[[butyl(hydroxy)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[ethyl(hydroxy)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[hydroxy(2-phenylethoxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S)-2-[[hydroxy(3-phenylpropoxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S)-2-[[hydroxy(methyl)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[hydroxy(phenyl)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[hydroxy(phenyl)phosphorothioyl]oxy]pentanedioic acid
-
-
(2S)-2-[[hydroxy(phenyl)phosphoryl]amino]pentanedioic acid
-
-
(2S)-2-[[[2-[4-(acetylamino)phenyl]ethoxy](hydroxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S,2'S,4R)-4-benzyl-N,N'-carbonyldiglutamic acid
-
-
(2S,2'S,4R,4'R)-4,4'-dibenzyl-N,N'-carbonyldiglutamic acid
-
-
(2S,2'S,4R,4'R)-N,N'-carbonyl-4,4'-dimethyldiglutamic acid
-
-
(2S,2'S,4S)-N,N'-carbonyl-4-methyldiglutamic acid
-
-
(2S,2'S,4S,4'S)-N,N'-carbonyl-4,4'-dimethyldiglutamic acid
-
-
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid
-
EPE, a phosphapeptide transition state analog of glutamyl-glutamate
(2S,4R)-2-[([[(1S,3R)-1,3-dicarboxybutyl]amino]carbonyl)amino]-4-methylpentanedioic acid
-
-
(2S,4S)-2-[([[(1S,3S)-1,3-dicarboxybutyl]amino]carbonyl)amino]-4-methylpentanedioic acid
-
-
(4S)-4-[([[(1S)-3-carboxy-1-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]-4-(2H-tetrazol-5-yl)butanoic acid
-
-
(9S,13S)-1-(3-iodophenyl)-3,11-dioxo-2,4,10,12-tetraazapentadecane-9,13,15-tricarboxylic acid
-
-
(R)-2-(3-mercaptopropyl)-pentanedioic acid
-
equally potent as the S-isomer, 0.000085 mM
(R)-2-(3-mercaptopropyl)-pentanedioic acid
-
antinociceptide effects in the chronic constriction injury model, cell culture model of cerebral ischemia
(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
-
40fold less potent than the S-isomer, IC50: 0.0014 mM
(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
-
neuroprotective effects in the middle cerebral artery occlusion model, cell culture model of cerebral ischemia
(R)-2-(phosphonomethyl)-pentanedioic acid
-
less potent than the S-isomer, IC50: 0.000030 mM
(R)-2-(phosphonomethyl)-pentanedioic acid
-
-
(S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid
-
DCMC
(S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid
-
DCFBC
(S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid
-
DCIBzL
(S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid
-
DCIT
(S)-2-(3-((S)-1-carboxy-5-(2-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(2-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-bromophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-chlorophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-fluorophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl)ureido)pentyl)ureido)pentanedioic acid
-
i.e. MIP-1095, the compound shows affinity to and uptake into prostate cancer cells, binding analysis, overview
(S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-phenylureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-bromobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-fluorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-iodobenzylamino)pentyl)ureido)pentanedioic acid
-
i.e. MIP-1072, the compound shows affinity to and uptake into prostate cancer cells, binding analysis, overview
(S)-2-(3-((S)-1-carboxy-5-(4-iodophenylsulfonamido)pentyl)-ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(naphthalen-1-ylmethylamino)pentyl)-ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-5-(benzylamino)-1-carboxypentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-(4-iodobenzyl)ureido)pentanedioic acid
-
-
(S)-2-(3-mercaptopropyl)-pentanedioic acid
-
equally potent as the R-isomer, 0.000067 mM
(S)-2-(3-mercaptopropyl)-pentanedioic acid
-
antinociceptide effects in the chronic constriction injury model, cell culture model of cerebral ischemia
(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
-
40fold more potent than the R-isomer, IC50: 0.000034 mM
(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
-
neuroprotective effects in the middle cerebral artery occlusion model, cell culture model of cerebral ischemia
(S)-2-(phosphonomethyl)-pentanedioic acid
-
more potent than the R-isomer, IC50: 0.0000001 mM
(S)-2-(phosphonomethyl)-pentanedioic acid
-
-
(S)-2-[3-((S)-1-carboxy-2-(4-hydroxyphenyl)ethyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-1-carboxy-2-(4-hydroxyphenyl)ethyl)ureido]pentanedioic acid
-
i.e. inhibitor ZJ17
(S)-2-[3-((S)-1-carboxy-2-phenylethyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl)ureido]pentanedioinc acid
-
i.e. inhibitor ZJ38
-
(S)-2-[3-((S)-1-carboxy-3-(methylsulfanyl)propyl)ureido]pentanedioic acid
-
i.e. inhibitor ZJ11
(S)-2-[3-((S)-1-carboxy-3-methylbutyl)ureido]pentanedioic acid
-
i.e. inhibitor ZJ43
(S)-2-[3-((S)-1-carboxy-3-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-3-carboxy-1-(1H-tetrazol-5-yl)propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-3-carboxy-1-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-alpha-carboxy-4-hydroxybenzyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-alpha-carboxybenzyl)ureido]pentanedioic acid
-
-
(S)-2-[3-(S)-(1,3-dicarboxypropyl)ureido]pentanedioinc acid
-
-
(S)-2-[3-(S)-(1,3-dicarboxypropyl)ureido]pentanedioinc acid
-
-
(S)-alpha-ethylglutamate
-
specific group II metabotropic glutamate receptor antagonist, in vivo activity
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-2,2'-ureylenedibutyric acid
-
-
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-4,4'-ureylenedibutyric acid
-
-
(S,S)-4,4'-di-(1H-tetrazol-5-yl)-2,2'-ureylenedibutyric acid
-
-
(S,S)-4,4'-di-(1H-tetrazol-5-yl)-4,4'-ureylenedibutyric acid
-
-
(S,S)-N,N'-carbonyl-2,2'-dimethyldiglutamic acid
-
-
(t-Bu)Cys-PSI[C-O]-Glu
-
IC50: 29 nM
(Z)-N-(N-Acetyldehydroaspartyl)-L-Glu
-
-
1,10-phenanthroline
-
1 mM, 90% inhibition
2-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 1700 nM
2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid
-
IC50: 2200 nM
2-(3-carboxybenyl)succinic acid
-
IC50: 0.015 mM
2-(3-cyanobenzyl)-5-mercaptopentanoic acid
-
IC50: 1800 nM
2-(3-hydroxybenzyl)-3-phosphonopropanoic acid
-
IC50: 508 nM
2-(3-mercaptopropyl)-pentanedioic acid
-
2-MPPA, specific, potent, competitive inhibition, has higher oral bioavailability compared to 2-PMPA, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia
2-(3-mercaptopropyl)-pentanedioic acid
-
2-MPPA, specific, potent, competitive inhibition, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia
2-(3-mercaptopropyl)-pentanedioic acid
-
i.e. 2-MPPA, IC50: 90 nM
2-(3-mercaptopropyl)-pentanedioic acid
-
i.e. 2-MPPA or GPI5693
2-(3-mercaptopropyl)-pentanedioic acid
-
2-MPPA, prevents morphine tolerance without affecting the acute morphine antinociception in vivo
2-(3-mercaptopropyl)pentanedioic acid
-
IC50: 90 nM. Orally bioavailable in rats
2-(3-mercaptopropyl)pentanedioic acid
-
orally bioavailable inhibitor
2-(3-sulfanylpropyl)pentanedioic acid
-
i.e. GPI-5693, attenuates cocaine-induced conditioned place preference
2-(phosphonomethyl)-4-(5H-tetrazol-5-yl)butanoic acid
-
IC50: 175 nM
2-(phosphonomethyl)-pentanedioic acid
-
-
2-(phosphonomethyl)-pentanedioic acid
-
2-PMPA
2-(phosphonomethyl)-pentanedioic acid
-
2-PMPA, specific, potent, competitive inhibition, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia
2-(phosphonomethyl)-pentanedioic acid
-
i.e. 2-PMPA, enzyme inhibition protects the rats in vivo against ischemic injury to the brain and spinal cord, and hypoxic and metabolic injury to neuronal cells in culture
2-(phosphonomethyl)-pentanedioic acid
Q9CZR2
2-PMPA, GCPIII IC50: 94 nM, GCPII IC50: 6.74 nM
2-(phosphonomethyl)-pentanedioic acid
-
2-PMPA, specific GCPII inhibitor, in vivo activity
2-(phosphonomethyl)-pentanedioic acid
-
i.e. 2-PMPA
2-(phosphonomethyl)-pentanedioic acid
-
i.e. 2-PMPA
2-(phosphonomethyl)-pentanedioic acid
-
2-PMPA
2-(phosphonomethyl)hexanedioic acid
-
IC50: 185 nM
2-(phosphonomethyl)hexanoic acid
-
IC50: 185 nM
2-(phosphonomethyl)pentanedioic acid
-
competitive
2-(phosphonomethyl)pentanedioic acid
-
IC50: 5.1 nM
2-(phosphonomethyl)pentanedioic acid
-
IC50: 0.3 nM
2-(phosphonomethyl)pentanedioic acid
-
-
2-(phosphonomethyl)pentanedioic acid
-
requires long-term daily dosing
2-(phosphonomethyl)pentanedioic acid
-
2-PMPA
2-(phosphonomethyl)pentanedioic acid
-
i.e. 2-PMPA, inhibits cocaine-induced behavioural sensitization
2-(phosphonomethyl)pentanedioic acid
-
i.e. 2-PMPA, a N-acetylated-alpha-linkedacidic dipeptidase inhibitor, attenuates cocaine self-administration and cocaine-induced reinstatement of drug seeking of rats
2-(Phosphonomethyl)pentanoate
-
-
2-(phosphonomethyl)succinic acid
-
IC50: 2200 nM
2-([hydroxy[3-(trifluoromethyl)benzyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 55 nM
2-([hydroxy[hydroxy(phenyl)methyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 55 nM
2-([hydroxy[hydroxy(pyridin-4-yl)methyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 10 nM
2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid
-
i.e. quisqualic acid, a glutamate-like inhibitor of GCPIII and GCPII
2-benzyl-3-phosphonopropanoic acid
-
IC50: 548 nM
2-benzyl-5-mercaptopentanoic acid
-
IC50: 1400 nM
2-oxoglutarate
-
0.1 mM, 46% inhibition
2-phosphonomethyl-pentanedoic acid
-
2-PMPA
2-[(hydroxy[[(4-methoxyphenyl)amino]methyl]phosphoryl)methyl]pentanedioic acid
-
IC50: 3 nM
2-[[(2,4-dicarboxybutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 0.5 nM
2-[[(2-carboxy-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 2 nM
2-[[(2-carboxy-4-phenylbutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 2 nM
2-[[(2-carboxyethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 1 nM
2-[[(2-carboxypropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 1.5 nM
2-[[(2-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 156 nM
2-[[(3,5-difluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 49 nM
2-[[(3-aminobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 143 nM
2-[[(3-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 70 nM
2-[[(4-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 64 nM
2-[[(anilinomethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 4 nM
2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 70 nM
2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 53 nM
2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 150 nM
2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 149 nM
2-[[hydroxy(3-nitrobenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50 59 nM
2-[[hydroxy(3-phenylpropyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 230 nM
2-[[hydroxy(4-methoxybenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 90 nM
2-[[hydroxy(4-methylbenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 68 nM
2-[[hydroxy(pentafluorobenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 82 nM. Significantly prevents neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In the chronic constrictive model of neuropathic pain, the inhibitor sifnificantly attenuats the hypersensitivity observed with saline-treated animals
2-[[hydroxy(phenyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 2930 nM
2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 560 nM
2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 360 nM
2-[[[(3-fluorophenyl)(hydroxy)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 16 nM
2-[[[(benzylamino)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 59 nM
2-[[[3,5-bis(trifluoromethyl)benzyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 55 nM
2-[[[3-(benzyloxy)-2-methyl-3-oxopropyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 95 nM
2-{[2-Carboxy-3-(4-methoxy-phenylamino)-propyl]-hydroxy-phosphinoylmethyl}-pentanedioic acid
-
IC50: 3 nM
3-(1-carboxy-4-mercaptobutoxy)benzoic acid
-
IC50: 14 nM
3-(2-carbamoyl-5-mercaptopentyl)benzoic acid
-
IC50: 640 nM
3-(2-carboxy-3-hydroxycarbamoylpropyl)benzoic acid
-
IC50: 0.015 mM
3-(2-carboxy-3-phosphonopropyl)benzoic acid
-
IC50: 120 nM
3-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 15 nM
3-(2-carboxy-5-mercaptopentyl)benzoic acid methyl ester
-
IC50: 2700 nM
3-(2-carboxy-5-mercaptosulfanylpentyl)benzoic acid
-
IC50: 0.02 mM
3-(2-carboxy-5-tritylsulfanylpentyl)benzoic acid
-
IC50: 0.02 mM
3-(3-mercaptopropyl)pentanedioic acid
-
presynaptic action of enzyme inhibition, enzyme inhibition depresses mossy fiber-CA3 synaptic transmission
3-(5-mercapto-2-methoxycarbonylpentyl)benzoic acid
-
IC50: 730 nM
3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid
-
IC50: 32 nM
3-[2-carboxy-3-(hydroxypentafluorophenylmethylphosphinoyl)propyl]benzoic acid
-
IC50: 2400 nM
4,4'-phosphinicobis(butane-1,3-dicarboxylic acid)
-
i.e. PBDA, effects of stereoisomers, overview
4,4'-phosphinicobis(butane-1,3-dicarboxylic acid)
-
i.e. PBDA
4-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 63 nM
4-(3-hydroxyphenyl)-2-(phosphonomethyl)butanoic acid
-
IC50: 508 nM
4-cyano-2-(phosphonomethyl)butanoic acid
-
IC50: 335 nM
4-phenyl-2-(phosphonomethyl)butanoic acid
-
IC50: 199 nM
5-oxoheptane-1,3,7-tricarboxylic acid
-
0.1 mM, 35% inhibition
5-oxononane-1,3,7,9-tetracarboxylic acid
-
inhibitor possesses mGluR3 agonist activity
Ala-Glu
-
0.0061 mM, 50% inhibition
Asp-Ala
-
0.1 mM, 26% inhibition
Asp-Asp
-
0.1 mM, 42% inhibition
Asp-Glu
-
0.0024 mM, 50% inhibition
Asp-Phe
-
0.1 mM, 22% inhibition
Asp-PSI[C-O-S]-Glu
-
IC50: 0.0461 mM
Asp-PSI[C-O]-Asp
-
IC50: 0.0038 mM
Asp-PSI[S]-Asp
-
0.1 mM, 42% inhibition
aspartate
-
0.1 mM, 42% inhibition
bestatin
-
0.29 mM, 79% inhibition
Cys-PSI[C-O-S]-Glu
-
IC50: 6.9 nM
cysteate
-
0.1 mM, 40% inhibition
cysteine sulfinate
-
0.1 mM, 42% inhibition
D-Glu-D-Glu
-
0.1 mM, 50% inhibition
D-Glu-PSI[C-O]-D-Glu
-
0.1 mM, 67% inhibition
D-Glu-PSI[C-O]-Glu
-
0.001 mM, 25% inhibition
diazabicycloalkane
-
cis- and trans-isomers, dipeptide mimetic
-
diphenyl 2-[[[2-[4-([[7-(diethylamino)-2-oxo-2H-chromen-3-yl]carbamoyl]amino)phenyl]ethoxy](hydroxy)phosphoryl]methyl]pentanedioate
-
-
dithiothreitol
-
1 mM, 94.8% inhibition
DUPA
-
enzyme active site binding structure, docking and modelling, detailed overview
EDTA
-
1 mM, 96.3% inhibition
EDTA
Q9CZR2
-
EGTA
-
1 mM, 92% inhibition
gamma-Glu-Glu
-
0.0095 mM, 50% inhibition
gamma-Glu-Glu
-
-
Glu-Asp
-
0.1 mM, 27% inhibition
Glu-Glu
-
0.00075 mM, 50% inhibition
Glu-Glu-Glu
-
0.062 mM, 50% inhibition
Glu-Glu-Glu
-
-
Glu-PSI[C-O-C-O]-Glu
-
0.001 mM, 9% inhibition
Glu-PSI[C-O]-Glu
-
IC50: 47 nM
glutathione
-
i.e. gamma-Glu-Cys-Gly, 0.019 mM, 50% inhibition
Gly-Glu
-
0.008 mM, 50% inhibition
Gly-Gly-Glu
-
0.00098 mM, 50% inhibition
Gly-PSI[C-O-S]-Glu
-
0.001 mM, 46% inhibition
GPI 5693
-
i.e. (R,S)-2-(3-mercaptopropyl)-pentanedioic acid or 2-MPPA, pharmacokinetics and safety of the NAALADase-inhibitor and its effects on the central nervous system after application in vivo, overview
GPI-16476
-
enantiomer of GPI-5693
GPI-16477
-
enantiomer of GPI-5693
GPI-18431
-
enzyme active site binding structure, docking and modelling, detailed overview
GPI-5693
-
-
GPI5232
-
i.e. 2-([((hydroxypentyfluorophenyl)methyl)phosphinoyl]methyl)pentanedioic acid
GPI5232
-
a 2-PMPA analogue
Ibotenate
-
0.1 mM, 45% inhibition
iodoacetate
-
1 mM, 38% inhibition
L-2-Amino-4-phosphonobutanoate
-
0.1 mM, 37% inhibition
L-Glu
-
0.032 mM, 50% inhibition
L-Glu
-
-
LY341495
-
-
N-(3,4-Dicarboxybutanoyl)glutamic acid
-
-
N-(Dicarboxymethyl)acetylglutaminic acid
-
-
N-(tert-butoxycarbonyl)glycyl-N-[4-[2-([[(2S)-2,4-dicarboxybutyl](hydroxy)phosphoryl]oxy)ethyl]phenyl]-L-prolinamide
-
-
N-(tert-butoxycarbonyl)glycylglycyl-N-[4-[2-([[(2S)-2,4-dicarboxybutyl](hydroxy)phosphoryl]oxy)ethyl]phenyl]glycinamide
-
-
N-Acetyl-Asp-Gln
-
0.1 mM, 49% inhibition
N-Acetyl-Asp-Glu-Asp
-
0.1 mM, 49% inhibition
N-Acetyl-Asp-Ser-Gly
-
0.1 mM, 37% inhibition
N-Acetyl-beta-L-Asp-L-Glu
-
-
N-Acetyl-beta-L-Asp-L-Glu
-
-
N-Acetyl-Glu-Asp
-
0.036 mM, 50% inhibition
N-Acetyl-Glu-Glu
-
0.00031 mM, 50% inhibition
N-acetyl-L-Asp
-
0.1 mM, 38% inhibition
N-Acetyl-L-Asp-L-Glu
-
0.00054 mM, 50% inhibition
N-acetyl-L-Glu
-
0.058 mM, 50% inhibition
N-Fumaryl-L-Glu
-
-
N-Succinyl-L-Glu
-
-
N-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]-L-glutamic acid
-
i.e. inhibitor ZJ17, antinociceptive effect of the inhibitor in the rat formalin test and the rat neuropathic pain model, overview
N-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]-L-glutamic acid
-
i.e. inhibitor ZJ17, antinociceptive effect of the inhibitor in the rat formalin test and the rat neuropathic pain model, agonist and antagonist activity on recombinantly expressed metabotropic glutamate receptor, overview
N-[[(1S)-1-carboxy-3-(methylsulfanyl)propyl]carbamoyl]-L-glutamic acid
-
i.e. inhibitor ZJ11, antinociceptive effect of the inhibitor in the rat formalin test and the rat neuropathic pain model, overview
N-[[(1S)-1-carboxy-3-(methylsulfanyl)propyl]carbamoyl]-L-glutamic acid
-
i.e. inhibitor ZJ11, antinociceptive effect of the inhibitor in the rat formalin test and the rat neuropathic pain model, agonist and antagonist activity on recombinantly expressed metabotropic glutamate receptor, overview
N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid
-
i.e. inhibitor ZJ43, antinociceptive effect of the inhibitor in the rat formalin test and the rat neuropathic pain model, overview
N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid
-
i.e. inhibitor ZJ43, antinociceptive effect of the inhibitor in the rat formalin test and the rat neuropathic pain model, agonist and antagonist activity on recombinantly expressed metabotropic glutamate receptor, overview
Phe-Glu
-
0.077 mM, 50% inhibition
pteroylglutamic acid
-
-
puromycin
-
0.5 mM, 55% inhibition
pyroglutamate
-
0.1 mM, 27% inhibition
pyropheophorbide-a conjugate
-
i.e. Ppa-2 conjugate, non-specificity of unconjugated Ppa, conjugation of a peptidomimetic inhibitor of PSMA to the porphyrinic PS, pyropheophorbide-a gives
quinolinate
-
0.1 mM, 41% inhibition
Quisqualic acid
-
0.00048 mM, 50% inhibition
Quisqualic acid
-
-
Quisqualic acid
-
-
S-2-((2-(S-4-(4-18F-fluorobenzamido)-4-carboxybutanamido)-S-2-carboxyethoxy)hydroxyphosphorylamino)-pentanedioic acid
-
-
S-2-((2-(S-4-amino-4-carboxybutanamido)-S-2-carboxyethoxy)-hydroxyphosphorylamino)-pentanedioic acid
-
phosphoramidate
Serine O-sulfate
-
0.042 mM, 50% inhibition
t-BuNHC(O)-Glu
-
0.001 mM, 10% inhibition
Tyr-Glu
-
0.1 mM, 45% inhibition
VA-033
-
i.e. 2-([(benzyloxy)phosphonyl]methyl)pentanedioic acid
VA-033
-
-
Val-Glu-Glu
-
0.036 mM, 50% inhibition
ZJ-43
-
i.e. (S)-2-[3-((S)-1-carboxy-3-methylbutyl)ureido]pentanedioic acid, the inhibitor enhances extracellular NAAG levels and reduces extracellular levels of amino acids neurotransmitter following traumatic brain injury in vivo
ZJ43
-
i.e. (S)-2-[3-((S)-1-carboxy-3-methylbutyl)ureido]pentanedioic acid
[HO2C(CH2)2CH(CO2H)CH2]2P(O)(OH)
-
-
MOPS
-
-
additional information
-
not inhibitory are pepstatin, iodoacetamide, amastatin
-
additional information
-
N-acetyl-L-Asp-D-Glu
-
additional information
-
GCPII inhibitors are attractive candidates for clinical treatment trials in amylotrophic lateral sclerosis
-
additional information
-
the androgen receptor negatively regulates the enzyme expression
-
additional information
-
glutamate receptor antagonists reduce the enzyme activity in vivo, overview
-
additional information
-
design of urea-based NAAG peptidase-specific inhibitors, IC50 values of the stereoisomers, inhibition strategies, overview, inhibitors are used in therapy of neurological disorders, overview, construction of a human traumatic brain injury, TBI, to test inhibitor effects, overview
-
additional information
-
design of urea-based NAAG peptidase-specific inhibitors, inhibition strategies, overview, construction of a stroke rat model and traumatic brain injury, TBI, to test inhibitor effects, overview
-
additional information
-
N-[N-((S)-1,3-dicarboxypropyl)carbamoyl]-S-3-iodo-L-tyrosine, i.e. DCIT, is a potent antagonist of the enzyme activity
-
additional information
-
GCPIII enzyme-inhibitor interactions and the architecture of the S1' pocket, overview
-
additional information
-
design and synthesis of a series of glutamate-urea-X heterodimeric inhibitors of PSMA, where X is epsilon-N-(o-I, m-I, p-I, p-Br, o-Cl, m-Cl, p-Cl, p-F, H)-benzyl-Lys and epsilon-(p-I, p-Br, p-Cl, p-F, H)-phenylureido-Lys, overview. PSMA binding of the benzyllysine series is significantly affected by the nature of the halogen substituent. The halogen atom has little affect on the binding affinity in the para-substituted phenylureido-Lys series
-
additional information
-
inhibitor in vivo distribution studies in mice bearing either PSMA-positive LNCaP or PSMA-negative PC-3 tumors, overview
-
additional information
-
phosphoramidate peptidomimetic PSMA inhibitors are capable of both cell-surface labeling of prostate cancer cells and intracellular delivery. Use of a PSMA inhibitor-conjugate of pyropheophorbide-a, i.e. Ppa-conjugate 2, for targeted photodynamic therapy to achieve apoptosis in PSMA and LNCaP cells, overview
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
dynorphin A
-
activates glutamate production in the spinal cord
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000066
N-acetyl-alpha-L-aspartyl-L-glutamate
-
recombinant mutant N195A
0.0001
N-acetyl-alpha-L-aspartyl-L-glutamate
-
recombinant mutant N121A
0.000321
N-acetyl-alpha-L-aspartyl-L-glutamate
-
recombinant wild-type enzyme
0.000334
N-acetyl-alpha-L-aspartyl-L-glutamate
-
recombinant mutant N638A
130
N-acetyl-Asp-Glu
-
pH 7.4, 37C
0.00014
N-Acetyl-L-Asp-L-Glu
-
-
0.0004
N-Acetyl-L-Asp-L-Glu
-
-
0.0005
N-Acetyl-L-Asp-L-Glu
-
no addition of Zn2+ to assay medium
0.0008
N-Acetyl-L-Asp-L-Glu
-
addition of Zn2+ to assay medium
0.065
N-Acetyl-L-Asp-L-Glu
-
-
540
N-Acetyl-L-Asp-L-Glu
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
4
N-acetyl-Asp-Glu
-
pH 7.4, 37C
1
N-acetyl-L-aspartyl-L-glutamate
-
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000008
(2S)-2-[([[(1S)-1,3-dicarboxypropyl]amino]carbonyl)amino]pentanedioic acid
-
pH 7.4, 37C
0.000003
(2S)-2-[([[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]carbonyl)amino]pentanedioic acid
-
pH 7.4, 37C
0.000012
(2S)-2-[([[(1S)-1-carboxy-2-phenylethyl]amino]carbonyl)amino]pentanedioic acid
-
pH 7.4, 37C
0.0000009
(2S)-2-[([[(1S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl]amino]carbonyl)amino]pentanedioic acid
-
pH 7.4, 37C
0.0000149
(2S)-2-[([[(1S)-1-carboxy-3-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]-4-(2H-tetrazol-5-yl)butanoic acid
-
pH 7.4, 37C
0.000335
(2S)-2-[([[(1S)-3-carboxy-1-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]pentanedioic acid
-
pH 7.4, 37C
0.0000059
(2S)-2-[([[(S)-carboxy(4-hydroxyphenyl)methyl]amino]carbonyl)amino]pentanedioic acid
-
pH 7.4, 37C
0.0000053
(2S)-2-[[([(1S)-1-carboxy-3-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl]amino)carbonyl]amino]pentanedioic acid
-
pH 7.4, 37C
0.002711
(2S)-2-[[([(1S)-3-carboxy-1-[2-(2-cyanoethyl)-2H-tetrazol-5-yl]propyl]amino)carbonyl]amino]pentanedioic acid
-
pH 7.4, 37C
0.000104
(2S)-2-[[butyl(hydroxy)phosphorothioyl]amino]pentanedioic acid
-
pH 7.4, 37C
0.00109
(2S)-2-[[ethyl(hydroxy)phosphorothioyl]amino]pentanedioic acid
-
pH 7.4, 37C
0.000719
(2S)-2-[[hydroxy(methyl)phosphorothioyl]amino]pentanedioic acid
-
pH 7.4, 37C
0.00639
(2S)-2-[[hydroxy(phenyl)phosphorothioyl]amino]pentanedioic acid
-
pH 7.4, 37C
0.0146
(2S)-2-[[hydroxy(phenyl)phosphorothioyl]oxy]pentanedioic acid
-
pH 7.4, 37C
0.00111
(2S)-2-[[hydroxy(phenyl)phosphoryl]amino]pentanedioic acid
-
pH 7.4, 37C
0.000095
(2S,2'S,4R)-4-benzyl-N,N'-carbonyldiglutamic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000953
(2S,2'S,4R)-4-benzyl-N,N'-carbonyldiglutamic acid
-
pH 7.4, 37C
0.000392
(2S,2'S,4R,4'R)-4,4'-dibenzyl-N,N'-carbonyldiglutamic acid
-
pH 7.4, 37C; pH 7.4, 37C, recombinant enzyme
0.00129
(2S,2'S,4R,4'R)-N,N'-carbonyl-4,4'-dimethyldiglutamic acid
-
pH 7.4, 37C, recombinant enzyme
0.000014
(2S,2'S,4S)-N,N'-carbonyl-4-methyldiglutamic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000144
(2S,2'S,4S)-N,N'-carbonyl-4-methyldiglutamic acid
-
pH 7.4, 37C
0.00111
(2S,2'S,4S,4'S)-N,N'-carbonyl-4,4'-dimethyldiglutamic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000129
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid
-
GCPII
0.0000346
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid
-
GCPIII
0.001285
(2S,4R)-2-[([[(1S,3R)-1,3-dicarboxybutyl]amino]carbonyl)amino]-4-methylpentanedioic acid
-
pH 7.4, 37C
0.001109
(2S,4S)-2-[([[(1S,3S)-1,3-dicarboxybutyl]amino]carbonyl)amino]-4-methylpentanedioic acid
-
pH 7.4, 37C
0.004388
(4S)-4-[([[(1S)-3-carboxy-1-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]-4-(2H-tetrazol-5-yl)butanoic acid
-
pH 7.4, 37C
0.0000015
(S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid
-
-
0.00000024
(S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
0.0000046
(S)-2-(3-((S)-1-carboxy-5-(4-iodobenzylamino)pentyl)ureido)pentanedioic acid
-
-
0.000003
(S)-2-[3-((S)-1-carboxy-2-(4-hydroxyphenyl)ethyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.000012
(S)-2-[3-((S)-1-carboxy-2-phenylethyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000009
(S)-2-[3-((S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000053
(S)-2-[3-((S)-1-carboxy-3-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.000335
(S)-2-[3-((S)-3-carboxy-1-(1H-tetrazol-5-yl)propyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.00271
(S)-2-[3-((S)-3-carboxy-1-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000059
(S)-2-[3-((S)-alpha-carboxy-4-hydroxybenzyl)ureido]pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000021
(S)-2-[3-((S)-alpha-carboxybenzyl)ureido]pentanedioic acid
-
pH 7.4, 37C; pH 7.4, 37C, recombinant enzyme
0.000008
(S)-2-[3-(S)-(1,3-dicarboxypropyl)ureido]pentanedioinc acid
-
pH 7.4, 37C, recombinant enzyme
0.00443
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-2,2'-ureylenedibutyric acid
-
pH 7.4, 37C, recombinant enzyme
0.004434
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-2,2'-ureylenedibutyric acid
-
pH 7.4, 37C
1
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-4,4'-ureylenedibutyric acid
-
above, pH 7.4, 37C, recombinant enzyme
0.000015
(S,S)-4,4'-di-(1H-tetrazol-5-yl)-2,2'-ureylenedibutyric acid
-
pH 7.4, 37C, recombinant enzyme
0.00439
(S,S)-4,4'-di-(1H-tetrazol-5-yl)-4,4'-ureylenedibutyric acid
-
pH 7.4, 37C, recombinant enzyme
0.000939
(S,S)-N,N'-carbonyl-2,2'-dimethyldiglutamic acid
-
pH 7.4, 37C; pH 7.4, 37C, recombinant enzyme
0.00003
2-(3-mercaptopropyl)-pentanedioic acid
-
-
0.0000002
2-(phosphonomethyl)-pentanedioic acid
-
-
0.0000003
2-(phosphonomethyl)-pentanedioic acid
-
-
0.0000014
2-(phosphonomethyl)-pentanedioic acid
-
pH 7.4, 37C, recombinant enzyme
0.0000002
2-(phosphonomethyl)pentanedioic acid
-
pH 7.4, 37C
0.0000014
2-(phosphonomethyl)pentanedioic acid
-
pH 7.4, 37C
0.00023
2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid
-
GCPIII
0.00102
2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid
-
GCPII
0.061
Ala-Glu
-
-
0.0024
Asp-Glu
-
-
0.1
D-Glu-D-Glu
-
-
0.000008
DUPA
-
-
0.095
gamma-Glu-Glu
-
-
0.00075
Glu-Glu
-
-
0.062
Glu-Glu-Glu
-
-
0.019
glutathione
-
i.e. gamma-Glu-Cys-Gly
0.008
Gly-Glu
-
-
0.00098
Gly-Gly-Glu
-
-
0.00003
GPI-18431
-
-
0.27
L-Glu
-
GCPIII
0.428
L-Glu
-
GCPII
0.036
N-Acetyl-Glu-Asp
-
-
0.00031
N-Acetyl-Glu-Glu
-
-
0.00054
N-Acetyl-L-Asp-L-Glu
-
-
0.058
N-acetyl-L-Glu
-
-
0.0000149
N-[[(1S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl]carbamoyl]-L-glutamic acid
-
pH 7.4, 37C
0.077
Phe-Glu
-
-
0.042
Serine O-sulfate
-
-
0.036
Val-Glu-Glu
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000002
(2S)-2-([hydroxy[2-(4-hydroxyphenyl)ethoxy]phosphoryl]methyl)pentanedioic acid
-
-
0.0003
(2S)-2-([[2-(4-fluorophenyl)ethoxy](hydroxy)phosphoryl]methyl)pentanedioic acid
-
-
0.0000007
(2S)-2-([[2-(4-[[N-(tert-butoxycarbonyl)glycyl]amino]phenyl)ethoxy](hydroxy)phosphoryl]methyl)pentanedioic acid
-
-
0.0000001
(2S)-2-[[(2-[4-[(tert-butoxycarbonyl)amino]phenyl]ethoxy)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
-
0.0000008
(2S)-2-[[hydroxy(2-phenylethoxy)phosphoryl]methyl]pentanedioic acid
-
-
0.000004
(2S)-2-[[hydroxy(3-phenylpropoxy)phosphoryl]methyl]pentanedioic acid
-
-
0.000004
(2S)-2-[[[2-[4-(acetylamino)phenyl]ethoxy](hydroxy)phosphoryl]methyl]pentanedioic acid
-
-
0.000018
(9S,13S)-1-(3-iodophenyl)-3,11-dioxo-2,4,10,12-tetraazapentadecane-9,13,15-tricarboxylic acid
-
-
0.0014
(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
-
40fold less potent than the S-isomer, IC50: 0.0014 mM
0.00003
(R)-2-(phosphonomethyl)-pentanedioic acid
-
less potent than the S-isomer, IC50: 0.000030 mM
0.000017
(S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid
-
-
0.000014
(S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid
-
-
0.00000006
(S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid
-
-
0.0000005
(S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid
-
-
0.000245
(S)-2-(3-((S)-1-carboxy-5-(2-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
0.000037
(S)-2-(3-((S)-1-carboxy-5-(2-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
0.000002
(S)-2-(3-((S)-1-carboxy-5-(3-(4-bromophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
0.000004
(S)-2-(3-((S)-1-carboxy-5-(3-(4-chlorophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
0.000003
(S)-2-(3-((S)-1-carboxy-5-(3-(4-fluorophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
0.00001
(S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
0.000277
(S)-2-(3-((S)-1-carboxy-5-(3-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
0.000443
(S)-2-(3-((S)-1-carboxy-5-(3-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
0.000012
(S)-2-(3-((S)-1-carboxy-5-(3-phenylureido)pentyl)ureido)pentanedioic acid
-
-
0.000043
(S)-2-(3-((S)-1-carboxy-5-(4-bromobenzylamino)pentyl)ureido)pentanedioic acid
-
-
0.000002
(S)-2-(3-((S)-1-carboxy-5-(4-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
0.0012
(S)-2-(3-((S)-1-carboxy-5-(4-fluorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
0.000022
(S)-2-(3-((S)-1-carboxy-5-(4-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
0.00001
(S)-2-(3-((S)-1-carboxy-5-(4-iodophenylsulfonamido)pentyl)-ureido)pentanedioic acid
-
-
0.000154
(S)-2-(3-((S)-1-carboxy-5-(naphthalen-1-ylmethylamino)pentyl)-ureido)pentanedioic acid
-
-
0.00296
(S)-2-(3-((S)-5-(benzylamino)-1-carboxypentyl)ureido)pentanedioic acid
-
-
0.000498
(S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido)pentanedioic acid
-
-
0.003
(S)-2-(3-(4-iodobenzyl)ureido)pentanedioic acid
-
-
0.000034
(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
-
40fold more potent than the R-isomer, IC50: 0.000034 mM
0.0000001
(S)-2-(phosphonomethyl)-pentanedioic acid
-
more potent than the R-isomer, IC50: 0.0000001 mM
0.000029
(t-Bu)Cys-PSI[C-O]-Glu
-
IC50: 29 nM
0.0017
2-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 1700 nM
0.0022
2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid
-
IC50: 2200 nM
0.015
2-(3-carboxybenyl)succinic acid
-
IC50: 0.015 mM
0.0018
2-(3-cyanobenzyl)-5-mercaptopentanoic acid
-
IC50: 1800 nM
0.000508
2-(3-hydroxybenzyl)-3-phosphonopropanoic acid
-
IC50: 508 nM
0.00009
2-(3-mercaptopropyl)-pentanedioic acid
-
i.e. 2-MPPA, IC50: 90 nM
0.00009
2-(3-mercaptopropyl)pentanedioic acid
-
IC50: 90 nM. Orally bioavailable in rats
0.000175
2-(phosphonomethyl)-4-(5H-tetrazol-5-yl)butanoic acid
-
IC50: 175 nM
0.00000674
2-(phosphonomethyl)-pentanedioic acid
Q9CZR2
2-PMPA, GCPIII IC50: 94 nM, GCPII IC50: 6.74 nM
0.000094
2-(phosphonomethyl)-pentanedioic acid
Q9CZR2
2-PMPA, GCPIII IC50: 94 nM, GCPII IC50: 6.74 nM
0.000185
2-(phosphonomethyl)hexanedioic acid
-
IC50: 185 nM
0.000185
2-(phosphonomethyl)hexanoic acid
-
IC50: 185 nM
0.0000003
2-(phosphonomethyl)pentanedioic acid
-
IC50: 0.3 nM
0.0000004
2-(phosphonomethyl)pentanedioic acid
-
-
0.0000051
2-(phosphonomethyl)pentanedioic acid
-
IC50: 5.1 nM
0.0022
2-(phosphonomethyl)succinic acid
-
IC50: 2200 nM
0.000055
2-([hydroxy[3-(trifluoromethyl)benzyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 55 nM
0.000055
2-([hydroxy[hydroxy(phenyl)methyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 55 nM
0.00001
2-([hydroxy[hydroxy(pyridin-4-yl)methyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 10 nM
0.000548
2-benzyl-3-phosphonopropanoic acid
-
IC50: 548 nM
0.0014
2-benzyl-5-mercaptopentanoic acid
-
IC50: 1400 nM
0.000003
2-[(hydroxy[[(4-methoxyphenyl)amino]methyl]phosphoryl)methyl]pentanedioic acid
-
IC50: 3 nM
0.0000005
2-[[(2,4-dicarboxybutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 0.5 nM
0.000002
2-[[(2-carboxy-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 2 nM
0.000002
2-[[(2-carboxy-4-phenylbutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 2 nM
0.000001
2-[[(2-carboxyethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 1 nM
0.0000015
2-[[(2-carboxypropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 1.5 nM
0.000156
2-[[(2-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 156 nM
0.000049
2-[[(3,5-difluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 49 nM
0.000143
2-[[(3-aminobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 143 nM
0.00007
2-[[(3-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 70 nM
0.000064
2-[[(4-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 64 nM
0.000004
2-[[(anilinomethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 4 nM
0.000053
2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 53 nM
0.00007
2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 70 nM
0.000149
2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 149 nM
0.00015
2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 150 nM
0.000059
2-[[hydroxy(3-nitrobenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50 59 nM
0.00023
2-[[hydroxy(3-phenylpropyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 230 nM
0.00009
2-[[hydroxy(4-methoxybenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 90 nM
0.000068
2-[[hydroxy(4-methylbenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 68 nM
0.000082
2-[[hydroxy(pentafluorobenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 82 nM. Significantly prevents neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In the chronic constrictive model of neuropathic pain, the inhibitor sifnificantly attenuats the hypersensitivity observed with saline-
0.00293
2-[[hydroxy(phenyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 2930 nM
0.00036
2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 360 nM
0.00056
2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 560 nM
0.000016
2-[[[(3-fluorophenyl)(hydroxy)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 16 nM
0.000059
2-[[[(benzylamino)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 59 nM
0.000055
2-[[[3,5-bis(trifluoromethyl)benzyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 55 nM
0.000095
2-[[[3-(benzyloxy)-2-methyl-3-oxopropyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 95 nM
0.000003
2-{[2-Carboxy-3-(4-methoxy-phenylamino)-propyl]-hydroxy-phosphinoylmethyl}-pentanedioic acid
-
IC50: 3 nM
0.000014
3-(1-carboxy-4-mercaptobutoxy)benzoic acid
-
IC50: 14 nM
0.00064
3-(2-carbamoyl-5-mercaptopentyl)benzoic acid
-
IC50: 640 nM
0.015
3-(2-carboxy-3-hydroxycarbamoylpropyl)benzoic acid
-
IC50: 0.015 mM
0.00012
3-(2-carboxy-3-phosphonopropyl)benzoic acid
-
IC50: 120 nM
0.000015
3-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 15 nM
0.0027
3-(2-carboxy-5-mercaptopentyl)benzoic acid methyl ester
-
IC50: 2700 nM
0.02
3-(2-carboxy-5-mercaptosulfanylpentyl)benzoic acid
-
IC50: 0.02 mM
0.02
3-(2-carboxy-5-tritylsulfanylpentyl)benzoic acid
-
IC50: 0.02 mM
0.00073
3-(5-mercapto-2-methoxycarbonylpentyl)benzoic acid
-
IC50: 730 nM
0.000032
3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid
-
IC50: 32 nM
0.0024
3-[2-carboxy-3-(hydroxypentafluorophenylmethylphosphinoyl)propyl]benzoic acid
-
IC50: 2400 nM
0.000063
4-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 63 nM
0.000508
4-(3-hydroxyphenyl)-2-(phosphonomethyl)butanoic acid
-
IC50: 508 nM
0.000335
4-cyano-2-(phosphonomethyl)butanoic acid
-
IC50: 335 nM
0.000199
4-phenyl-2-(phosphonomethyl)butanoic acid
-
IC50: 199 nM
0.0461
Asp-PSI[C-O-S]-Glu
-
IC50: 0.0461 mM
0.0038
Asp-PSI[C-O]-Asp
-
IC50: 0.0038 mM
0.0000069
Cys-PSI[C-O-S]-Glu
-
IC50: 6.9 nM
0.000002
diphenyl 2-[[[2-[4-([[7-(diethylamino)-2-oxo-2H-chromen-3-yl]carbamoyl]amino)phenyl]ethoxy](hydroxy)phosphoryl]methyl]pentanedioate
-
-
0.000047
Glu-PSI[C-O]-Glu
-
IC50: 47 nM
0.000007
N-(tert-butoxycarbonyl)glycyl-N-[4-[2-([[(2S)-2,4-dicarboxybutyl](hydroxy)phosphoryl]oxy)ethyl]phenyl]-L-prolinamide
-
-
0.000008
N-(tert-butoxycarbonyl)glycylglycyl-N-[4-[2-([[(2S)-2,4-dicarboxybutyl](hydroxy)phosphoryl]oxy)ethyl]phenyl]glycinamide
-
-
0.000102
pyropheophorbide-a conjugate
-
pH 7.4, 37C
0.000014
S-2-((2-(S-4-(4-18F-fluorobenzamido)-4-carboxybutanamido)-S-2-carboxyethoxy)hydroxyphosphorylamino)-pentanedioic acid
-
-
0.00000068
S-2-((2-(S-4-amino-4-carboxybutanamido)-S-2-carboxyethoxy)-hydroxyphosphorylamino)-pentanedioic acid
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.000000054 - 0.000000148
-
-
0.0000036
-
-
additional information
-
assay method
additional information
-
-
additional information
Q9CZR2
-
additional information
-
activity in prostate tissue homogenate in comparison to other species, overview
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5
-
second optimum at pH 8
7.4
-
assay at
7.4
-
activity assay
7.5
Q9CZR2
assay at
7.7
-
assay at, recombinant enzyme
8
-
second optimum at pH 5
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6 - 7.4
-
more than 50% of maximal activity in this range
additional information
Q9CZR2
pH profile
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
-
assay at
37
-
assay at
37
Q9CZR2
assay at
37
-
in vivo assay at
37
-
activity assay
37
-
assay at, recombinant enzyme
37
-
assay at
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
25 - 80
-
more than 50% of maximal activity in this range
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
regional distribution
Manually annotated by BRENDA team
-
highest in cerebellum, lowest in telencephalic structures
Manually annotated by BRENDA team
-
amygdala, caudate-putamen, central gray, dorsal raphe, globus pallidus, hippocampus, hypothalamus, locus coerulus, medial and lateral geniculate, olfactory bulb, periaqueductal gray, solitary nucleus, spinal trigeminal nucleus, substantia nigra, superior colliculus, thalamus, corpus callosum, fornix, habenular commissure, solitary tract, stria medularis, stria therminalis
Manually annotated by BRENDA team
-
decreased gene expression and activity in the frontal and temporal lobe, the dorsolateral prefrontal cortex, and the hippocampus in schizophrenia, overview, no intracellular activity in pyramidal cells and their dendrites
Manually annotated by BRENDA team
-
especially midbrain and cerebellum, quantitative detection of GCPII content in the brain by labeling with [125I]-N-[N-((S)-1,3-dicarboxypropyl)carbamoyl]-S-3-iodo-L-tyrosine is a potent antagonist of the enzyme activity
Manually annotated by BRENDA team
Q9CZR2
GCPII
Manually annotated by BRENDA team
Mus musculus C57/Bl
-
-
-
Manually annotated by BRENDA team
-
quantitative expression analysis
Manually annotated by BRENDA team
-
prostate cancer cell line
Manually annotated by BRENDA team
-
glomeruli in the cerebellum
Manually annotated by BRENDA team
-
cortical cells dissociated in cell culture
Manually annotated by BRENDA team
-
ventricular, lumbar, and subarachnoid
Manually annotated by BRENDA team
-
cerebral ischemia cell culture model
Manually annotated by BRENDA team
-
low expression level
Manually annotated by BRENDA team
-
very low enzyme expression level
Manually annotated by BRENDA team
-
prostate gland
Manually annotated by BRENDA team
-
dorsal root ganglia
Manually annotated by BRENDA team
-
PSMA is expressed in the neovasculature of multiple nonprostatic solid tumors, it shows a unique expression pattern limited to tumor-associated endothelial cells. Expression in liver metastasis from colorectal cancers and lymph node metastasis from colorectal cancers
Manually annotated by BRENDA team
Q9CZR2
GCPII, not GCPIII
Manually annotated by BRENDA team
-
CA3 region, dorsal
Manually annotated by BRENDA team
-
hippocampus-stratum lucidum
Manually annotated by BRENDA team
-
kidney cortex, specifically in the brush border of proximal convoluted tubules
Manually annotated by BRENDA team
-
prostate cancer cell line
Manually annotated by BRENDA team
-
quantitative expression analysis
Manually annotated by BRENDA team
-
originating from a prostate cancer lymph node metastasis
Manually annotated by BRENDA team
-
lymph node metastasis prostate cancer cells
Manually annotated by BRENDA team
-
subline C4-2
Manually annotated by BRENDA team
Q9CZR2
GCPIII
Manually annotated by BRENDA team
-
CA3 pyramidal neuron
Manually annotated by BRENDA team
Q9CZR2
GCPIII
Manually annotated by BRENDA team
-
very low enzyme expression level
Manually annotated by BRENDA team
-
epithelial cells
Manually annotated by BRENDA team
-
high enzyme expression level
Manually annotated by BRENDA team
-
overexpression of the enzyme in prostate cancer
Manually annotated by BRENDA team
-
prostate-specific membrane antigen, PSMA
Manually annotated by BRENDA team
-
high PSMA expression level, overexpression in advanced stage prostate adenocarcinomas. PSMA expression analysis and distribution pattern of PSMA in primary and metastatic tumors, immunohistochemic detection, overview
Manually annotated by BRENDA team
-
highly up-regulated PSMA
Manually annotated by BRENDA team
-
PSMA is a transmembrane protein commonly found on the surface of late-stage and metastatic prostate cancer
Manually annotated by BRENDA team
-
overexpression of PMSA
Manually annotated by BRENDA team
-
prostrate carcinoma cell line LNCaP
Manually annotated by BRENDA team
-
epithelial cells
Manually annotated by BRENDA team
-
prostate form of the enzyme is termed prostate-specific membrane antigen
Manually annotated by BRENDA team
-
prostate-specific membrane antigen, PSMA
Manually annotated by BRENDA team
-
prostatic adenocarcinoma and intraepithelial neoplasia
Manually annotated by BRENDA team
-
lymph node metastasis, PSMA is highly expressed in 100% of the lymph node metastases originating from prostate cancer
Manually annotated by BRENDA team
-
expressed during late embryonal and early postnatal development. During the first prenatal week the enzyme is downregulated in myelinating Schwann cells while the total enzyme concentrations in the nerves are transiently increased
Manually annotated by BRENDA team
-
higher level in patients with prostrate cancer, lower levels in healthy male donors
Manually annotated by BRENDA team
-
membrane brush border
Manually annotated by BRENDA team
Q9CZR2
GCPIII
Manually annotated by BRENDA team
additional information
-
analysis of enzyme expression in prostate tissue during carcinoma development
Manually annotated by BRENDA team
additional information
Q9CZR2
tissue distribution of GCPIII activity and expression, overview
Manually annotated by BRENDA team
additional information
-
no activity in PC-3 cells
Manually annotated by BRENDA team
additional information
-
no activity in the PSMA-negative prostate cancer cell line DU 145
Manually annotated by BRENDA team
additional information
-
PC-3 cells are PSMA-negative
Manually annotated by BRENDA team
additional information
-
PC-3 cells lack PSMA
Manually annotated by BRENDA team
additional information
-
PSMA expression analysis, overview
Manually annotated by BRENDA team
additional information
-
quantitative PSMA expression analysis in cancer cell lines and tissues, overview
Manually annotated by BRENDA team
additional information
-
quantitative PSMA expression analysis in cancer cells, overview
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
intestinal brush border membrane
Manually annotated by BRENDA team
-
of glia and nonmyelinating Schwann cells
Manually annotated by BRENDA team
-
PSMA is a transmembrane protein commonly found on the surface of late-stage and metastatic prostate cancer
Manually annotated by BRENDA team
-
present in neurophil cytoplasm, absent from neuronal cytoplasm
Manually annotated by BRENDA team
-
extracellular site of Schwann cell membrane
Manually annotated by BRENDA team
-
inner face of plasma membrane
Manually annotated by BRENDA team
-
synaptic plasma membranes
Manually annotated by BRENDA team
-
type II membrane protein
Manually annotated by BRENDA team
-
type II transmembrane protein
Manually annotated by BRENDA team
-
the enzyme is associated with the cell surface membrane. The recombinant enzyme and the mutant enzyme omitting the transmembrane domain is associated with the cell surface membrane, the recombinantly expressed extracellular domain has a cytosolic localization
Manually annotated by BRENDA team
-
type II membrane glycoprotein
Manually annotated by BRENDA team
-
type II transmembrane glycoprotein
Manually annotated by BRENDA team
-
PSMA is a transmembrane glycoprotein
Manually annotated by BRENDA team
-
PSMA is a transmembrane protein commonly found on the surface of late-stage and metastatic prostate cancer
Manually annotated by BRENDA team
-
PSMA is a type II membrane protein
Manually annotated by BRENDA team
-
PSMA is a type II transmembrane glycoprotein
Manually annotated by BRENDA team
-
PSMA is a type II transmembrane metallopeptidase
Manually annotated by BRENDA team
-
PSMA is a type II transmembrane protein
Manually annotated by BRENDA team
Mus musculus C57/Bl
-
-
-
Manually annotated by BRENDA team
-
direct targeting of the enzyme to the apical plasma membrane, correct sorting into appropriate post-Golgi vesicles depends on the N-glycosylation of the enzyme, integrity of the microtubule skeleton is required for enzyme localization in the apical plasma membrane
Manually annotated by BRENDA team
-
the enzyme is a type II membrane glycoprotein with an intracellular segment, a transmembrane domain, and an extensive extracellular domain
Manually annotated by BRENDA team
-
type II transmembrane glycoprotein
Manually annotated by BRENDA team
-
synaptoneurosome
-
Manually annotated by BRENDA team
additional information
-
Vinca alkaloids destabilize the microtubules leading to basolateral expression of the enzyme and its integration into the basolateral membrane
-
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
84000
-
calculation from sequence of cDNA, short intracellular domain, single transmembrane element, large glubular extracellular domain
137218
84490
-
sequence of cDNA, nonglycosylated enzyme form, the extracellular domain contains nine potential N- glycosylation sites
137215
85000
-
determined by SDS-PAGE and Western Blot analysis
698502
100000
-
determined by SDS-PAGE and Western Blot analysis
701258
100000
-
about
708256
additional information
-
domain structure, sequence alignment with transferrin receptor, the catalytic domain can be assigned to the peptidase family M28
137211
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 97000, SDS-PAGE
?
-
x * 94000, SDS-PAGE
?
-
x * 110000-120000, SDS-PAGE
dimer
-
homodimer, the enzyme folds into three domains: a protease-like, an apical, and a C-terminal domain which are all involved in substrate binding, three-dimensional structure analysis, crystal structure
additional information
-
the enzyme is a is monomeric or dimeric type II membrane glycoprotein with an intracellular segment, a transmembrane domain, and an extensive extracellular domain
additional information
-
the enzyme is a type II membrane glycoprotein with an intracellular segment, a transmembrane domain, and an extensive extracellular domain
additional information
-
the enzyme is monomeric or dimeric a type II membrane glycoprotein with an intracellular segment of amino acid residues 1-18, a transmembrane domain of residues 19-43, and an extensive extracellular domain comprising residues 44-750
additional information
-
the enzyme posseses an extracellular domain, a transmembrane segment, and a cytoplasmic tail
additional information
-
overall fold and quaternary arrangement of the GCPIII molecule, overview
additional information
-
the PSMA protein has intracellular, transmembrane and extracellular domains
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
-
-
glycoprotein
-
type II transmembrane glycoprotein
glycoprotein
-
10 possible N-glycosylation sites
glycoprotein
-
identification of the N-glycosylation sites, e.g. N121, N153, N195, N638, and N140, the enzyme is heavily glycosylated
glycoprotein
-
N-glycosylation, correct sorting into appropriate post-Golgi vesicles for targeting into the apical plasma membrane depends on the N-glycosylation of the enzyme, inhibition of N-glycosylation abolishes the polarized enzyme expression, overview
glycoprotein
-
the enzyme is a type II membrane glycoprotein
glycoprotein
-
type II membrane glycoprotein
glycoprotein
-
type II transmembrane glycoprotein, N- and O-glycosylation, mannose-rich glycosylation renders the enzyme trypsin-insensitive, which is typical for Golgi-located enzyme, overview
glycoprotein
-
PSMA is a transmembrane glycoprotein
glycoprotein
-
PSMA is a type II transmembrane glycoprotein
glycoprotein
-
the enzyme is a type II membrane glycoprotein
glycoprotein
-
the extracellular domain contains nine potential glycosylation sites
glycoprotein
-
the enzyme is a type II membrane glycoprotein
glycoprotein
-
type II membrane glycoprotein
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
GCPIII ectodomain in a pseudo-unliganded state and in a complex with product L-glutamate, or the phosphapeptide transition state mimetic (2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid, or quisqualic acid, a glutamate biostere, X-ray diffraction structure determination and analysis at 1.29-1.56 A resolution, modelling
-
prostate-specific membrane antigen crystal structure analysis
-
purified recombinant extracellular portion of the enzyme, comprising residues 44-750, in complex with GPI-18431, a iodobenzyl derivative of inhibitor 2-PMPA, hanging drop vapour diffusion method, room temperature, 0.002 ml protein solution, containing 0.2 mM GPI-18431, is mixed with 0.002 ml well solution containing 20 mM HEPES, pH 7.5, 0.2 M NaCl, 5% w/v PEG 400, and 15%w/v PEG 1500, 1-2 weeks, X-ray diffraction structure determination and analysis at 2.2 A resolution
-
purified recombinant His6-tagged extracellular portion, which contains bound Zn2+, hanging drop vapour diffusion method, 0.0008 ml of 10 mg/ml protein in 20 mM Tris, pH 7.5, is mixed with an equal volume of reservoir solution containing 18% PEG 3350, 0.2 M sodium thiocyanate, 4C, cryoprotection by 20% glycerol, X-ray diffrcation structure determination and analysis at 3.5 A resolution
-
the crystal structure of GCPII(E424A) in complex with N-acetyl-L-aspartyl-L-glutamate is determined at 1.70 A resolution
-
the structures of human GCPII in complex with (S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid, (S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid, (S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid and (S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid are solved to a resolution of 1.75, 1.54, 1.69 and 1.55 A, respectively
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
FLAG affinity chromatography, full-length enzyme and mutant enzymes DELTA1-42 and DELTA20-42
-
native enzyme from LNCaP cells by conformational epitope-specific antibody-affinity chromatography in presence of Zn2+ in a native and active conformation
-
partially by membrane preparation
-
purification consists of four steps, QAE-Sephadex A50 batch chromatography, chromatography on a Source 15S column, affinity chromatography using lentil lectin Sepharose, and gel filtration on a Superdex 200 column
-
recombinant enzyme from CHO cells partially by membrane preparation
-
recombinant His6-tagged extracellular portion of the enzyme from High5 by nickel affinity chromatography and gel filtration
-
membrane fractions are prepared using mouse brain tissue samples
-
partially by membrane preparation
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cloning and expression of the His6-tagged extracellular portion of the enzyme in High5 cells using the baculovirus transfection system, secretion of the glycosylated extracellular domain
-
construction of the DNA vaccines carrying truncated human tPSMA gene driven by the cytomegalovirus promoter and mouse 4-1BBL gene driven by an IRES
-
expression in CHO cells
-
expression in COS-1 cells, mannose-rich glycosylation of the recombinant enzyme in absence of an inhibitor, recombinant glycosylation and subcellular transport analysis, overview, stable expression in MDCK cells at the cell surface
-
expression in DU145 cell line
-
expression of the full-length enzyme and the mutant enzymes DEALTA20-42 and DELTA1-42 in HEK293 cells
-
expression of wild-type and mutant enzymes in PC3 cells
-
for expression in Drosophila Schneiders S2 cells
-
gene FOLH1, DNA sequence variants analysis, expression regulation by PMSA enhancer, PSME, involving Ca2+, overview, localization on chromosome 11p11-12, another highly homologous gene is located at 11q14.3 and is expressed in several tissues, e.g. kidney and liver, but not in prostate
-
genetic structure, overview
-
stable expression in MDCK cells of truncated PMSA-DELTA103-750 as GFP-fusion protein and of the extracellular domain
-
stable expression of wild-type and mutant enzymes in S2 cells, secretion of the enzyme, which is prevented by blocking the N-glycosylation
-
the extracellular part, amino acids 44-750, of human GCPII is cloned and heterologously overexpressed in Drosophila Schneiders S2 cells
-
a 20.7 kb gene fragment encoding exons 1-3 is subcloned and analyzed by restriction mapping
-
gene Naalad2, DNA and amino acid sequence determination and analysis, expression of GCPIII in CHO cells
Q9CZR2
gene PMSA, DNA sequence variants analysis, expression regulation by PMSA enhancer, PSME, involving Ca2+, overview
-
recombinant expression
-
the gene is homologuos to the prostrate-specific membrane antigen
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
inhibition of LNCaP cell growth by mono- and bispecific antisense oligonucleotides directed against bcl-2 and epidermal growth factor receptor, EGFR, inhibition of expression of non-targeted proteins prostate-specific membrane antigen only by bcl-2-monospecific oligos, overview
-
Lentivirus-mediated RNAi inhibits PSMA mRNA and protein expression in LNCaP and DU-145 cells, PSMA RNAi induces the changes of cell cycle, overview
-
docetaxel down-regulates the expression of androgen receptor and prostate-specific antigen but not prostate-specific membrane antigen in prostate cancer cell lines
-
androgen ablation can up-regulate PSMA expression
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
DELTA1-42
-
the recombinantly expressed extracellular domain has a cytosolic localization compared to sell surface membrane localization of the full-length enzyme. Less than 5% of the activity of the wild-type enzyme
DELTA20-42
-
mutant enzyme omitting the transmembrane domain is associated with the cell surface membrane as is the full-length enzyme. Less than 5% of the activity of the wild-type enzyme
E424A
-
mutant, complete loss of catalytic activity
H380G
-
site-directed mutagenesis, active site mutant, inactive mutant
H475Y
-
C1561T single nucleotide polymorphism located in the putative catalytic region of the enzyme
N121A
-
site-directed mutagenesis of an N-glycosylation site, nearly inactive enzyme
N140A
-
site-directed mutagenesis of an N-glycosylation site, nearly inactive enzyme
N153A
-
site-directed mutagenesis of an N-glycosylation site, nearly inactive enzyme
N195A
-
site-directed mutagenesis of an N-glycosylation site, nearly inactive enzyme
N336A
-
site-directed mutagenesis of an N-glycosylation site leads to 45% reduced activity compared to the wild-type enzyme
N336A
-
site-directed mutagenesis, glycosylation site E mutant, inactive mutant, no endocytic internalization
N459A
-
site-directed mutagenesis, glycosylation site E mutant, inactive mutant, no endocytic internalization
N476A
-
site-directed mutagenesis of an N-glycosylation site leads to 70% reduced activity compared to the wild-type enzyme
N476A
-
site-directed mutagenesis, glycosylation site E mutant, inactive mutant, no iendocytic nternalization
N51A
-
site-directed mutagenesis of an N-glycosylation site leads to 75% reduced activity compared to the wild-type enzyme
N638A
-
site-directed mutagenesis of an N-glycosylation site, nearly inactive enzyme
N638A
-
site-directed mutagenesis, glycosylation site F mutant, inactive mutant
N76A
-
site-directed mutagenesis of an N-glycosylation site leads to 25% reduced activity compared to the wild-type enzyme
L4A/L5A
-
site-directed mutagenesis, internalization motif mutant, active mutant, no endocytic internalization
additional information
-
antitumor immune respone in female C57BL/6 (H-2kb) mice to DNA vaccine and efficiency of truncated human prostate-specific membrane antigen can be can be enhanced by a genetically enhanced adjuvant 4-1BB ligand [4-1BBL] from mouse, overview
additional information
-
downregulation of prostate-specific membrane antigen expression by lentivirus-mediated RNA interference significantly suppresses the growth rates of LNCaP and DU-145 cells. The specific down-regulation arrests cells in G0/G1 phase of cell cycle
additional information
-
highly efficient capture and enumeration of low abundance prostate cancer cells using prostate-specific membrane antigen aptamers immobilized to a polymeric microfluidic device, method development and evaluation, overview. PSMA can be used as a marker to select these cells from highly heterogeneous clinical samples, selective isolation of rare circulating prostate tumor cells resident in a peripheral blood matrix, overview
additional information
-
in vivo detection of PSMA-positive tumors in mice by labeled monoclonal antibodies, method development and evaaluation, overview
additional information
-
synthesis of a series of PSMA-targeted 99mTc-chelate complexes for imaging PSMA-expressing human prostate cancer cells, in silico docking studies using the crystal structure of PSMA, overview. Synthesis of core ligand 2-[3-(3-benzyloxycarbonyl-1-tert-butoxycarbonyl-propyl)-ureido]pentanedioic acid di-tert-butyl ester and deprotected core ligand 2-[3-(1,3-bis-tert-butoxycarbonyl-propyl)-ureido]pentanedioic acid 1-tert-butyl ester
additional information
-
synthesis of a series of PSMA-targeted 99mTc-chelate complexes for imaging PSMA-expressing human prostate cancer cells, in silico docking studies using the crystal structure of PSMA, overview. The method offers a potential for use in localizing prostate cancer masses, monitoring response to therapy, detecting prostate cancer recurrence following surgery, and selecting patients for subsequent PSMA-targeted chemotherapy. Molecular dynamics, overview
additional information
-
the PSMA splice variant of the protein remains intracellular without extracellular domain
additional information
-
usage of the ectodomain of PSMA as target for a retargeted measles virus, that harbors a single-chain antibody specific for the extracellular domain of PSMA (J591) inserted as a C-terminal extension on its viral attachment protein. Live attenuated vaccine strain of measles virus has promising antitumor activity. Fully retargetedMVthat infects cells exclusively through the PSMA receptor, which is overexpressed on prostate cancer cells and tumor neovasculature, method, overview. Stable transfection of LNCaP cells. The construct leads to tumor regression
T640A
-
site-directed mutagenesis of an N-glycosylation site, nearly inactive enzyme
additional information
Q9CZR2
GCPII knockout mutant mice do not show an altered phenotype
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
-
synthesis of a series of PSMA-targeted 99mTc-chelate complexes, with core ligand 2-[3-(3-benzyloxycarbonyl-1-tert-butoxycarbonyl-propyl)-ureido]pentanedioic acid di-tert-butyl ester, for imaging PSMA-expressing human prostate cancer cells, in silico docking studies using the crystal structure of PSMA, overview. The method offers a potential for use in localizing prostate cancer masses, monitoring response to therapy, detecting prostate cancer recurrence following surgery, and selecting patients for subsequent PSMAtargeted chemotherapy
diagnostics
-
prostate-specific membrane antigen is a tumor marker
diagnostics
-
the enzyme, prostate-specific membrane antigen, is a good marker for prostate cancer
diagnostics
-
PSMA is a biomarker for prostate cancer
diagnostics
-
PSMA is a validated molecular marker for prostate cancer
diagnostics
-
PSMA is a well-known imaging biomarker for staging and monitoring therapy, assessment of an 18F-labeled phosphoramidate peptidomimetic as a PSMA-targeted imaging agent for prostate cancer
diagnostics
-
PSMA is an established enzyme-biomarker for prostate cancer
diagnostics
-
PSMA is used in cancer diagnosis
diagnostics
-
PSMA overexpression in prostate cancer patients is related to a worse prognosis
drug development
-
PSMA is a target for drug design
medicine
-
detection of cancerous cells in prostrate or blood, target for diagnostic and therapeutic strategies in prostrate cancer, immunotherapy, antibody therapy
medicine
-
the enzyme is an important marker in the diagnosis of prostate cancer
medicine
-
glutamate carboxypeptidase II is a therapeutic target for neurodegeneration and prostate cancer
medicine
-
glutamate carboxypeptidase II may represent a viable therapeutic target for intervention on psychiatric disease
medicine
-
maternal total homocysteine concentration is affected by C1561T polymorphism, maternal GCPII C1561T variant is associated with neonatal methylmalonic acid concentration
medicine
-
urea-based, low molecular weight ligands of glutamate carboxypeptidase II have demonstrated efficacy in various models of neurological disorders and can serve as imaging agents for prostate cancer
pharmacology
-
enzyme inhibitors are used in therapy of neruological disorders, overview
pharmacology
-
the enzyme is a drug target in neuronal damage and prostate cancer
pharmacology
-
the enzyme is a target for specific inhibitor design in therapy of neurodegenerative disorders, overview
pharmacology
-
the enzyme NAALADase is a target for drug treatment in neuropathic pain
pharmacology
-
effects of PSMA-targeted photodynamic therapy on cytoskeletal networks in prostate cancer cells
pharmacology
-
PSMA is a target for imaging and therapeutic applications for prostate cancer
pharmacology
-
usage of the ectodomain of PSMA as target for a retargeted measles virus, that harbors a single-chain antibody specific for the extracellular domain of PSMA (J591) inserted as a C-terminal extension on its viral attachment protein. Live attenuated vaccine strain of measles virus has promising antitumor activity. Fully retargeted MV that infects cells exclusively through the PSMA receptor, which is overexpressed on prostate cancer cells and tumor neovasculature, method, overview. The construct leads to tumor regression
medicine
-
design of inhibitors may lead to effective neuroprotective agents, possibility to employ GCPII inhibitors in stroke therapy
medicine
-
GCPII inhibitors are attractive candidates for clinical treatment trials in amylotrophic lateral sclerosis
medicine
-
inhibitors of NAADLADase protect against chronic glutamate-mediated motor neuron degeneration and may prove therapeutic towards amyotrophic lateral sclerosis
medicine
-
NAALADase inhibition may provide a new aproach for the treatment of both neurodegenerative disorders and peripheral neuropathies
medicine
-
for establishing new strategies to treat peripheral neuropathies