Page last updated: 2024-08-07 13:30:08
Glutamate carboxypeptidase 2
A glutamate carboxypeptidase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q04609]
Synonyms
EC 3.4.17.21;
Cell growth-inhibiting gene 27 protein;
Folate hydrolase 1;
Folylpoly-gamma-glutamate carboxypeptidase;
FGCP;
Glutamate carboxypeptidase II;
GCPII;
Membrane glutamate carboxypeptidase;
mGCP;
N-acetylated-
Research
Bioassay Publications (22)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (31.82) | 29.6817 |
| 2010's | 11 (50.00) | 24.3611 |
| 2020's | 4 (18.18) | 2.80 |
Compounds (13)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| isospaglumic acid | Homo sapiens (human) | Km | 11.0250 | 4 | 4 |
Novel substrate-based inhibitors of human glutamate carboxypeptidase II with enhanced lipophilicity.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
PSMA-targeted small-molecule docetaxel conjugate: Synthesis and preclinical evaluation.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Preparation and Evaluation of Radiolabeled Antibody Recruiting Small Molecules That Target Prostate-Specific Membrane Antigen for Combined Radiotherapy and Immunotherapy.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
Preparation of asymmetric urea derivatives that target prostate-specific membrane antigen for SPECT imaging.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:12, 2012
Multivalent scaffolds for affinity maturation of small molecule cell surface binders and their application to prostate tumor targeting.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
Enantiospecificity of glutamate carboxypeptidase II inhibition.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 13, Issue:13, 2003
δ-Thiolactones as prodrugs of thiol-based glutamate carboxypeptidase II (GCPII) inhibitors.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Design, synthesis, and pharmacological evaluation of glutamate carboxypeptidase II (GCPII) inhibitors based on thioalkylbenzoic acid scaffolds.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:12, 2012
The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
Enantiospecificity of glutamate carboxypeptidase II inhibition.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 13, Issue:13, 2003
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 27, Issue:2, 2019
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
Novel substrate-based inhibitors of human glutamate carboxypeptidase II with enhanced lipophilicity.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| metallocarboxypeptidase activity | molecular function | Catalysis of the hydrolysis of a single C-terminal amino acid residue from a polypeptide chain by a mechanism in which water acts as a nucleophile, one or two metal ions hold the water molecule in place, and charged amino acid side chains are ligands for the metal ions. [https://www.ebi.ac.uk/merops/about/glossary.shtml#CARBOXYPEPTIDASE] |
| peptidase activity | molecular function | Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181] |
| dipeptidase activity | molecular function | Catalysis of the hydrolysis of a dipeptide. [https://www.ebi.ac.uk/merops/about/glossary.shtml#DIPEPTIDASE, PMID:19879002] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| Ac-Asp-Glu binding | molecular function | Binding to Ac-Asp-Glu. [GO_REF:0000067, GOC:BHF, GOC:hal, GOC:TermGenie, PMID:24863754] |
| tetrahydrofolyl-poly(glutamate) polymer binding | molecular function | Binding to tetrahydrofolyl-poly(glutamate) polymer. [GO_REF:0000067, GOC:BHF, GOC:hal, GOC:TermGenie, PMID:24863754] |
| carboxypeptidase activity | molecular function | Catalysis of the hydrolysis of a single C-terminal amino acid residue from a polypeptide chain. [https://www.ebi.ac.uk/merops/about/glossary.shtml#CARBOXYPEPTIDASE] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 3 target(s):
| Target | Category | Definition |
|---|
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| folic acid-containing compound metabolic process | biological process | The chemical reactions and pathways involving a folic acid-containing compound, i.e. any of a group of heterocyclic compounds based on the pteroic acid skeleton conjugated with one or more L-glutamic acid or L-glutamate units. [GOC:ai, GOC:mah] |
| C-terminal protein deglutamylation | biological process | The removal of a C-terminal, gene-encoded glutamate residue from a protein. [GOC:sp, PMID:21074048] |