ArticleFEBS open bio2017
Mouse glutamate carboxypeptidase II (GCPII) has a similar enzyme activity and inhibition profile but a different tissue distribution to human GCPII.
Article in FEBS open bio, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 26 citations in OpenAlex.
- Effective treatment of human prostate carcinoma xenografts with Single-Dose PSMA-targeted [European journal of nuclear medicine and molecular imaging · 2026Article
- Inflammatory bowel disease and prostate cancer: from epidemiological controversy to mechanistic hypotheses.Frontiers in immunology · 2026Review
- Future Prospect of Low-Molecular-Weight Prostate-Specific Membrane Antigen Radioisotopes Labeled as Theranostic Agents for Metastatic Castration-Resistant Prostate Cancer.Molecules (Basel, Switzerland) · 2024Review
- Searching for Protein Off-Targets of Prostate-Specific Membrane Antigen-Targeting Radioligands in the Salivary Glands.Cancer biotherapy & radiopharmaceuticals · 2024Article
- DNA-encoded chemical libraries enable the discovery of potent PSMA-ligands with substantially reduced affinity towards the GCPIII anti-target.Chemical science · 2024Article
- GCP III is not the "off-target" for urea-based PSMA ligands.European journal of nuclear medicine and molecular imaging · 2023Article
- Predicting the effect of different folate doses on [EJNMMI research · 2023Article
- Characterization of Non-Specific Uptake and Retention Mechanisms of [Pharmaceuticals (Basel, Switzerland) · 2023Article
- The "Ins and Outs" of Prostate Specific Membrane Antigen (PSMA) as Specific Target in Prostate Cancer Therapy.Advances in experimental medicine and biology · 2023Article
- Article
- Evaluation of anScientific reports · 2022Article
- In Silico Predictions of Ecological Plasticity Mediated by Protein Family Expansions in Early-Diverging Fungi.Journal of fungi (Basel, Switzerland) · 2022Article
- Dendrimer-2PMPA Delays Muscle Function Loss and Denervation in a Murine Model of Amyotrophic Lateral Sclerosis.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2022Article
- Design of PSMA ligands with modifications at the inhibitor part: an approach to reduce the salivary gland uptake of radiolabeled PSMA inhibitors?EJNMMI radiopharmacy and chemistry · 2021Article
- PSMA PET Imaging in Glioblastoma: A Preclinical Evaluation and Theranostic Outlook.Frontiers in oncology · 2021Article
- Structural basis of prostate-specific membrane antigen recognition by the A9g RNA aptamer.Nucleic acids research · 2020Article
- A Perspective on the Evolving Story of PSMA Biology, PSMA-Based Imaging, and Endoradiotherapeutic Strategies.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2018Review
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glutamate carboxypeptidase II (GCPII), also known as prostate-specific membrane antigen (PSMA) or folate hydrolase, is a metallopeptidase expressed predominantly in the human brain and prostate. GCPII expression is considerably increased in prostate carcinoma, and the enzyme also participates in glutamate excitotoxicity in the brain. Therefore, GCPII represents an important diagnostic marker of prostate cancer progression and a putative target for the treatment of both prostate cancer and neuronal disorders associated with glutamate excitotoxicity. For the development of novel therapeutics, mouse models are widely used. However, although mouse GCPII activity has been characterized, a detailed comparison of the enzymatic activity and tissue distribution of the mouse and human GCPII orthologs remains lacking. In this study, we prepared extracellular mouse GCPII and compared it with human GCPII. We found that mouse GCPII possesses lower catalytic efficiency but similar substrate specificity compared with the human protein. Using a panel of GCPII inhibitors, we discovered that inhibition constants are generally similar for mouse and human GCPII. Furthermore, we observed highest expression of GCPII protein in the mouse kidney, brain, and salivary glands. Importantly, we did not detect GCPII in the mouse prostate. Our data suggest that the differences in enzymatic activity and inhibition profile are rather small; therefore, mouse GCPII can approximate human GCPII in drug development and testing. On the other hand, significant differences in GCPII tissue expression must be taken into account when developing novel GCPII-based anticancer and therapeutic methods, including targeted anticancer drug delivery systems, and when using mice as a model organism.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.