ArticleJournal of medicinal chemistry2008
Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 74 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
74 citing papers in PubMed, 181 citations in OpenAlex.
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- Biological determinants of PSMA expression, regulation and heterogeneity in prostate cancer.Nature reviews. Urology · 2025Review
- Development of a homotrimeric PSMA radioligand based on the NOTI chelating platform.EJNMMI radiopharmacy and chemistry · 2024Article
- Searching for Protein Off-Targets of Prostate-Specific Membrane Antigen-Targeting Radioligands in the Salivary Glands.Cancer biotherapy & radiopharmaceuticals · 2024Article
- Synthesis and Preclinical Evaluation of a Bispecific PSMA-617/RM2 Heterodimer Targeting Prostate Cancer.ACS medicinal chemistry letters · 2024Article
- Towards a 'clicked' PSMA targeting gene delivery bioconjugate-polyplex for prostate cancer.RSC advances · 2024Article
- Automated radiosynthesis and preclinical evaluation of two new PSMA-617 derivatives radiolabelled via [EJNMMI radiopharmacy and chemistry · 2024Article
- Anticancer activity, DFT study, ADMET prediction, and molecular docking of novel α-sulfamidophosphonates.Molecular diversity · 2024Article
- Recent advances in the development ofAnalytical sciences : the international journal of the Japan Society for Analytical Chemistry · 2024Review
- Structural, Biochemical, and Computational Characterization of Sulfamides as Bimetallic Peptidase Inhibitors.Journal of chemical information and modeling · 2024Article
14 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
Abstract
Urea-based, low molecular weight ligands of glutamate carboxypeptidase II (GCPII) have demonstrated efficacy in various models of neurological disorders and can serve as imaging agents for prostate cancer. To enhance further development of such compounds, we determined X-ray structures of four complexes between human GCPII and urea-based inhibitors at high resolution. All ligands demonstrate an invariant glutarate moiety within the S1' pocket of the enzyme. The ureido linkage between P1 and P1' inhibitor sites interacts with the active-site Zn(1)(2+) ion and the side chains of Tyr552 and His553. Interactions within the S1 pocket are defined primarily by a network of hydrogen bonds between the P1 carboxylate group of the inhibitors and the side chains of Arg534, Arg536, and Asn519. Importantly, we have identified a hydrophobic pocket accessory to the S1 site that can be exploited for structure-based design of novel GCPII inhibitors with increased lipophilicity.
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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.