ArticleBioorganic & medicinal chemistry letters2010
Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies.
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed.
- The Impact of Monosodium Glutamate onJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Trial
- Bimodal Fluorescent Conjugate Based on Prostate-Specific Membrane Antigen Ligands with the Chelating Agent DOTA and SulfoCy5 Dye: Synthesis, Radiolabeling, and Biological Activity.International journal of molecular sciences · 2026Article
- Prodrugs Targeting Prostate-Specific Membrane Antigen against Prostate Cancer.Journal of medicinal chemistry · 2025Review
- Towards a 'clicked' PSMA targeting gene delivery bioconjugate-polyplex for prostate cancer.RSC advances · 2024Article
- Characterization of Non-Specific Uptake and Retention Mechanisms of [Pharmaceuticals (Basel, Switzerland) · 2023Article
- Metamorphosis of prostate specific membrane antigen (PSMA) inhibitors.Biophysical reviews · 2022Review
- Preclinical evaluation and first in human study of AlFrontiers in oncology · 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
- Polypeptide-Based Molecular Platform and Its Docetaxel/Sulfo-Cy5-Containing Conjugate for Targeted Delivery to Prostate Specific Membrane Antigen.Molecules (Basel, Switzerland) · 2020Article
- Image-Guided Surgery: Are We Getting the Most Out of Small-Molecule Prostate-Specific-Membrane-Antigen-Targeted Tracers?Bioconjugate chemistry · 2020Review
- 2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.ACS medicinal chemistry letters · 2018Article
- Clinical implications of PET/CT in prostate cancer management.Translational andrology and urology · 2018Review
- Synthesis and in vitro and in vivo evaluation of urea-based PSMA inhibitors with increased lipophilicity.EJNMMI research · 2018Article
- The use of PET/CT in prostate cancer.Prostate cancer and prostatic diseases · 2018Review
- The New Age of -omics in Urothelial Cancer - Re-wording Its Diagnosis and Treatment.EBioMedicine · 2018Review
- Metal-Based PSMA Radioligands.Molecules (Basel, Switzerland) · 2017Review
- MR-Guided Delivery of Hydrophilic Molecular Imaging Agents Across the Blood-Brain Barrier Through Focused Ultrasound.Molecular imaging and biology · 2017Article
- Occurrence of urea-based soluble epoxide hydrolase inhibitors from the plants in the order Brassicales.PloS one · 2017Article
- The therapeutic and diagnostic potential of the prostate specific membrane antigen/glutamate carboxypeptidase II (PSMA/GCPII) in cancer and neurological disease.British journal of pharmacology · 2016Review
- Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
We report a strategy based on bioisosterism to improve the physicochemical properties of existing hydrophilic, urea-based GCPII inhibitors. Comprehensive structure-activity relationship studies of the P1' site of ZJ-43- and DCIBzL-based compounds identified several glutamate-free inhibitors with K(i) values below 20nM. Among them, compound 32d (K(i)=11nM) exhibited selective uptake in GCPII-expressing tumors by SPECT-CT imaging in mice. A novel conformational change of amino acids in the S1' pharmacophore pocket was observed in the X-ray crystal structure of GCPII complexed with 32d.
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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.