ArticleJournal of the American Chemical Society2010
A remote arene-binding site on prostate specific membrane antigen revealed by antibody-recruiting small molecules.
Article in Journal of the American Chemical Society, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 73 papers, 2 of them syntheses that pooled it.
What it found
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The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
73 citing papers in PubMed, 2 syntheses or guidelines pooled it.
- Lutetium-177-labelled anti-prostate-specific membrane antigen antibody and ligands for the treatment of metastatic castrate-resistant prostate cancer: a systematic review and meta-analysis.Prostate cancer and prostatic diseases · 2017Pooled it
- Antibody-recruiting molecules: an emerging paradigm for engaging immune function in treating human disease.ACS chemical biology · 2012Pooled it
- In Vitro and In Silico Assessment of Anticancer Activity of Venom-Derived and Biomimetic Neurotransmitter Inhibitor Pentapeptides.Cell biochemistry and biophysics · 2026Article
- Design, Synthesis, and In Vitro Evaluation of a PSMA-Targeted Doxorubicin Conjugate.ChemMedChem · 2026Article
- Engineering NIR Probes to Enhance Affinity and Clinical Workflow Compatibility for Prostate Cancer Imaging.Angewandte Chemie (International ed. in English) · 2026Article
- Preclinical evaluation and first-in-human study ofEuropean journal of nuclear medicine and molecular imaging · 2026Article
- Synthesis of Bispecific Conjugates by ADP-Ribosyl Cyclases.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Engineering NIR probes to enhance affinity and clinical workflow compatibility for prostate cancer imaging.bioRxiv : the preprint server for biology · 2025Article
- [The effect of PSMA PET/CT performed in primary staging on the clinical decision].Magyar onkologia · 2025Article
- Prodrugs Targeting Prostate-Specific Membrane Antigen against Prostate Cancer.Journal of medicinal chemistry · 2025Review
- An Antibody-Recruiting Molecule Enhances Fcγ Receptor-Mediated Uptake and Killing of Mycobacterial Pathogens by Macrophages.ACS infectious diseases · 2025Article
- Structure-Activity Relationships and Biological Insights into PSMA-617 and Its Derivatives with Modified Lipophilic Linker Regions.ACS omega · 2025Article
- In-silico identification of novel inhibitors of human androgen receptors and prostrate-specific membrane antigen: a comprehensive target-based molecular docking, molecular dynamics simulation, and ADME-toxicity studies.In silico pharmacology · 2025Article
- Development of a homotrimeric PSMA radioligand based on the NOTI chelating platform.EJNMMI radiopharmacy and chemistry · 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
- PSMA-targeted radiotheranostics in modern nuclear medicine: then, now, and what of the future?Theranostics · 2024Article
- Offsetting Low-Affinity Carbohydrate Binding with Covalency to Engage Sugar-Specific Proteins for Tumor-Immune Proximity Induction.ACS central science · 2023Article
- Preclinical Evaluation of a PSMA-Targeting Homodimer with an Optimized Linker for Imaging of Prostate Cancer.Molecules (Basel, Switzerland) · 2023Article
- Combination ofJournal of chemical information and modeling · 2023Article
13 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
Prostate specific membrane antigen (PSMA) is a membrane-bound glutamate carboxypeptidase overexpressed in many forms of prostate cancer. Our laboratory has recently disclosed a class of small molecules, called ARM-Ps (antibody-recruiting molecule targeting prostate cancer) that are capable of enhancing antibody-mediated immune recognition of prostate cancer cells. Interestingly, during the course of these studies, we found ARM-Ps to exhibit extraordinarily high potencies toward PSMA, compared to previously reported inhibitors. Here, we report in-depth biochemical, crystallographic, and computational investigations which elucidate the origin of the observed affinity enhancement. These studies reveal a previously unreported arene-binding site on PSMA, which we believe participates in an aromatic stacking interaction with ARMs. Although this site is composed of only a few amino acid residues, it drastically enhances small molecule binding affinity. These results provide critical insights into the design of PSMA-targeted small molecules for prostate cancer diagnosis and treatment; more broadly, the presence of similar arene-binding sites throughout the proteome could prove widely enabling in the optimization of small molecule-protein interactions.
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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.