ArticleCancers2021
Small Molecule-Based Prodrug Targeting Prostate Specific Membrane Antigen for the Treatment of Prostate Cancer.
Article in Cancers, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
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Who cites it
16 citing papers in PubMed, 32 citations in OpenAlex.
- PSMA-1-DOTA Potentially for Effective Targeted Radioligand Therapy of Prostate Cancer.Molecular imaging and biology · 2025Article
- Prodrugs Targeting Prostate-Specific Membrane Antigen against Prostate Cancer.Journal of medicinal chemistry · 2025Review
- Prostate Specific Membrane Antigen Expression in a Syngeneic Breast Cancer Mouse Model.Molecular imaging and biology · 2024Article
- PSMA-targeted combination brusatol and docetaxel nanotherapeutics for the treatment of prostate cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2024Article
- A Synergistic Strategy Combining Chemotherapy and Photodynamic Therapy to Eradicate Prostate Cancer.International journal of molecular sciences · 2024Article
- Emerging non-antibody‒drug conjugates (non-ADCs) therapeutics of toxins for cancer treatment.Acta pharmaceutica Sinica. B · 2024Review
- Structure-activity relationship study of mesyl and busyl phosphoramidate antisense oligonucleotides for unaided and PSMA-mediated uptake into prostate cancer cells.Frontiers in chemistry · 2024Article
- Article
- Synthesis and Evaluation of ePSMA-DM1: A New Theranostic Small-Molecule Drug Conjugate (T-SMDC) for Prostate Cancer.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Old Drug, New Delivery Strategy: MMAE Repackaged.International journal of molecular sciences · 2023Article
- Payload-Binding Fab Fragments Increase the Therapeutic Index of MMAE Antibody-Drug Conjugates.Molecular cancer therapeutics · 2023Article
- Modular Smart Molecules for PSMA-Targeted Chemotherapy.Molecular cancer therapeutics · 2022Article
- Targeted Chemoradiotherapy of Prostate Cancer Using Gold Nanoclusters with Protease Activatable Monomethyl Auristatin E.ACS applied materials & interfaces · 2022Article
- Drug resistance in metastatic castration-resistant prostate cancer: an update on the status quo.Cancer drug resistance (Alhambra, Calif.) · 2022Review
- A low molecular weight multifunctional theranostic molecule for the treatment of prostate cancer.Theranostics · 2022Article
- Prostate-Specific Membrane Antigen-Targeted Turn-on Probe for Imaging Cargo Release in Prostate Cancer Cells.Bioconjugate chemistry · 2021Article
Corrections and comments
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Authors and funding
19 authors at 4 institutions in 1 country.
Funding
Abstract
Metastatic castration-resistant prostate cancer poses a serious clinical problem with poor outcomes and remains a deadly disease. New targeted treatment options are urgently needed. PSMA is highly expressed in prostate cancer and has been an attractive biomarker for the treatment of prostate cancer. In this study, we explored the feasibility of targeted delivery of an antimitotic drug, monomethyl auristatin E (MMAE), to tumor tissue using a small-molecule based PSMA lig-and. With the aid of Cy5.5, we found that a cleavable linker is vital for the antitumor activity of the ligand-drug conjugate and have developed a new PSMA-targeting prodrug, PSMA-1-VcMMAE. In in vitro studies, PSMA-1-VcMMAE was 48-fold more potent in killing PSMA-positive PC3pip cells than killing PSMA-negative PC3flu cells. In in vivo studies, PSMA-1-VcMMAE significantly inhibited tumor growth leading to prolonged animal survival in different animal models, including metastatic prostate cancer models. Compared to anti-PSMA antibody-MMAE conjugate (PSMA-ADC) and MMAE, PSMA-1-VcMMAE had over a 10-fold improved maximum tolerated dose, resulting in improved therapeutic index. The small molecule-drug conjugates reported here can be easily synthesized and are more cost efficient than anti-body-drug conjugates. The therapeutic profile of the PSMA-1-VcMMAE encourages further clin-ical development for the treatment of advanced prostate cancer.
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What OpenQuestion holds
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.