ArticleMolecular pharmaceutics2011
Development of a peptide-drug conjugate for prostate cancer therapy.
Article in Molecular pharmaceutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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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.
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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
31 citing papers in PubMed, 90 citations in OpenAlex.
- Synthesis and Characterization of Polymer-Drug Conjugates by Strain-Promoted Azide-Alkyne Cycloaddition-Mediated Polymerization.Journal of applied polymer science · 2025Article
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- Peptide-based delivery of therapeutics in cancer treatment.Materials today. Bio · 2022Review
- Role of Serine Proteases at the Tumor-Stroma Interface.Frontiers in immunology · 2022Review
- First-principles studies on two-dimensional BJournal of molecular modeling · 2021Article
- Identification of a peptide binding to cancer antigen Kita-kyushu lung cancer antigen 1 from a phage-display library.Cancer science · 2021Article
- Development and Characterization of a Novel Peptide-Drug Conjugate with DM1 for Treatment of FGFR2-Positive Tumors.Biomedicines · 2021Article
- Current applications and prospects of nanoparticles for antifungal drug delivery.EXCLI journal · 2021Review
- Review
- Enzyme-responsive polymeric micelles of cabazitaxel for prostate cancer targeted therapy.Acta biomaterialia · 2020Article
- Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery.Molecules (Basel, Switzerland) · 2019Review
- Smart Targeting To Improve Cancer Therapeutics.Drug design, development and therapy · 2019Review
- Synthesis and PI3 Kinase Inhibition Activity of Some Novel Trisubstituted Morpholinopyrimidines.Molecules (Basel, Switzerland) · 2018Article
- Synthesis and PI 3-Kinase Inhibition Activity of Some Novel 2,4,6-Trisubstituted 1,3,5-Triazines.Molecules (Basel, Switzerland) · 2018Article
- Anticancer activities of emetine prodrugs that are proteolytically activated by the prostate specific antigen (PSA) and evaluation of in vivo toxicity of emetine derivatives.Bioorganic & medicinal chemistry · 2017Article
- Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma-a novel strategy for tumor-targeted therapy.Oncology letters · 2017Article
- Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells.The Prostate · 2017Article
- Targeting PEPT1: a novel strategy to improve the antitumor efficacy of doxorubicin in human hepatocellular carcinoma therapy.Oncotarget · 2017Article
- Advancement and applications of peptide phage display technology in biomedical science.Journal of biomedical science · 2016Article
- Design, synthesis, and evaluation of cisplatin-containing EGFR targeting bioconjugates as potential therapeutic agents for brain tumors.OncoTargets and therapy · 2016Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate to specifically deliver TGX-221 to HER2 overexpressing prostate cancer cells. Four TGX-221 derivatives with added hydroxyl groups were synthesized for peptide conjugation. Among them, TGX-D1 exhibited a similar bioactivity to TGX-221, and it was selected for conjugation with a peptide promoiety containing a HER2-targeting ligand and a prostate specific antigen (PSA) substrate linkage. From this selection, the peptide-drug conjugate was proven to be gradually cleaved by PSA to release TGX-D1. Cellular uptake of the peptide-drug conjugate was significantly higher in prostate cancer cells compared to the parent drug. Moreover, both the peptide-drug conjugate and its cleaved products demonstrated comparable activities as the parent drug TGX-D1. Our results suggest that this peptide-drug conjugate may provide a promising chemotherapy for prostate cancer patients.
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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.