ArticleJournal of medicinal chemistry2012
Synthesis and characterization of a novel prostate cancer-targeted phosphatidylinositol-3-kinase inhibitor prodrug.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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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
15 citing papers in PubMed, 39 citations in OpenAlex.
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- Development of a Prostate-Specific Antigen Targeted Dual Drug Conjugate for Prostate Cancer Therapy.ACS omega · 2025Article
- One-Pot Regio- and Diastereoselective Gold-Catalyzed Propargylation of in Situ Activated Chromones and Consecutive Cyclization.Organic letters · 2024Article
- Identification of drug responsive enhancers by predicting chromatin accessibility change from perturbed gene expression profiles.NPJ systems biology and applications · 2024Article
- Role of the PI3K/Akt pathway in cadmium induced malignant transformation of normal prostate epithelial cells.Toxicology and applied pharmacology · 2020Article
- Synthesis and PI3 Kinase Inhibition Activity of a Wortmannin-Leucine Derivative.Molecules (Basel, Switzerland) · 2018Article
- 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
- Identification of a Potent Phosphoinositide 3-Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs.ChemMedChem · 2017Article
- Anti-androgenic effects of flavonols in prostate cancer.Ecancermedicalscience · 2015Review
- Tumor-targeting of EGFR inhibitors by hypoxia-mediated activation.Angewandte Chemie (International ed. in English) · 2014Article
- Combination of the PI3K inhibitor ZSTK474 with a PSMA-targeted immunotoxin accelerates apoptosis and regression of prostate cancer.Neoplasia (New York, N.Y.) · 2013Article
- Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors.Bioorganic & medicinal chemistry · 2013Review
- Behavioral stress accelerates prostate cancer development in mice.The Journal of clinical investigation · 2013Article
- Personalized prostate cancer therapy based on systems analysis of the apoptosis regulatory network.Asian journal of andrologyReview
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The phosphatidylinositol-3-kinase/Akt (PI3K/Akt) pathway is constitutively activated in a substantial proportion of prostate tumors and is considered a key mechanism supporting progression toward an androgen-independent status, for which no effective therapy is available. Therefore, PI3K inhibitors, alone or in combination with other cytotoxic drugs, could potentially be used to treat cancer with a constitutive activated PI3K/Akt pathway. To selectively target advanced prostate tumors with a constitutive activated PI3K/Akt pathway, a prostate cancer-specific PI3K inhibitor was generated by coupling the chemically modified form of the quercetin analogue LY294002 (HO-CH(2)-LY294002, compound 8) with the peptide Mu-LEHSSKLQL, in which the internal sequence HSSKLQ is a substrate for the prostate-specific antigen (PSA) protease. The result is a water-soluble and latent PI3K inhibitor prodrug (compound 11), its activation being dependent on PSA cleavage. Once activated, the L-O-CH(2)-LY294002 (compound 10) can specifically inhibit PI3K in PSA-secreting prostate cancer cells and induce apoptosis with a potency comparable to that of the original LY294002 compound.
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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.