ArticleThe Journal of biological chemistry2009
Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases.
Article in The Journal of biological chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
What it found
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Who cites it
34 citing papers in PubMed, 80 citations in OpenAlex.
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- Valproate reactivates HTLV-1 tax and reduces ABCB1/MDR1 expression in PBMCs derived from ATLL patients.Frontiers in oncology · 2026Article
- Use of Microfluidics for Study of FOXO3 Translocation Dynamics.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Progress in Research of Nanotherapeutics for Overcoming Multidrug Resistance in Cancer.International journal of molecular sciences · 2024Review
- AI-organoid integrated systems for biomedical studies and applications.Bioengineering & translational medicine · 2024Review
- Conditional fluorescent mouse translocation reporters for ERK1/2 and AKT signaling.Developmental biology · 2023Article
- Mechanism of anticancer effect of ETP-45658, a PI3K/AKT/mTOR pathway inhibitor on HT-29 Cells.Medical oncology (Northwood, London, England) · 2023Article
- Multiplexed cellular profiling identifies an organoselenium compound as an inhibitor of CRM1-mediated nuclear export.Traffic (Copenhagen, Denmark) · 2022Article
- mTORC2 Is the Major Second Layer Kinase Negatively Regulating FOXO3 Activity.Molecules (Basel, Switzerland) · 2022Article
- Target identification for small-molecule discovery in the FOXO3a tumor-suppressor pathway using a biodiverse peptide library.Cell chemical biology · 2021Article
- Therapeutic strategies targeting FOXO transcription factors.Nature reviews. Drug discovery · 2021Review
- Pooled CRISPR screens with imaging on microraft arrays reveals stress granule-regulatory factors.Nature methods · 2020Article
- Current perspective on the regulation of FOXO4 and its role in disease progression.Cellular and molecular life sciences : CMLS · 2020Review
- Role of Overexpressed Transcription Factor FOXO1 in Fatal Cardiovascular Septal Defects in Patau Syndrome: Molecular and Therapeutic Strategies.International journal of molecular sciences · 2018Article
- Regulatory T cells in the treatment of disease.Nature reviews. Drug discovery · 2018Review
- Rapid Renal Regulation of Peroxisome Proliferator-activated Receptor γ Coactivator-1α by Extracellular Signal-Regulated Kinase 1/2 in Physiological and Pathological Conditions.The Journal of biological chemistry · 2016Article
- Empowering Regulatory T Cells in Autoimmunity.Trends in molecular medicine · 2016Review
- Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling.PloS one · 2016Article
- Methylseleninic acid promotes antitumour effects via nuclear FOXO3a translocation through Akt inhibition.Pharmacological research · 2015Article
- FOXO3 and related transcription factors in development, aging, and exceptional longevity.The journals of gerontology. Series A, Biological sciences and medical sciences · 2015Article
Corrections and comments
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Authors and funding
19 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Activation of the phosphoinositide 3-kinase (PI3K)/Akt signaling pathway is one the most frequent genetic events in human cancer. A cell-based imaging assay that monitored the translocation of the Akt effector protein, Forkhead box O (FOXO), from the cytoplasm to the nucleus was employed to screen a collection of 33,992 small molecules. The positive compounds were used to screen kinases known to be involved in FOXO translocation. Pyrazolopyrimidine derivatives were found to be potent FOXO relocators as well as biochemical inhibitors of PI3Kalpha. A combination of virtual screening and molecular modeling led to the development of a structure-activity relationship, which indicated the preferred substituents on the pyrazolopyrimidine scaffold. This leads to the synthesis of ETP-45658, which is a potent and selective inhibitor of phosphoinositide 3-kinases and demonstrates mechanism of action in tumor cell lines and in vivo in treated mice.
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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.