ArticleClinical cancer research : an official journal of the American Association for Cancer Research2014
SETting OP449 into the PP2A-activating drug family.
Article in Clinical cancer research : an official journal of the American Association for Cancer Research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 34 citations in OpenAlex.
- SET alpha and SET beta mRNA isoforms in chronic lymphocytic leukaemia.British journal of haematology · 2019Trial
- Targeting SET to counteract Lyn activation demonstrates anti-cancer potential in diffuse large B-cell lymphoma.Clinical and experimental medicine · 2025Article
- In Silico and In Vivo Studies of a Tumor-Penetrating and Interfering Peptide with Antitumoral Effect on Xenograft Models of Breast Cancer.Pharmaceutics · 2023Article
- Review
- PPP2CA Is a Novel Therapeutic Target in Neuroblastoma Cells That Can Be Activated by the SET Inhibitor OP449.Frontiers in oncology · 2022Article
- Deregulation of protein phosphatase 2A inhibitor SET is associated with malignant progression in breast cancer.Scientific reports · 2021Article
- Robust inference of kinase activity using functional networks.Nature communications · 2021Article
- Small Cell Lung Cancer from Traditional to Innovative Therapeutics: Building a Comprehensive Network to Optimize Clinical and Translational Research.Journal of clinical medicine · 2020Review
- Protein phosphatase 2A activation as a therapeutic strategy for managing MYC-driven cancers.The Journal of biological chemistry · 2020Article
- Aurora B kinase activity is regulated by SET/TAF1 on Sgo2 at the inner centromere.The Journal of cell biology · 2019Article
- Mission Possible: Advances in MYC Therapeutic Targeting in Cancer.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2019Review
- The NMR-based characterization of the FTY720-SET complex reveals an alternative mechanism for the attenuation of the inhibitory SET-PP2A interaction.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- Targeting SET to restore PP2A activity disrupts an oncogenic CIP2A-feedforward loop and impairs triple negative breast cancer progression.EBioMedicine · 2019Article
- Macrocyclic peptides decrease c-Myc protein levels and reduce prostate cancer cell growth.Cancer biology & therapy · 2017Article
- Overlapping SETBP1 gain-of-function mutations in Schinzel-Giedion syndrome and hematologic malignancies.PLoS genetics · 2017Article
- Cellular and Molecular Networks in Chronic Myeloid Leukemia: The Leukemic Stem, Progenitor and Stromal Cell Interplay.Current drug targets · 2017Review
- Combined targeting of SET and tyrosine kinases provides an effective therapeutic approach in human T-cell acute lymphoblastic leukemia.Oncotarget · 2016Article
- Cooperation of imipramine blue and tyrosine kinase blockade demonstrates activity against chronic myeloid leukemia.Oncotarget · 2016Article
- Overexpression of PP2A inhibitor SET oncoprotein is associated with tumor progression and poor prognosis in human non-small cell lung cancer.Oncotarget · 2015Article
- Cardamonin Suppresses TGF-β1-Induced Epithelial Mesenchymal Transition via Restoring Protein Phosphatase 2A Expression.Biomolecules & therapeutics · 2015Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
The protein phosphatase 2A (PP2A) tumor suppressor is inactivated in different leukemias through the activity of its endogenous inhibitors (e.g., SET), which are aberrantly regulated by oncogenic tyrosine kinases. Like other effective and nontoxic PP2A-activating drugs (PAD), OP449 inhibits SET and impairs leukemogenesis. This further supports the immediate use of PADs in patients with leukemia.
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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.