ArticleInternational journal of cancer2013
The phosphatidylinositol-3 kinase I inhibitor BKM120 induces cell death in B-chronic lymphocytic leukemia cells in vitro.
Article in International journal of cancer, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 42 citations in OpenAlex.
- Review
- PI3K inhibitors in chronic lymphocytic leukemia: where do we go from here?Haematologica · 2023Review
- The Superior Cytotoxicity of Dual Targeting of BCR/ABL and PI3K in K562 Cells: Proposing a Novel Therapeutic Potential for the Treatment of CML.Indian journal of hematology & blood transfusion : an official journal of Indian Society of Hematology and Blood Transfusion · 2022Article
- The influence of PI3K inhibition on the radiotherapy response of head and neck cancer cells.Scientific reports · 2020Article
- PI3K Inhibitors and Their Role as Novel Agents for Targeted Therapy in Lymphoma.Current treatment options in oncology · 2020Review
- Precision spherical nucleic acids for delivery of anticancer drugs.Chemical science · 2017Article
- Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.Nature communications · 2017Article
- Effects of PI3K inhibitor NVP-BKM120 on overcoming drug resistance and eliminating cancer stem cells in human breast cancer cells.Cell death & disease · 2015Article
- The pan-class I phosphatidyl-inositol-3 kinase inhibitor NVP-BKM120 demonstrates anti-leukemic activity in acute myeloid leukemia.Scientific reports · 2015Article
- Pharmacological targeting of PI3K isoforms as a therapeutic strategy in chronic lymphocytic leukaemia.Leukemia research reports · 2015Review
- PI3K/Akt/mTOR pathway inhibitors enhance radiosensitivity in radioresistant prostate cancer cells through inducing apoptosis, reducing autophagy, suppressing NHEJ and HR repair pathways.Cell death & disease · 2014Article
- Activity of the pan-class I phosphoinositide 3-kinase inhibitor NVP-BKM120 in T-cell acute lymphoblastic leukemia.Leukemia · 2014Article
- Idelalisib for the treatment of chronic lymphocytic leukemia.ISRN oncology · 2014Review
- Isotype-specific inhibition of the phosphatidylinositol-3-kinase pathway in hematologic malignancies.OncoTargets and therapy · 2014Review
- Resistance to Dasatinib in primary chronic lymphocytic leukemia lymphocytes involves AMPK-mediated energetic re-programming.Oncotarget · 2013Article
- Clinical development of phosphatidylinositol 3-kinase inhibitors for non-Hodgkin lymphoma.Biomarker research · 2013Article
- Article
- Pharmacological targeting of eIF4E in primary CLL lymphocytes.Blood cancer journal · 2013Article
- Clinical development of phosphatidylinositol 3-kinase inhibitors for cancer treatment.BMC medicine · 2012Review
- Development and Clinical Applications of PI3K/AKT/mTOR Pathway Inhibitors as a Therapeutic Option for Leukemias.Cancer diagnosis & prognosisReview
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
BKM120, a pan class I PI3K inhibitor, was cytotoxic in the majority of primary B-chronic lymphocytic leukemia (CLL) lymphocytes, including samples from patients who have a high-risk for poor response to treatment (patient with del11 and del17) at clinically obtainable concentrations. The PI3Kδ inhibitor Cal-101 is cytotoxic in B-CLL lymphocytes in vitro and is active in the treatment of CLL in vivo. Interestingly, we demonstrated that BKM120 is 3.6 fold more toxic than Cal-101 in malignant B-CLL lymphocytes in vitro. BKM120 cytotoxicity correlated with the basal expression of proteins involved in the PI3K/Akt pathway. A protein signature of PI3K pathway proteins predicts the response to BKM120 treatment. In the primary B-CLL lymphocytes tested in vitro, BKM120 decreased the phosphorylation status of molecular biomarkers used as indicators of PI3K pathway inhibition in vivo. Also, BKM120 induced apoptosis in primary B-CLL cells culture in the presence and absence of stromal cell support. Our findings suggest that BKM120 should be tested clinically in CLL.
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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.