ArticleMolecular cancer therapeutics2009
Novel benzylidene-thiazolidine-2,4-diones inhibit Pim protein kinase activity and induce cell cycle arrest in leukemia and prostate cancer cells.
Article in Molecular cancer therapeutics, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 97 citations in OpenAlex.
- PIM1 kinase and its diverse substrate in solid tumors.Cell communication and signaling : CCS · 2024Review
- Review
- Pim-1 kinase is a positive feedback regulator of the senescent lung fibroblast inflammatory secretome.American journal of physiology. Lung cellular and molecular physiology · 2022Article
- Green Synthesis of Thiazolidine-2,4-dione Derivatives and Their Lipoxygenase Inhibition Activity With QSAR and Molecular Docking Studies.Frontiers in chemistry · 2022Article
- Article
- Urazolium diacetate as a new, efficient and reusable Brønsted acid ionic liquid for the synthesis of novel derivatives of thiazolidine-4-ones.RSC advances · 2019Article
- Review
- Development of a Novel Series of Anticancer and Antidiabetic: Spirothiazolidines Analogs.Molecules (Basel, Switzerland) · 2019Article
- PIM kinase inhibitor, AZD1208, inhibits protein translation and induces autophagy in primary chronic lymphocytic leukemia cells.Oncotarget · 2019Article
- PIM-2 protein kinase negatively regulates T cell responses in transplantation and tumor immunity.The Journal of clinical investigation · 2018Article
- High glucose promotes vascular smooth muscle cell proliferation by upregulating proto-oncogene serine/threonine-protein kinase Pim-1 expression.Oncotarget · 2017Article
- Targeting the PIM protein kinases for the treatment of a T-cell acute lymphoblastic leukemia subset.Oncotarget · 2017Article
- Upregulation of PIM2 by Underexpression of MicroRNA-135-5p Improves Survival Rates of Skin Allografts by Suppressing Apoptosis of Fibroblast Cells.Medical science monitor : international medical journal of experimental and clinical research · 2017Article
- Protein profiling identifies mTOR pathway modulation and cytostatic effects of Pim kinase inhibitor, AZD1208, in acute myeloid leukemia.Leukemia & lymphoma · 2016Article
- A facile synthesis and antimicrobial activity evaluation of sydnonyl-substituted thiazolidine derivatives.Molecules (Basel, Switzerland) · 2015Article
- Pim kinases in hematological malignancies: where are we now and where are we going?Journal of hematology & oncology · 2014Review
- The Pim-1 protein kinase is an important regulator of MET receptor tyrosine kinase levels and signaling.Molecular and cellular biology · 2014Article
- A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas.Neoplasia (New York, N.Y.) · 2014Article
- Inhibition of Pim2-prolonged skin allograft survival through the apoptosis regulation pathway.Cellular & molecular immunology · 2012Article
- Pim kinase inhibitors sensitize prostate cancer cells to apoptosis triggered by Bcl-2 family inhibitor ABT-737.Cancer research · 2012Article
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
The Pim protein kinases play important roles in cancer development and progression, including prostate tumors and hematologic malignancies. To investigate the potential role of these enzymes as anticancer drug targets, we have synthesized novel benzylidene-thiazolidine-2,4-diones that function as potent Pim protein kinase inhibitors. With IC(50) values in the nanomolar range, these compounds block the ability of Pim to phosphorylate peptides and proteins in vitro and, when added to DU145 prostate cancer cells overexpressing Pim, inhibit the ability of this enzyme to phosphorylate a known substrate, the BH(3) protein BAD. When added to prostate cancer cell lines, including PC3, DU145, and CWR22Rv1, and human leukemic cells, MV4;11, K562, and U937 cells, these compounds induce G(1)-S cell cycle arrest and block the antiapoptotic effect of the Pim protein kinase. The cell cycle arrest induced by these compounds is associated with an inhibition of cyclin-dependent kinase 2 and activity and translocation of the Pim-1 substrate p27(Kip1), a cyclin-dependent kinase 2 inhibitory protein, to the nucleus. Furthermore, when added to leukemic cells, these compounds synergize with the mammalian target of rapamycin inhibitor rapamycin to decrease the phosphorylation level of the translational repressor 4E-BP1 at sites phosphorylated by mammalian target of rapamycin. Combinations of rapamycin and the benzylidene-thiazolidine-2,4-diones synergistically block the growth of leukemic cells. Thus, these agents represent novel Pim inhibitors and point to an important role for the Pim protein kinases in cell cycle control in multiple types of cancer cells.
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