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decitabine

TET2-Mediated Epigenetic Reprogramming of Breast Cancer Cells Impairs Lysosome Biogenesis

[Life Science Alliance] The authors sought to alter transcriptional programs by enforcing expression of the catalytic domain of the methylcytosine dioxygenase TET2 in breast cancer cells.

Methylation-Mediated Silencing of Protein Kinase C Zeta Induces Apoptosis Avoidance through ATM/CHK2 Inactivation in Dedifferentiated Chondrosarcoma

[British Journal of Cancer] Researchers identified genes downregulated in dedifferentiated chondrosarcoma vs. conventional chondrosarcoma due to DNA methylation using in silico analysis.

The DNMT1 Inhibitor GSK-3484862 Mediates Global Demethylation in Murine Embryonic Stem Cells

[Epigenetics & Chromatin] Researchers determined whether GSK-3484862 can induce demethylation more effectively than 5-azanucleosides. They determined the cytotoxicity and optimal concentration of GSK-3484862 by treating wild-type or Dnmt1/3a/3b triple knockout mESC with different concentrations of the compound, which was obtained from two commercial sources.

Targeting DNMT1 by Demethylating Agent OR-2100 Increases Tyrosine Kinase Inhibitors-Sensitivity and Depletes Leukemic Stem Cells in Chronic Myeloid Leukemia

[Cancer Letters] OR21 exhibited anti-tumor effects as a monotherapy, and in combination therapy it increased tyrosine kinase inhibitors -induced apoptosis and induction of tumor suppressor genes including PTPN6 encoding SHP-1 in chronic myeloid leukemia cells.

Targeting DNMTs to Overcome Enzalutamide Resistance in Prostate Cancer

[Molecular Cancer therapeutics] Scientists suggested that DNA methylation pathway is deregulated after enzalutamide resistance onset and that targeting DNA methyltransferases restored the sensitivity to enzalutamide in prostate cancer cells.

Discovery of a First-in-Class Reversible DNMT1-Selective Inhibitor with Improved Tolerability and Efficacy in Acute Myeloid Leukemia

[Nature Cancer] Due to improved in vivo tolerability compared with decitabine, GSK3685032 yielded superior tumor regression and survival mouse models of acute myeloid leukemia.

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