Search Results - "STRESEMANN, Carlo"
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Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine
Published in International journal of cancer (01-07-2008)“…The cytosine analogues 5‐azacytosine (azacytidine) and 2′‐deoxy‐5‐azacytidine (decitabine) are the currently most advanced drugs for epigenetic cancer…”
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Methylation of Human MicroRNA Genes in Normal and Neoplastic Cells
Published in Cell cycle (Georgetown, Tex.) (02-05-2007)“…MicroRNAs (miRNAs) are small RNA molecules that control gene expression by inhibition of protein translation or by degradation of cognate target mRNAs. Even…”
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EZH2 Inhibition Blocks Multiple Myeloma Cell Growth through Upregulation of Epithelial Tumor Suppressor Genes
Published in Molecular cancer therapeutics (01-02-2016)“…Multiple myeloma is a plasma cell malignancy characterized by marked heterogeneous genomic instability including frequent genetic alterations in epigenetic…”
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Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines
Published in Cancer research (Chicago, Ill.) (01-03-2006)“…DNA methyltransferase inhibitors represent promising new drugs for cancer therapies. The first of these compounds (5-azacytidine, Vidaza) has recently been…”
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Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreatic cancer
Published in Genes & development (01-04-2016)“…Pancreatic ductal adenocarcinoma (PDAC) is a lethal form of cancer with few therapeutic options. We found that levels of the lysine methyltransferase SMYD2…”
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A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition
Published in Scientific reports (19-01-2024)“…The market approval of Tazemetostat (TAZVERIK) for the treatment of follicular lymphoma and epithelioid sarcoma has established “enhancer of zeste homolog 2”…”
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Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2
Published in Journal of medicinal chemistry (26-05-2016)“…Protein lysine methyltransferases have recently emerged as a new target class for the development of inhibitors that modulate gene transcription or signaling…”
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Functional diversity of inhibitors tackling the differentiation blockage of MLL-rearranged leukemia
Published in Journal of hematology and oncology (28-06-2019)“…The chromosomal rearrangements of the mixed-lineage leukemia gene MLL (KMT2A) have been extensively characterized as a potent oncogenic driver in leukemia. For…”
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Azacytidine causes complex DNA methylation responses in myeloid leukemia
Published in Molecular cancer therapeutics (01-09-2008)“…Aberrant DNA methylation patterns play an important role in the pathogenesis of hematologic malignancies. The DNA methyltransferase inhibitors azacytidine and…”
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Identification of Small Molecules that Modulate Mutant p53 Condensation
Published in iScience (25-09-2020)“…Structural mutants of p53 induce global p53 protein destabilization and misfolding, followed by p53 protein aggregation. First evidence indicates that p53 can…”
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Human concentrative nucleoside transporter 1-mediated uptake of 5-azacytidine enhances DNA demethylation
Published in Molecular cancer therapeutics (01-01-2009)“…The DNA methyltransferase inhibitors 5-azacytidine (5-azaCyd) and 5-aza-2′-deoxycytidine have found increasing use for the treatment of myeloid leukemias and…”
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Antiproliferative effects of DNA methyltransferase 3B depletion are not associated with DNA demethylation
Published in PloS one (01-05-2012)“…Silencing of genes by hypermethylation contributes to cancer progression and has been shown to occur with increased frequency at specific genomic loci…”
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The human let-7a-3 locus contains an epigenetically regulated MicroRNA gene with oncogenic function
Published in Cancer research (Chicago, Ill.) (15-02-2007)“…MicroRNAs (miRNAs) are small noncoding RNAs that repress their target mRNAs by complementary base pairing and induction of the RNA interference pathway. It has…”
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Abstract 4475: SMYD2 inhibitor BAY-598 reveals the giant scaffold AHNAK as a novel multi-methylated substrate
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract The SET and MYND domain-containing protein 2 (SMYD2) has been reported to mono-methylate several lysine residues on histone and non-histone proteins…”
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MYCN mediates cysteine addiction and sensitizes neuroblastoma to ferroptosis
Published in Nature cancer (01-04-2022)“…Aberrant expression of MYC transcription factor family members predicts poor clinical outcome in many human cancers. Oncogenic MYC profoundly alters metabolism…”
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Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling
Published in Cell chemical biology (18-07-2024)“…This study describes the identification and target deconvolution of small molecule inhibitors of oncogenic Yes-associated protein (YAP1)/TAZ activity with…”
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Characterization of the Menin-MLL Interaction as Therapeutic Cancer Target
Published in Cancers (14-01-2020)“…Inhibiting the interaction of menin with the histone methyltransferase MLL1 (KMT2A) has recently emerged as a novel therapeutic strategy. Beneficial…”
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Abstract 4973: MYCN mediates cysteine addiction and sensitizes to ferroptosis in cancer cells
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Aberrant expression of MYC family members predicts poor clinical outcome in many human cancers. Oncogenic MYC profoundly alters metabolism and…”
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Quantification of histone H3 Lys27 trimethylation (H3K27me3) by high-throughput microscopy enables cellular large-scale screening for small-molecule EZH2 inhibitors
Published in Journal of biomolecular screening (01-02-2015)“…EZH2 inhibition can decrease global histone H3 lysine 27 trimethylation (H3K27me3) and thereby reactivates silenced tumor suppressor genes. Inhibition of EZH2…”
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