A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia.
Sign Up to like & getrecommendations! Published in 2019 at "Cancer cell"
DOI: 10.1016/j.ccell.2019.11.001
Abstract: Inhibition of the Menin (MEN1) and MLL (MLL1, KMT2A) interaction is a potential therapeutic strategy for MLL-rearranged (MLL-r) leukemia. Structure-based design yielded the potent, highly selective, and orally bioavailable small-molecule inhibitor VTP50469. Cell lines carrying… read more here.
Keywords: mll; mll rearranged; menin mll; mll inhibitor ... See more keywords
Systematic chemical and molecular profiling of MLL-rearranged infant acute lymphoblastic leukemia reveals efficacy of romidepsin
Sign Up to like & getrecommendations! Published in 2017 at "Leukemia"
DOI: 10.1038/leu.2016.165
Abstract: To address the poor prognosis of mixed lineage leukemia (MLL)-rearranged infant acute lymphoblastic leukemia (iALL), we generated a panel of cell lines from primary patient samples and investigated cytotoxic responses to contemporary and novel Food… read more here.
Keywords: infant acute; lymphoblastic leukemia; rearranged infant; acute lymphoblastic ... See more keywords
Preclinical efficacy of gemcitabine in MLL-rearranged infant acute lymphoblastic leukemia
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DOI: 10.1038/s41375-020-0895-9
Abstract: The treatment of children diagnosed with acute lymphoblastic leukemia (ALL) has improved significantly over recent decades, with 5-year event-free survival (EFS) approaching 85% [1]. However, 5-year EFS for infants diagnosed at less than 1 year… read more here.
Keywords: mll rearranged; rearranged infant; acute lymphoblastic; lymphoblastic leukemia ... See more keywords
A novel small molecule that kills a subset of MLL-rearranged leukemia cells by inducing mitochondrial dysfunction
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DOI: 10.1038/s41388-018-0666-5
Abstract: Survival rates for pediatric patients suffering from mixed lineage leukemia (MLL)-rearranged leukemia remain below 50% and more targeted, less toxic therapies are urgently needed. A screening method optimized to discover cytotoxic compounds selective for MLL-rearranged… read more here.
Keywords: mll rearranged; subset mll; leukemia cells; rearranged leukemia ... See more keywords
Antileukemic Efficacy of BET Inhibitor in a Preclinical Mouse Model of MLL-AF4+ Infant ALL
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DOI: 10.1158/1535-7163.mct-17-1123
Abstract: MLL-rearranged acute lymphoblastic leukemia (ALL) occurring in infants is a rare but very aggressive leukemia, typically associated with a dismal prognosis. Despite the development of specific therapeutic protocols, infant patients with MLL-rearranged ALL still suffer… read more here.
Keywords: mll af4; model mll; mouse model; mll rearranged ... See more keywords
Rewiring the Epigenetic Networks in MLL-Rearranged Leukemias: Epigenetic Dysregulation and Pharmacological Interventions
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DOI: 10.3389/fcell.2019.00081
Abstract: Leukemias driven by chromosomal translocation of the mixed-lineage leukemia gene (MLL or KMT2A) are highly prevalent in pediatric oncology. The poor survival rate and lack of an effective targeted therapy for patients with MLL-rearranged (MLL-r)… read more here.
Keywords: networks mll; leukemias epigenetic; epigenetic networks; rewiring epigenetic ... See more keywords
Quinazoline-based analog of adenine as an antidote against MLL-rearranged leukemia cells: synthesis, inhibition assays and docking studies.
Sign Up to like & getrecommendations! Published in 2022 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2021-0251
Abstract: Background: Post-translational modifications of histones constitute a dynamic process impacting gene expression. A well-studied modification is lysine methylation. Among the lysine histone methyltransferases, DOT1L is implicated in various diseases, making it a very interesting target… read more here.
Keywords: based analog; adenine antidote; mll rearranged; antidote mll ... See more keywords