Results 31 to 40 of about 12,929 (212)
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors
ACS Medicinal Chemistry Letters, 2020 Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1.
Victor S. Gehling +19 more
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Pharmacological inhibition of LSD1 activity blocks REST-dependent medulloblastoma cell migration
Cell Communication and Signaling, 2018 Background Medulloblastoma (MB) is the most common malignant brain tumor in children. Current problems in the clinic include metastasis, recurrence, and treatment-related sequelae that highlight the need for targeted therapies.
Keri Callegari +3 more
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Histone Demethylase LSD1 Regulates Adipogenesis [PDF]
Journal of Biological Chemistry, 2010 Epigenetic mechanisms, in particular the enzymatic modification of histones, are a crucial element of cell differentiation, a regulated process that allows a precursor cell basically to turn into a different cell type while maintaining the same genetic equipment.
Marcelina Párrizas +5 more
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Pharmacological inhibition of LSD1 for the treatment of MLL-rearranged leukemia
Journal of Hematology & Oncology, 2016 Background Mixed lineage leukemia (MLL) gene translocations are found in ~75 % infant and 10 % adult acute leukemia, showing a poor prognosis. Lysine-specific demethylase 1 (LSD1) has recently been implicated to be a drug target for this subtype of ...
Zizhen Feng +10 more
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Effect of LSD1 on Proliferation and Metastasis of Ovarian Cancer Cells by Regulating Foxo3a
Zhongliu Fangzhi Yanjiu, 2018 Objective To investigate the effects of lysine-specific demethylation 1 (LSD1) on the proliferation and metastasis of ovarian cancer cells by regulating Foxo3a.
WANG Pinhao +4 more
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Discovery of novel sulphonamide hybrids that inhibit LSD1 against bladder cancer cells
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022 Aim:A series of sulphonamide hybrids were designed, synthesised, and identified as potential lysine-specific demethylase 1 (LSD1) inhibitors.Materials and methods: Bladder cancer cell lines were cultured to evaluate the antiproliferative activity ...
Jia Liu +3 more
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Cells, 2021 Salicylic acid (SA) is well known hormonal molecule involved in cell death regulation. In response to a broad range of environmental factors (e.g., high light, UV, pathogens attack), plants accumulate SA, which participates in cell death induction and ...
Maciej Jerzy Bernacki +3 more
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LSD1 Histone Demethylase Assays and Inhibition [PDF]
, 2016 The lysine-specific demethylase (LSD1) is a flavin-dependent amine oxidase that selectively removes one or two methyl groups from histone H3 at the Lys4 position. Along with histone deacetylases 1 and 2, LSD1 is involved in epigenetically silencing gene expression. LSD1 has been implicated as a potential therapeutic target in cancer and other diseases.
Philip A. Cole, Dawn Hayward
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Integrative analysis reveals histone demethylase LSD1 promotes RNA polymerase II pausing
iScience, 2022 Summary: Lysine-specific demethylase 1 (LSD1) is well-known for its role in decommissioning enhancers during mouse embryonic stem cell (ESC) differentiation.
Hani Jieun Kim +5 more
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The Deubiquitinase USP28 Stabilizes LSD1 and Confers Stem-Cell-like Traits to Breast Cancer Cells
Cell Reports, 2013 LSD1 is a critical chromatin modulator that controls cellular pluripotency and differentiation through the demethylation of H3K4me1/2. Overexpression of LSD1 has been observed in many types of tumors and is correlated with its oncogenic effects in ...
Yadi Wu +7 more
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