Acta Pharmaceutica Sinica B · 2019 · 79 citations · 44 references
MedicineMedicinal ChemistryPharmacologyDrug DiscoveryEpigeneticsMolecular PharmacologyCancer EpigeneticsChemical EpigeneticsEpigenetic Alterations In CancerEpigenetic Regulation In CancerHistone ModificationsPotency OptimizationAntiproliferative AgentsAntiproliferative Drug ActionHistone Demethylase InhibitionHistone DemethylasesHistone DemethylationHistone-lysine MethylationMedicinal Chemistry ApplicationsModulator Selectivity
induced expression of CD86 and CD11b in THP-1 cells, confirming its cellular activity and ability of inducing differentiation. The findings further indicate that targeting LSD1 is a promising strategy for AML treatment, the triazole-fused pyrimidine derivatives are new scaffolds for the development of LSD1/KDM1A inhibitors.
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The Determination of Enzyme Dissociation Constants
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Histone Demethylation Mediated by the Nuclear Amine Oxidase Homolog LSD1
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LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription
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DNMT3L connects unmethylated lysine 4 of histone H3 to de novo methylation of DNA
Steen K.T. Ooi, Chen Qiu, Emily Bernstein et al. · Nature · 2007 · 1.6K citations · Full text