Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
about
PHF8, a gene associated with cleft lip/palate and mental retardation, encodes for an Nepsilon-dimethyl lysine demethylaseScreening chelating inhibitors of HIF-prolyl hydroxylase domain 2 (PHD2) and factor inhibiting HIF (FIH)Design of small molecule epigenetic modulatorsThe role of histone demethylases in cancer therapy8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase InhibitorsCrystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylaseSelective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic ApproachesQuantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase InhibitorsInhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl CompoundsThe oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylasesStructural and Evolutionary Basis for the Dual Substrate Selectivity of Human KDM4 Histone Demethylase FamilyLinking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylasesPlant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone DemethylasesA High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase ScreeningSubstituted 2-(2-aminopyrimidin-4-yl)pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone demethylasesDevelopment and application of a fluoride-detection-based fluorescence assay for γ-butyrobetaine hydroxylaseInhibition of 2-oxoglutarate dependent oxygenasesOpen access target validation is a more efficient way to accelerate drug discoveryImposing function down a (cupin)-barrel: secondary structure and metal stereochemistry in the αKG-dependent oxygenases.A miniaturized screen for inhibitors of Jumonji histone demethylases.Development of homogeneous luminescence assays for histone demethylase catalysis and binding.The small molecule JIB-04 disrupts O2 binding in the Fe-dependent histone demethylase KDM4A/JMJD2A.A photoreactive small-molecule probe for 2-oxoglutarate oxygenases.Computational methods for de novo protein design and its applications to the human immunodeficiency virus 1, purine nucleoside phosphorylase, ubiquitin specific protease 7, and histone demethylases.Chemical and biochemical approaches in the study of histone methylation and demethylationMethods for Activity Analysis of the Proteins that Regulate Histone MethylationIdentification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.Epigenetics of prostate cancer and the prospect of identification of novel drug targets by RNAi screening of epigenetic enzymes.Configuration of a high-content imaging platform for hit identification and pharmacological assessment of JMJD3 demethylase enzyme inhibitors.Small-molecule-based inhibition of histone demethylation in cells assessed by quantitative mass spectrometry.Perspectives on the discovery of small-molecule modulators for epigenetic processes.Targeting histone lysine demethylases - progress, challenges, and the futureKDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor.Arginine demethylation is catalysed by a subset of JmjC histone lysine demethylasesSmall-molecular modulators of cancer-associated epigenetic mechanisms.A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth.Targeting protein lysine methylation and demethylation in cancers.Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells.Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.Targeting epigenetic regulations in cancer
P2860
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P2860
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
description
2008 nî lūn-bûn
@nan
2008 թուականի Նոյեմբերին հրատարակուած գիտական յօդուած
@hyw
2008 թվականի նոյեմբերին հրատարակված գիտական հոդված
@hy
2008年の論文
@ja
2008年論文
@yue
2008年論文
@zh-hant
2008年論文
@zh-hk
2008年論文
@zh-mo
2008年論文
@zh-tw
2008年论文
@wuu
name
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@ast
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@en
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@nl
type
label
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@ast
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@en
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@nl
prefLabel
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@ast
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@en
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@nl
P2093
P50
P3181
P356
P1476
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
@en
P2093
Benoît M R Liénard
Jasmin Mecinović
Simon H Bello
Stanley S Ng
P304
P3181
P356
10.1021/JM800936S
P407
P577
2008-11-27T00:00:00Z