Chemical probes targeting epigenetic proteins: Applications beyond oncology

scientific article

Chemical probes targeting epigenetic proteins: Applications beyond oncology is …
instance of (P31):
scholarly articleQ13442814
review articleQ7318358

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P356DOI10.1080/15592294.2017.1279371
P932PMC publication ID5453191
P698PubMed publication ID28080202

P50authorSusanne MüllerQ41781636
Peter J. BrownQ42713845
P2093author name stringSuzanne Ackloo
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The unfolded protein response in immunity and inflammationQ29248713
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A key role for autophagy and the autophagy gene Atg16l1 in mouse and human intestinal Paneth cellsQ29614565
Histone deacetylase inhibitors arrest polyglutamine-dependent neurodegeneration in DrosophilaQ29616737
Selective inhibition of tumor oncogenes by disruption of super-enhancersQ29617301
Protein arginine methyltransferase 6 enhances polyglutamine-expanded androgen receptor function and toxicity in spinal and bulbar muscular atrophy.Q30370542
Targeting the Bromome: are we there yet?Q30489777
Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferaseQ33272939
The Systemic Inflammatory Response Syndrome (SIRS) in acutely hospitalised medical patients: a cohort study.Q33589699
Regulation of NF-kappaB by NSD1/FBXL11-dependent reversible lysine methylation of p65.Q33591456
EZH2 is crucial for both differentiation of regulatory T cells and T effector cell expansionQ35758563
The TrxG Complex Mediates Cytokine Induced De Novo Enhancer Formation in IsletsQ35822529
The Role of H3K4me3 in Transcriptional Regulation Is Altered in Huntington's DiseaseQ35860836
Recent Progress in Histone Demethylase InhibitorsQ35879610
Barrier-to-Autointegration Factor influences specific histone modificationsQ35883260
Inhibition of KDM6 activity during murine ESC differentiation induces DNA damageQ35892322
Long noncoding RNA derived from CD244 signaling epigenetically controls CD8+ T-cell immune responses in tuberculosis infectionQ35895721
Inhibition of G9a methyltransferase stimulates fetal hemoglobin production by facilitating LCR/γ-globin loopingQ35904956
H3K27 Demethylation at the Proviral Promoter Sensitizes Latent HIV to the Effects of Vorinostat in Ex Vivo Cultures of Resting CD4+ T CellsQ35914266
Histone H4 acetylation and the epigenetic reader Brd4 are critical regulators of pluripotency in embryonic stem cellsQ35915213
Monomethylated and unmethylated FUS exhibit increased binding to Transportin and distinguish FTLD-FUS from ALS-FUS.Q35928701
Brd4 bridges the transcriptional regulators, Aire and P-TEFb, to promote elongation of peripheral-tissue antigen transcripts in thymic stromal cellsQ35961245
Epstein-Barr virus oncoprotein super-enhancers control B cell growthQ35963272
BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-CellQ35967957
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responsesQ36008355
Leveraging Cancer Therapeutics for the HIV Cure Agenda: Current Status and Future DirectionsQ36030989
EHMT1 and EHMT2 inhibition induces fetal hemoglobin expression.Q36169265
BET bromodomain inhibitors--a novel epigenetic approach in castration-resistant prostate cancerQ36211507
PRMT1 and PRMT4 Regulate Oxidative Stress-Induced Retinal Pigment Epithelial Cell Damage in SIRT1-Dependent and SIRT1-Independent Manners.Q36259933
Mutations in DNMT1 cause autosomal dominant cerebellar ataxia, deafness and narcolepsyQ36301666
Epigenetic regulation of MHC-II and CIITA genesQ36548065
BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in miceQ36575895
The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor StudiesQ36584337
Epigenetic Histone Modifications Involved in Profibrotic Gene Regulation by 12/15-Lipoxygenase and Its Oxidized Lipid Products in Diabetic NephropathyQ36656799
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine MethyltransferasesQ36703511
BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.Q36718203
Corepressor-dependent silencing of fetal hemoglobin expression by BCL11A.Q36781887
The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFbQ36790027
Asymmetric arginine dimethylation of RelA provides a repressive mark to modulate TNFα/NF-κB responseQ36831485
Proteomic dissection of LPS-inducible, PHF8-dependent secretome reveals novel roles of PHF8 in TLR4-induced acute inflammation and T cell proliferationQ36835605
BET Inhibition Attenuates Helicobacter pylori-Induced Inflammatory Response by Suppressing Inflammatory Gene Transcription and Enhancer Activation.Q36906022
Histone demethylases in physiology and cancer: a tale of two enzymes, JMJD3 and UTX.Q36936241
Promoter-enhancer looping at the PPARγ2 locus during adipogenic differentiation requires the Prmt5 methyltransferaseQ37021516
BET proteins promote efficient murine leukemia virus integration at transcription start sitesQ37031911
Reactivation of HIV latency by a newly modified Ingenol derivative via protein kinase Cδ-NF-κB signalingQ37041173
The H3K9 methyltransferase Setdb1 regulates TLR4-mediated inflammatory responses in macrophagesQ37044958
H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis.Q37073091
PRMT5 dimethylates R30 of the p65 subunit to activate NF-κB.Q37103890
Pyruvate dehydrogenase kinase regulates hepatitis C virus replication.Q37137222
Antiinflammatory effects of bromodomain and extraterminal domain inhibition in cystic fibrosis lung inflammationQ37161413
Protein arginine methylation facilitates KCNQ channel-PIP2 interaction leading to seizure suppressionQ37201261
The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs.Q39486701
Deletion of Polycomb Repressive Complex 2 From Mouse Intestine Causes Loss of Stem CellsQ39656702
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.Q39731654
Loss of the Brm-type SWI/SNF chromatin remodeling complex is a strong barrier to the Tat-independent transcriptional elongation of human immunodeficiency virus type 1 transcriptsQ39804456
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment HitQ39821089
The arginine methyltransferase PRMT5 regulates CIITA-dependent MHC II transcriptionQ39924470
Role of the histone H3 lysine 4 methyltransferase, SET7/9, in the regulation of NF-kappaB-dependent inflammatory genes. Relevance to diabetes and inflammationQ39957980
Super enhancers at the miR-146a and miR-155 genes contribute to self-regulation of inflammationQ40014974
Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.Q40173008
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical ProbeQ40400270
Activating and inhibitory functions for the histone lysine methyltransferase G9a in T helper cell differentiation and function.Q40463701
Inhibition of Super-Enhancer Activity in Autoinflammatory Site-Derived T Cells Reduces Disease-Associated Gene ExpressionQ40521055
BRD4 is associated with raccoon polyomavirus genome and mediates viral gene transcription and maintenance of a stem cell state in neuroglial tumour cellsQ40549858
DOT1L Activity Promotes Proliferation and Protects Cortical Neural Stem Cells from Activation of ATF4-DDIT3-Mediated ER Stress In VitroQ40615754
Targeting bromodomain-containing protein 4 (BRD4) benefits rheumatoid arthritisQ40817673
The Brd4 acetyllysine-binding protein is involved in activation of polyomavirus JC.Q40837175
Control of Paneth Cell Fate, Intestinal Inflammation, and Tumorigenesis by PKCλ/ι.Q41240523
pUL69 of Human Cytomegalovirus Recruits the Cellular Protein Arginine Methyltransferase 6 via a Domain That Is Crucial for mRNA Export and Efficient Viral ReplicationQ41583100
BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism.Q41641646
PRMT1 Upregulated by Epithelial Proinflammatory Cytokines Participates in COX2 Expression in Fibroblasts and Chronic Antigen-Induced Pulmonary Inflammation.Q41706711
NF-κB directs dynamic super enhancer formation in inflammation and atherogenesisQ41971115
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.Q42151914
Inhibition of H3K27me3-specific histone demethylases JMJD3 and UTX blocks reactivation of herpes simplex virus 1 in trigeminal ganglion neuronsQ42175829
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.Q42383290
Inhibition of Bromodomain and Extraterminal Domain Family Proteins Ameliorates Experimental Renal Damage.Q42496540
Therapeutic targeting of BET protein BRD4 delays murine lupusQ42700066
Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase-dependent NF-κB activation in rheumatoid fibroblast-like synoviocytesQ42700796
Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation.Q42701254
Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosisQ42710737
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitorsQ42713766
S-adenosylhomocysteine induces inflammation through NFkB: A possible role for EZH2 in endothelial cell activationQ43137066
From endoplasmic-reticulum stress to the inflammatory responseQ37225354
The endoplasmic reticulum stress response in immunity and autoimmunityQ37231726
Methyltransferase and demethylase profiling studies during brown adipocyte differentiation.Q37274144
Bromo- and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integrationQ37336436
Arginine methylation increases the stability of human immunodeficiency virus type 1 Tat.Q37410634
The NF-kappaB factor RelB and histone H3 lysine methyltransferase G9a directly interact to generate epigenetic silencing in endotoxin toleranceQ37459848
Targeting BET bromodomain proteins in solid tumorsQ37619860
S6K1 Phosphorylation of H2B Mediates EZH2 Trimethylation of H3: A Determinant of Early AdipogenesisQ37666046
Epigenetic chemical probes.Q38055063
Lost in transcription: molecular mechanisms that control HIV latencyQ38091888
Transcriptional control by NF-κB: elongation in focusQ38102509
Discovery of a PCAF Bromodomain Chemical ProbeQ38434399
Immune attack: the role of inflammation in Alzheimer disease.Q38492631
Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidenceQ38542092
Specific regulation of PRMT1 expression by PIAS1 and RKIP in BEAS-2B epithelia cells and HFL-1 fibroblasts in lung inflammation.Q38622162
Bromodomains: Structure, function and pharmacology of inhibitionQ38680455
PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and DiseaseQ38719854
Arginine methylation enhances the RNA chaperone activity of the West Nile virus host factor AUF1 p45.Q38752143
BET inhibitors in cancer therapeutics: a patent reviewQ38753987
BRD7 plays an anti-inflammatory role during early acute inflammation by inhibiting activation of the NF-кB signaling pathwayQ38760091
Citrullination-acetylation interplay guides E2F-1 activity during the inflammatory responseQ38785264
Histone H3K27 Demethylase JMJD3 in Cooperation with NF-κB Regulates Keratinocyte Wound Healing.Q38800102
PDGF-BB induces PRMT1 expression through ERK1/2 dependent STAT1 activation and regulates remodeling in primary human lung fibroblasts.Q38800830
Glucose-induced expression of the homeotic transcription factor Prep1 is associated with histone post-translational modifications in skeletal muscleQ38829133
BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory ResponsesQ38849159
Using sequential immunoprecipitation and mass spectrometry to identify methylation of NF-κB.Q38903969
Set7 facilitates hepatitis C virus replication via enzymatic activity-dependent attenuation of the IFN-related pathway.Q38909782
The Epigenetic Reader BRD2 as a Specific Modulator of PAI-1 Expression in Lipopolysaccharide-Stimulated Mouse Primary AstrocytesQ38945469
KATapulting toward Pluripotency and CancerQ38976614
Methyltransferase G9A regulates T cell differentiation during murine intestinal inflammationQ38997053
Overexpression of PRMT6 does not suppress HIV-1 Tat transactivation in cells naturally lacking PRMT6.Q39135199
Single-cell dynamics of genome-nuclear lamina interactionsQ39176932
Control of proinflammatory gene programs by regulated trimethylation and demethylation of histone H4K20.Q39291348
UTX-1 regulates Tat-induced HIV-1 transactivation via changing the methylated status of histone H3.Q39348883
Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell diseaseQ33628389
Brd2 disruption in mice causes severe obesity without Type 2 diabetesQ33642463
Role of LDB1 in the transition from chromatin looping to transcription activation.Q33789575
Involvement of histone H3 lysine 9 (H3K9) methyltransferase G9a in the maintenance of HIV-1 latency and its reactivation by BIX01294.Q33883423
Lysine-specific demethylase 1 is a therapeutic target for fetal hemoglobin inductionQ33907537
BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction.Q33936571
A gain-of-function mouse model identifies PRMT6 as a NF-κB coactivatorQ33983567
BET bromodomain inhibition as a novel strategy for reactivation of HIV-1Q34032827
RNA polymerase II stalling promotes nucleosome occlusion and pTEFb recruitment to drive immortalization by Epstein-Barr virusQ34064221
The art of the chemical probeQ34098693
The cellular bromodomain protein Brd4 has multiple functions in E2-mediated papillomavirus transcription activationQ34102298
Identification of a PRMT5-dependent repressor complex linked to silencing of human fetal globin gene expressionQ34124980
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cellsQ34144669
Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitorsQ34295282
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cellsQ34302726
BET bromodomain inhibition suppresses TH17-mediated pathologyQ34375887
Epigenetic drugs against cancer: an evolving landscapeQ34431964
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.Q34479551
The promise and peril of chemical probesQ34486195
Recruitment of Brd4 to the human papillomavirus type 16 DNA replication complex is essential for replication of viral DNA.Q34568110
Epigenetic heterogeneity in HIV-1 latency establishmentQ34877762
Specific interaction between genotype, smoking and autoimmunity to citrullinated alpha-enolase in the etiology of rheumatoid arthritisQ35011877
The histone methyltransferase Smyd2 is a negative regulator of macrophage activation by suppressing interleukin 6 (IL-6) and tumor necrosis factor α (TNF-α) productionQ35126599
Cyclin-dependent kinase 1 (CDK1)-mediated phosphorylation of enhancer of zeste 2 (Ezh2) regulates its stabilityQ35150248
Epigenetic silencing of HIV-1 by the histone H3 lysine 27 methyltransferase enhancer of Zeste 2.Q35192959
Inhibiting STAT5 by the BET bromodomain inhibitor JQ1 disrupts human dendritic cell maturationQ35205506
Transcriptional activity of the islet β cell factor Pdx1 is augmented by lysine methylation catalyzed by the methyltransferase Set7/9.Q35352055
BET bromodomain inhibition suppresses graft-versus-host disease after allogeneic bone marrow transplantation in miceQ35533619
Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.Q35549296
CXCL8 histone H3 acetylation is dysfunctional in airway smooth muscle in asthma: regulation by BETQ35574709
Repression of hypoxia-inducible factor α signaling by Set7-mediated methylationQ35610555
Histone demethylation maintains Prdm14 and Tsix expression and represses xIst in embryonic stem cellsQ35629117
The HIV-1 Tat transactivator protein: a therapeutic target?Q35652191
Transcriptomic Profiling and H3K27me3 Distribution Reveal Both Demethylase-Dependent and Independent Regulation of Developmental Gene Transcription in Cell Differentiation.Q35742850
P275copyright licenseCreative Commons Attribution-NonCommercial-NoDerivs 4.0 InternationalQ24082749
P433issue5
P921main subjectenzymeQ8047
nucleoproteinQ419245
transport proteinQ2111029
epigenomicsQ3589153
small molecule librariesQ50573438
nuclear proteinQ16860021
P304page(s)378-400
P577publication date2017-01-12
2017-05-04
P1433published inEpigeneticsQ15753739
P1476titleChemical probes targeting epigenetic proteins: Applications beyond oncology
P478volume12

Reverse relations

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Q88160150Epigenetics of Skeletal Diseases
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