Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia

scientific article

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1182/BLOOD-2014-06-581082
P932PMC publication ID4287641
P698PubMed publication ID25395428
P5875ResearchGate publication ID268280999

P50authorGang G WangQ80521785
Deyou ZhengQ37390105
P2093author name stringMasoud Vedadi
Benjamin A Garcia
Fengling Li
Ying Liu
Shichong Liu
Stephen V Frye
Jian Jin
Ling Cai
Samantha G Pattenden
Shira Rockowitz
Anqi Ma
Bowen Xu
David F Allison
Doan M On
Kyle D Konze
Trevor Parton
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Ectopic expression of the histone methyltransferase Ezh2 in haematopoietic stem cells causes myeloproliferative disease.Q50594569
Ezh2 augments leukemogenicity by reinforcing differentiation blockage in acute myeloid leukemia.Q50803016
Dependency on the polycomb gene Ezh2 distinguishes fetal from adult hematopoietic stem cells.Q54341375
A transgenic mouse model demonstrating the oncogenic role of mutations in the polycomb-group gene EZH2 in lymphomagenesisQ57261238
Ezh1 Is Required for Hematopoietic Stem Cell Maintenance and Prevents Senescence-like Cell Cycle ArrestQ60033499
Switching on epigenetic therapyQ82223266
Selective inhibition of BET bromodomainsQ24301009
An H3K36 methylation-engaging Tudor motif of polycomb-like proteins mediates PRC2 complex targetingQ24307370
Covalent histone modifications--miswritten, misinterpreted and mis-erased in human cancersQ24605342
EZH1 mediates methylation on histone H3 lysine 27 and complements EZH2 in maintaining stem cell identity and executing pluripotencyQ24645960
Haematopoietic malignancies caused by dysregulation of a chromatin-binding PHD fingerQ27655436
Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic MutationsQ27681082
Structural Context of Disease-Associated Mutations and Putative Mechanism of Autoinhibition Revealed by X-Ray Crystallographic Analysis of the EZH2-SET DomainQ27681087
Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center originQ27851546
The language of covalent histone modificationsQ27860931
Histone methylation: a dynamic mark in health, disease and inheritanceQ28263573
Distinct factors control histone variant H3.3 localization at specific genomic regionsQ28275277
The Polycomb complex PRC2 and its mark in lifeQ29547358
Cancer epigenetics: from mechanism to therapyQ29614799
MLL translocations, histone modifications and leukaemia stem-cell developmentQ29615368
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutationsQ29615392
Cancer epigenomics: DNA methylomes and histone-modification mapsQ29615524
Epigenetic protein families: a new frontier for drug discoveryQ29616621
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemiaQ29617201
Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.Q33716402
Quantitative mass spectrometry of histones H3.2 and H3.3 in Suz12-deficient mouse embryonic stem cells reveals distinct, dynamic post-translational modifications at Lys-27 and Lys-36Q33854968
The Polycomb complex PRC2 supports aberrant self-renewal in a mouse model of MLL-AF9;Nras(G12D) acute myeloid leukemia.Q33915185
Polycomb repressor complex 2 regulates HOXA9 and HOXA10, activating ID2 in NK/T-cell linesQ33951701
Examining histone posttranslational modification patterns by high-resolution mass spectrometryQ33978003
Chromatin immunoprecipitation and microarray-based analysis of protein locationQ34003310
DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation.Q34017960
The role of mutations in epigenetic regulators in myeloid malignanciesQ34033164
Chromatin proteins and modifications as drug targetsQ34038652
Characterization of an antagonistic switch between histone H3 lysine 27 methylation and acetylation in the transcriptional regulation of Polycomb group target genesQ34080062
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cellsQ34302726
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferationQ34317380
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1Q34341058
Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomasQ34397318
Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cellsQ34619655
Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growthQ35030824
Inhibition of histone methyltransferase EZH2 depletes leukemia stem cell of mixed lineage leukemia fusion leukemia through upregulation of p16.Q35051547
Polycomb repressive complex 2 is required for MLL-AF9 leukemiaQ35882496
Ezh1 and Ezh2 maintain repressive chromatin through different mechanismsQ36810306
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.Q36835530
EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformationQ36926825
The molecular biology of mixed lineage leukemiaQ37522825
Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphomaQ39021479
DZNep, inhibitor of S-adenosylhomocysteine hydrolase, down-regulates expression of SETDB1 H3K9me3 HMTase in human lung cancer cellsQ39112529
P433issue2
P407language of work or nameEnglishQ1860
P921main subjectleukemiaQ29496
P1104number of pages12
P304page(s)346-357
P577publication date2014-11-13
P1433published inBloodQ885070
P1476titleSelective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia
P478volume125

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