Development of secondary mutations in wild-type and mutant EZH2 alleles cooperates to confer resistance to EZH2 inhibitors.
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Targeting EZH2 in cancerPolycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination.Decreased ATF4 expression as a mechanism of acquired resistance to long-term amino acid limitation in cancer cellsIdentification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, SFunctional and therapeutic significance of EZH2 in urological cancersTargeting EZH2 and PRC2 dependence as novel anticancer therapy.Exploiting the Epigenome to Control Cancer-Promoting Gene-Expression Programs.Blocking EZH2 methylation transferase activity by GSK126 decreases stem cell-like myeloma cells.Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors.Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2.Targeting epigenetic regulators for cancer therapy: modulation of bromodomain proteins, methyltransferases, demethylases, and microRNAs.The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.Inhibitors of Protein Methyltransferases and Demethylases.Recently discovered EZH2 and EHMT2 (G9a) inhibitors.EZH2 inhibitors: a patent review (2014-2016).Role of the Polycomb Repressive Complex 2 (PRC2) in Transcriptional Regulation and Cancer.H3K27 Methylation: A Focal Point of Epigenetic Deregulation in Cancer.Drug discovery and therapeutic delivery for the treatment of B and T cell tumors.Targeting Enhancer of Zeste Homolog 2 as a promising strategy for cancer treatmentDeveloping EZH2-Targeted Therapy for Lung Cancer.Polycomb Repressor Complex 2 in Genomic Instability and CancerAlternative Splicing of EZH2 pre-mRNA by SF3B3 Contributes to the Tumorigenic Potential of Renal Cancer.Ezh2-dependent therapies in bladder cancer: synthetic lethality.WD40 repeat domain proteins: a novel target class?Structure, mechanism, and regulation of polycomb repressive complex 2.Initial testing (stage 1) of tazemetostat (EPZ-6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program.Chromatin biology: Breaking into the PRC2 cage.Allosteric Activation Dictates PRC2 Activity Independent of Its Recruitment to Chromatin.Protein kinase A-mediated phosphorylation regulates STAT3 activation and oncogenic EZH2 activity.Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells.Mechanisms of resistance to EZH2 inhibitors in diffuse large B-cell lymphomas.Phenotypic Plasticity, Bet-Hedging, and Androgen Independence in Prostate Cancer: Role of Non-Genetic Heterogeneity.An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
P2860
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P2860
Development of secondary mutations in wild-type and mutant EZH2 alleles cooperates to confer resistance to EZH2 inhibitors.
description
2015 nî lūn-bûn
@nan
2015年の論文
@ja
2015年学术文章
@wuu
2015年学术文章
@zh-cn
2015年学术文章
@zh-hans
2015年学术文章
@zh-my
2015年学术文章
@zh-sg
2015年學術文章
@yue
2015年學術文章
@zh
2015年學術文章
@zh-hant
name
Development of secondary mutat ...... resistance to EZH2 inhibitors.
@en
type
label
Development of secondary mutat ...... resistance to EZH2 inhibitors.
@en
prefLabel
Development of secondary mutat ...... resistance to EZH2 inhibitors.
@en
P2093
P2860
P356
P1433
P1476
Development of secondary mutat ...... resistance to EZH2 inhibitors
@en
P2093
A Q Hassan
P2860
P2888
P304
P356
10.1038/ONC.2015.114
P407
P50
P577
2015-04-20T00:00:00Z
P6179
1020679377