Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells

Identification 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, Suitable for Phase I Clinical Trials for B-Cell Lymphomas

(2016) Rishi G. Vaswani et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

(2016) Kevin W. Kuntz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Uveal melanoma cells are resistant to EZH2 inhibition regardless of BAP1 status

(2016) Marie Schoumacher et al.   NATURE MEDICINE

Targeting EZH2 in cancer

(2016) Kimberly H Kim et al.   NATURE MEDICINE

Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

(2016) Alexei Brooun et al.   Nature Communications

S-Adenosyl-L-methionine-competitive inhibitors of the histone methyltransferase EZH2 induce autophagy and enhance drug sensitivity in cancer cells

(2015) Tsang-Pai Liu et al.   ANTI-CANCER DRUGS

Epigenetic regulation of autophagy by the methyltransferase EZH2 through an MTOR-dependent pathway

(2015) Fu-Zheng Wei et al.   Autophagy

Targeting EZH2 and PRC2 dependence as novel anticancer therapy

(2015) Bowen Xu et al.   EXPERIMENTAL HEMATOLOGY

ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors

(2015) Ping Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

Development of secondary mutations in wild-type and mutant EZH2 alleles cooperates to confer resistance to EZH2 inhibitors

(2015) V Gibaja et al.   ONCOGENE

Pharmacological inhibition of EZH2 as a promising differentiation therapy in embryonal RMS

(2014) Roberta Ciarapica et al.   BMC CANCER

EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells

(2014) Bryson W Katona et al.   CANCER BIOLOGY & THERAPY

An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1

(2013) Kyle D. Konze et al.   ACS Chemical Biology

The Polycomb group (PcG) protein EZH2 supports the survival of PAX3-FOXO1 alveolar rhabdomyosarcoma by repressing FBXO32 (Atrogin1/MAFbx)

(2013) R Ciarapica et al.   ONCOGENE

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

(2012) Sergio Valente et al.   BIOCHIMIE

Identification of Small-Molecule Enhancers of Arginine Methylation Catalyzed by Coactivator-Associated Arginine Methyltransferase 1

(2012) Sabrina Castellano et al.   JOURNAL OF MEDICINAL CHEMISTRY

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

(2012) Michael T. McCabe et al.   NATURE

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

(2012) Sarah K Knutson et al.   Nature Chemical Biology

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

(2012) Sharad K. Verma et al.   ACS Medicinal Chemistry Letters

Novel 3,5-Bis(bromohydroxybenzylidene)piperidin-4-ones as Coactivator-Associated Arginine Methyltransferase 1 Inhibitors: Enzyme Selectivity and Cellular Activity

(2011) Donghang Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

TNF/p38α/Polycomb Signaling to Pax7 Locus in Satellite Cells Links Inflammation to the Epigenetic Control of Muscle Regeneration

(2010) Daniela Palacios et al.   Cell Stem Cell

Polycomb Group Proteins: Multi-Faceted Regulators of Somatic Stem Cells and Cancer

(2010) Martin Sauvageau et al.   Cell Stem Cell

Polycomb-like 2 Associates with PRC2 and Regulates Transcriptional Networks during Mouse Embryonic Stem Cell Self-Renewal and Differentiation

(2010) Emily Walker et al.   Cell Stem Cell

Design, Synthesis and Biological Evaluation of Carboxy Analogues of Arginine Methyltransferase Inhibitor 1 (AMI-1)

(2010) Sabrina Castellano et al.   ChemMedChem

Jarid2 and PRC2, partners in regulating gene expression

(2010) G. Li et al.   GENES & DEVELOPMENT

DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation

(2009) T. B. Miranda et al.   MOLECULAR CANCER THERAPEUTICS

AEBP2 as a potential targeting protein for Polycomb Repression Complex PRC2

(2009) Hana Kim et al.   NUCLEIC ACIDS RESEARCH

Epigenetic Multiple Ligands: Mixed Histone/Protein Methyltransferase, Acetyltransferase, and Class III Deacetylase (Sirtuin) Inhibitors

(2008) Antonello Mai et al.   JOURNAL OF MEDICINAL CHEMISTRY