Discovery of a first-in-class EZH2 selective degrader

EZH2 cooperates with gain‐of‐function p53 mutants to promote cancer growth and metastasis

(2019) Yu Zhao et al.   EMBO JOURNAL

Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation

(2019) Jia Yi Fong et al.   CANCER CELL

Involvement of both caspase-8 and Noxa-activated pathways in endoplasmic reticulum stress-induced apoptosis in triple-negative breast tumor cells

(2018) Ana Cano-González et al.   Cell Death & Disease

Polycomb- and Methylation-Independent Roles of EZH2 as a Transcription Activator

(2018) Jung Kim et al.   Cell Reports

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497)

(2017) Pei-Pei Kung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Salmon provides fast and bias-aware quantification of transcript expression

(2017) Rob Patro et al.   NATURE METHODS

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

Structure–Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors

(2016) Xiaobao Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

Targeting EZH2 in cancer

(2016) Kimberly H Kim et al.   NATURE MEDICINE

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Structural basis of oncogenic histone H3K27M inhibition of human polycomb repressive complex 2

(2016) Neil Justin et al.   Nature Communications

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

(2016) Alexei Brooun et al.   Nature Communications

Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells

(2015) Edward Curry et al.   Clinical Epigenetics

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

(2014) B. Xu et al.   BLOOD

Pharmacological targeting of the pseudokinase Her3

(2014) Ting Xie et al.   Nature Chemical Biology

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

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

DZNep, inhibitor of S-adenosylhomocysteine hydrolase, down-regulates expression of SETDB1 H3K9me3 HMTase in human lung cancer cells

(2013) Ju-Kyung Lee et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Pathview: an R/Bioconductor package for pathway-based data integration and visualization

(2013) Weijun Luo et al.   BIOINFORMATICS

Targeted disruption of the EZH2–EED complex inhibits EZH2-dependent cancer

(2013) Woojin Kim et al.   Nature Chemical Biology

The Cancer Genome Atlas Pan-Cancer analysis project

(2013) John N Weinstein et al.   NATURE GENETICS

Targeting the unfolded protein response in disease

(2013) Claudio Hetz et al.   NATURE REVIEWS DRUG DISCOVERY

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

(2013) S. K. Knutson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Clinicopathologic features, patterns of recurrence, and survival among women with triple-negative breast cancer in the National Comprehensive Cancer Network

(2012) Nancy U. Lin et al.   CANCER

Global H3K27 trimethylation and EZH2 abundance in breast tumor subtypes

(2012) Karolina Holm et al.   Molecular Oncology

Greasy tags for protein removal

(2012) Taavi K. Neklesa et al.   NATURE

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

EZH2 Oncogenic Activity in Castration-Resistant Prostate Cancer Cells Is Polycomb-Independent

(2012) K. Xu et al.   SCIENCE

Increased risk for distant metastasis in patients with familial early-stage breast cancer and high EZH2 expression

(2011) Sharon Hensley Alford et al.   BREAST CANCER RESEARCH AND TREATMENT

Triple-negative breast cancer in Hispanic patients

(2011) Fernando Lara-Medina et al.   CANCER

EZH2 Promotes Expansion of Breast Tumor Initiating Cells through Activation of RAF1-β-Catenin Signaling

(2011) Chun-Ju Chang et al.   CANCER CELL

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Triple-negative breast cancer--current status and future directions

(2009) O. Gluz et al.   ANNALS OF ONCOLOGY

GAGE: generally applicable gene set enrichment for pathway analysis

(2009) Weijun Luo et al.   BMC BIOINFORMATICS

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

CDKN1C (p57KIP2) Is a Direct Target of EZH2 and Suppressed by Multiple Epigenetic Mechanisms in Breast Cancer Cells

(2009) Xiaojing Yang et al.   PLoS One

Downregulation of EZH2 decreases growth of estrogen receptor-negative invasive breast carcinoma and requires BRCA1

(2008) M E Gonzalez et al.   ONCOGENE