Discovery of precision targeting EZH2 degraders for triple-negative breast cancer

Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2

(2021) Zhihao Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

(2021) Yalin Tu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for Triple-Negative Breast Cancer with Wild-Type BRCA

(2021) Cheng Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polycomb Repressive Complex 2 Modulation through the Development of EZH2–EED Interaction Inhibitors and EED Binders

(2021) Stefano Tomassi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease

(2021) Lailiang Qu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

EZH2 Inhibition Sensitizes CARM1-High, Homologous Recombination Proficient Ovarian Cancers to PARP Inhibition

(2020) Sergey Karakashev et al.   CANCER CELL

Insights into Molecular Classifications of Triple-Negative Breast Cancer: Improving Patient Selection for Treatment

(2019) Ana C. Garrido-Castro et al.   Cancer Discovery

Breast Cancer Treatment

(2019) Adrienne G. Waks et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Discovery of a first-in-class EZH2 selective degrader

(2019) Anqi Ma et al.   Nature Chemical Biology

CARM1-expressing ovarian cancer depends on the histone methyltransferase EZH2 activity

(2018) Sergey Karakashev et al.   Nature Communications

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

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Waste disposal—An attractive strategy for cancer therapy

(2017) Jemilat Salami et al.   SCIENCE

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

Targeting EZH2 in cancer

(2016) Kimberly H Kim et al.   NATURE MEDICINE

Triple-negative breast cancer: challenges and opportunities of a heterogeneous disease

(2016) Giampaolo Bianchini et al.   Nature Reviews Clinical Oncology

Induced protein degradation: an emerging drug discovery paradigm

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

SWI/SNF-mutant cancers depend on catalytic and non-catalytic activity of EZH2

(2015) Kimberly H Kim et al.   NATURE MEDICINE

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

(2015) Edward Curry et al.   Clinical Epigenetics

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

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

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

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

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

Ezh1 and Ezh2 Maintain Repressive Chromatin through Different Mechanisms

(2008) Raphael Margueron et al.   MOLECULAR CELL