4.5 Article

Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Review Chemistry, Medicinal

Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective

Thomas Webb et al.

Summary: Epigenetic modulators play a crucial role in gene expression and their dysregulation is associated with disease pathogenesis. Small molecule inhibitors targeting epigenetic proteins have limitations, but protein degraders can better exploit target druggability.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

Article Chemistry, Medicinal

Targeting EZH2 for cancer therapy: From current progress to novel strategies

Jia Zeng et al.

Summary: This article reviews the structure and biological functions of the EZH2 protein, as well as its relationship with various diseases. It also provides an overview of the current development of specific inhibitors for EZH2, and highlights the latest progress in new strategies such as drug combination, dual-target inhibitors, targeted protein degradation technology, and protein-protein interaction inhibitors.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas

Bin Zhou et al.

Summary: EZH2, the catalytic subunit of PRC2, is associated with various malignancies. A novel inhibitor 29 targeting EZH2 with high selectivity and potential therapeutic efficacy has been discovered. It shows promising pharmacokinetic properties and improved efficacy in mouse models, suggesting its potential as a therapeutic candidate for EZH2 mutant cancers.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

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

Zhihao Liu et al.

Summary: This study presents a novel strategy for treating cancer by targeting proteasomal degradation to block the oncogenic activity of EZH2, offering a new approach compared to current EZH2 inhibitors.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

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

Yalin Tu et al.

Summary: In this study, PROTAC-based EZH2 degraders were developed to target whole EZH2 in lymphoma, showing better therapeutic activity compared to traditional EZH2 inhibitors, especially in DLBCL. This research demonstrates the potential of EZH2 degraders as a promising anticancer strategy for treating lymphoma.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors

Hualong He et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

Article Pharmacology & Pharmacy

Tazemetostat: First Approval

Sheridan M. Hoy

Article Chemistry, Medicinal

Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer

M. Cynthia Martin et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Developmental Biology

PRC2 functions in development and congenital disorders

Orla Deevy et al.

DEVELOPMENT (2019)

Article Chemistry, Medicinal

Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays

Yunlong Wu et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016)

Article Chemistry, Medicinal

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

Kevin W. Kuntz et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Multidisciplinary Sciences

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

Alexei Brooun et al.

NATURE COMMUNICATIONS (2016)

Article Chemistry, Medicinal

Discovery, design, and synthesis of indole-based EZH2 inhibitors

Victor S. Gehling et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Article Chemistry, Medicinal

SAH derived potent and selective EZH2 inhibitors

Pei-Pei Kung et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Review Pharmacology & Pharmacy

Targeting histone lysine methylation in cancer

John McGrath et al.

PHARMACOLOGY & THERAPEUTICS (2015)

Article Chemistry, Medicinal

Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors

Jimin Woo et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)

Review Oncology

Regulation and Role of EZH2 in Cancer

Hirohito Yamaguchi et al.

CANCER RESEARCH AND TREATMENT (2014)

Review Multidisciplinary Sciences

Chromatin proteins and modifications as drug targets

Kristian Helin et al.

NATURE (2013)

Review Biochemistry & Molecular Biology

Cancer Epigenetics: From Mechanism to Therapy

Mark A. Dawson et al.

Article Biochemistry & Molecular Biology

A687V EZH2 is a gain-of-function mutation found in lymphoma patients

Christina R. Majer et al.

FEBS LETTERS (2012)

Article Multidisciplinary Sciences

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

Michael T. McCabe et al.

NATURE (2012)

Article Multidisciplinary Sciences

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Michael T. McCabe et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2012)

Article Biochemistry & Molecular Biology

The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states

Tim J. Wigle et al.

FEBS LETTERS (2011)

Review Multidisciplinary Sciences

The Polycomb complex PRC2 and its mark in life

Raphael Margueron et al.

NATURE (2011)

Article Multidisciplinary Sciences

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

Christopher J. Sneeringer et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2010)

Review Biotechnology & Applied Microbiology

Protein methyltransferases as a target class for drug discovery

Robert A. Copeland et al.

NATURE REVIEWS DRUG DISCOVERY (2009)

Review Biotechnology & Applied Microbiology

Roles of the EZH2 histone methyltransferase in cancer epigenetics

Jeffrey A. Simon et al.

MUTATION RESEARCH-FUNDAMENTAL AND MOLECULAR MECHANISMS OF MUTAGENESIS (2008)

Article Multidisciplinary Sciences

Role of histone H3 lysine 27 methylation in polycomb-group silencing

R Cao et al.

SCIENCE (2002)

Article Biochemistry & Molecular Biology

Histone methyltransferase activity of a Drosophila polycomb group repressor complex

J Müller et al.