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Discovery of a first-in-class EZH2 selective degrader

A hydrophobic tagging method is used to develop a selective degrader for the chromatin regulator EZH2, which inhibits proliferation of triple-negative breast cancer cell lines in vitro and in vivo.

Anqi Ma
Elias Stratikopoulos
Jian Jin
Research09 Dec 2019
Nature Chemical Biology

Volume: 16, P: 214-222
Development of a brain-penetrant G9a methylase inhibitor to target Alzheimer’s disease-associated proteopathology

The authors describe a new mechanism of AD pathogenesis in which the histone methylase G9a regulates translation of hippocampal proteins associated with AD pathology. Targeting this mechanism with a brain-penetrant inhibitor of G9a helped rescue brain pathology in AD mouse models.

Ling Xie
Ryan N. Sheehy
Xian Chen
ResearchOpen Access07 May 2025
Nature Communications

Volume: 16, P: 1-18
EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis

Wang et al. reveal a noncanonical mechanism for EZH2 in binding the oncoprotein cMyc to promote tumorigenesis, and develop a small-molecule degrader, MS177, to target both canonical and noncanonical functions of EZH2 to suppress tumour growth.

Jun Wang
Xufen Yu
Gang Greg Wang
Research24 Feb 2022
Nature Cell Biology

Volume: 24, P: 384-399
Advancing targeted protein degradation for cancer therapy

The development of small-molecule degraders such as proteolysis-targeting chimeras (PROTACs) has made it possible to target oncoproteins previously considered undruggable. This Review discusses recent advances in the field, with a focus on opportunities and challenges for future development.

Brandon Dale
Meng Cheng
Jian Jin
Reviews15 Jun 2021
Nature Reviews Cancer

Volume: 21, P: 638-654
Complete chloroplast and ribosomal sequences for 30 accessions elucidate evolution of Oryza AA genome species

Kyunghee Kim
Sang-Choon Lee
Tae-Jin Yang
ResearchOpen Access28 Oct 2015
Scientific Reports

Volume: 5, P: 1-13

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Discovery of a first-in-class EZH2 selective degrader

Development of a brain-penetrant G9a methylase inhibitor to target Alzheimer’s disease-associated proteopathology

EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis

Advancing targeted protein degradation for cancer therapy

Complete chloroplast and ribosomal sequences for 30 accessions elucidate evolution of Oryza AA genome species

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