Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Recent genomic studies have resulted in an emerging understanding of the role of
chromatin regulators in the development of cancer. EZH2, a histone methyl transferase …

Antagonism of protein–protein interactions (PPIs) with small molecules is becoming more
feasible as a therapeutic approach. Successful PPI inhibitors tend to target proteins …

Abstract Polycomb repressive complex 2 (PRC2) consists of three core subunits, EZH2, EED
and SUZ12, and plays pivotal roles in transcriptional regulation. The catalytic subunit EZH2 …

Summary Polycomb repressive complex 2 (PRC2) is composed of EED, SUZ12, and EZH1/2
and mediates mono-, di-, and trimethylation of histone H3 at lysine 27. At least two …

Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

Protein degradation via the use of bivalent chemical degraders provides an alternative
strategy to block protein function and assess the biological roles of putative drug targets …

Diffuse large B-cell lymphoma (DLBCL) is a highly heterogeneous disease and represents
the most common subtype of lymphoma. Although 60–70% of all patients can be cured by …

Dysregulation of the histone methyltransferase EZH2 plays a critical role in the development
of a variety of malignancies including B-cell lymphomas. As a result, a series of small …

Polycomb repressive complex 2 (PRC2) has been shown to play a major role in
transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3 …