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

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 …

In recent decades, the development of targeted drugs has featured prominently in the
treatment of cancer, which is among the major causes of mortality globally. Triazole-fused …

Abstract Polycomb repressive complex 2 (PRC2) is a key epigenetic multiprotein complex
involved in the regulation of gene expression in metazoans. PRC2 is formed by a tetrameric …

PRC2 is a therapeutic target for several types of cancers currently undergoing clinical trials.
Its activity is regulated by a positive feedback loop whereby its terminal enzymatic product …

All major biological macromolecules (DNA, RNA, proteins and lipids) undergo enzyme-
catalysed covalent modifications that impact their structure, function and stability. A variety of …

Epigenetic processes are essential for normal development and the maintenance of tissue-
specific gene expression in mammals. Changes in gene expression and malignant cellular …

Polycomb Repressive Complex 2 (PRC2) plays an important role in transcriptional
regulation during animal development and in cell differentiation, and alteration of PRC2 …

Enhancer of zeste homolog 2 (EZH2), the catalytic subunit of the Polycomb repressive
complex 2 (PRC2), catalyzes the methylation of lysine 27 of histone H3 (H3K27) up to its …

EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which along
with other PRC2 components mediates gene expression suppression via the methylation of …