Epigenetic vulnerabilities of leukemia harboring inactivating EZH2 mutations

Epigenetic regulation encompasses the covalent modification of histone proteins, such as acetylation, phosphorylation, and ubiquitylation, resulting in the activation or inhibition of gene transcription and regulation of chromatin structure (1). Dysregulation of histone methylation is associated with various stages of carcinogenesis, including tumor initiation, promotion, and progression. Thus, targeting histone methyltransferases is being explored as a cancer therapeutic approach (2). The polycomb repressive complex 2 (PRC2), which is responsible for the mono-, di- and tri-methylation of histone 3 at lysine 27 promotes the compaction of the nucleosome and the repression of genes involved in development, cell differentiation, and proliferation (3).

Source: Experimental Hematology - December 8, 2023 Category: Hematology Authors: Mona A. Alqazzaz, Genna M. Luciani, Victoria Vu, Raquel Martinez Machado, Magdalena M. Szewczyk, Ella C. Adamson, Sehyun Cheon, Fengling Li, Cheryl H. Arrowsmith, Mark D. Minden, Dalia Barsyte-Lovejoy Tags: Article Source Type: research