[HTML][HTML] EZH2: a novel target for cancer treatment

R Duan, W Du, W Guo - Journal of hematology & oncology, 2020 - Springer
Enhancer of zeste homolog 2 (EZH2) is enzymatic catalytic subunit of polycomb repressive
complex 2 (PRC2) that can alter downstream target genes expression by trimethylation of …

EZH2-targeted therapies in cancer: hype or a reality

ML Eich, M Athar, JE Ferguson III, S Varambally - Cancer research, 2020 - AACR
Next-generation genomic sequencing has identified multiple novel molecular alterations in
cancer. Since the identification of DNA methylation and histone modification, it has become …

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

J Wang, X Yu, W Gong, X Liu, KS Park, A Ma… - Nature cell …, 2022 - nature.com
Canonically, EZH2 serves as the catalytic subunit of PRC2, which mediates H3K27me3
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 …

H3K27me3 conditions chemotolerance in triple-negative breast cancer

J Marsolier, P Prompsy, A Durand, AM Lyne… - Nature …, 2022 - nature.com
The persistence of cancer cells resistant to therapy remains a major clinical challenge. In
triple-negative breast cancer, resistance to chemotherapy results in the highest recurrence …

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

KP Bhat, H Ümit Kaniskan, J Jin… - Nature Reviews Drug …, 2021 - nature.com
Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …

Targeting EZH2 in cancer

KH Kim, CWM Roberts - Nature medicine, 2016 - nature.com
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 …

Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

S Pan, A Ding, Y Li, Y Sun, Y Zhan, Z Ye… - Chemical Society …, 2023 - pubs.rsc.org
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

EZH2 is a potential therapeutic target for H3K27M-mutant pediatric gliomas

F Mohammad, S Weissmann, B Leblanc, DP Pandey… - Nature medicine, 2017 - nature.com
Diffuse intrinsic pontine glioma (DIPG) is an aggressive brain tumor that is located in the
pons and primarily affects children. Nearly 80% of DIPGs harbor mutations in histone H3 …

Maintaining cell identity: PRC2-mediated regulation of transcription and cancer

I Comet, EM Riising, B Leblanc, K Helin - Nature Reviews Cancer, 2016 - nature.com
Enhancer of zeste homologue 2 (EZH2), the catalytic subunit of Polycomb repressive
complex 2 (PRC2), has attracted broad research attention in the past few years because of …