[HTML][HTML] Targeting EZH2 and PRC2 dependence as novel anticancer therapy

B Xu, KD Konze, J Jin, GG Wang - Experimental hematology, 2015 - Elsevier
Distinctive patterns of chromatin modification control gene expression and define cellular
identity during development and cell differentiation. Polycomb repressive complex 2 (PRC2) …

Multiple histone lysine methyltransferases are required for the establishment and maintenance of HIV-1 latency

K Nguyen, B Das, C Dobrowolski, J Karn - MBio, 2017 - Am Soc Microbiol
We showed previously that the histone lysine methyltransferase (HKMT) H3K27me3 (EZH2)
is the catalytic subunit of Polycomb repressive complex 2 (PRC2) and is required for the …

Regulation of EZH2 protein stability: new mechanisms, roles in tumorigenesis, and roads to the clinic

Y Guo, R Cheng, Y Wang, ME Gonzalez, H Zhang… - …, 2024 - thelancet.com
The importance of EZH2 as a key methyltransferase has been well documented
theoretically. Practically, the first EZH2 inhibitor Tazemetostat (EPZ6438), was approved by …

Small molecule approaches for targeting the polycomb repressive complex 2 (PRC2) in cancer

MC Martin, G Zeng, J Yu, GE Schiltz - Journal of Medicinal …, 2020 - ACS Publications
The polycomb repressive complex 2 (PRC2) is composed of three core subunits, enhancer
of zeste 2 (EZH2), embryonic ectoderm development (EED), and suppressor of zeste 12 …

Polycomb repressive complex 2 modulation through the development of EZH2–EED interaction inhibitors and EED binders

S Tomassi, A Romanelli, C Zwergel… - Journal of Medicinal …, 2021 - ACS Publications
Epigenetics is nowadays a well-accepted area of research. In the last years, tremendous
progress was made regarding molecules targeting EZH2, directly or indirectly. Recently …

MDM2 associates with polycomb repressor complex 2 and enhances stemness-promoting chromatin modifications independent of p53

M Wienken, A Dickmanns, A Nemajerova, D Kramer… - Molecular cell, 2016 - cell.com
The MDM2 oncoprotein ubiquitinates and antagonizes p53 but may also carry out p53-
independent functions. Here we report that MDM2 is required for the efficient generation of …

Acetylation of VGLL4 regulates Hippo-YAP signaling and postnatal cardiac growth

Z Lin, H Guo, Y Cao, S Zohrabian, P Zhou, Q Ma… - Developmental cell, 2016 - cell.com
Binding of the transcriptional co-activator YAP with the transcription factor TEAD stimulates
growth of the heart and other organs. YAP overexpression potently stimulates fetal …

[HTML][HTML] Re-patterning of H3K27me3, H3K4me3 and DNA methylation during fibroblast conversion into induced cardiomyocytes

Z Liu, O Chen, M Zheng, L Wang, Y Zhou, C Yin, J Liu… - Stem cell …, 2016 - Elsevier
Direct conversion of fibroblasts into induced cardiomyocytes (iCMs) offers an alternative
strategy for cardiac disease modeling and regeneration. During iCM reprogramming, the …

EZH2 in cancer progression and potential application in cancer therapy: a friend or foe?

KS Yan, CY Lin, TW Liao, CM Peng, SC Lee… - International journal of …, 2017 - mdpi.com
Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, catalyzes tri-methylation
of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic …

Inhibition of enhancer of zeste homolog 2 (EZH2) overcomes enzalutamide resistance in castration-resistant prostate cancer

Y Bai, Z Zhang, L Cheng, R Wang, X Chen… - Journal of Biological …, 2019 - ASBMB
Enzalutamide, approved by the United States Food and Drug Administration in 2018 for the
management of metastatic castration-resistant prostate cancer (CRPC), is an androgen …