EZH2 inhibition and cisplatin as a combination anticancer therapy: an overview of preclinical studies

I Samaržija, M Tomljanović, R Novak Kujundžić… - Cancers, 2022 - mdpi.com
Simple Summary Cisplatin is a chemotherapy drug widely used in the treatment of different
cancer types. However, cisplatin displays a high range of toxicity and its use usually leads to …

Tumor-suppressive functions of protein lysine methyltransferases

N Aziz, YH Hong, HG Kim, JH Kim… - Experimental & Molecular …, 2023 - nature.com
Protein lysine methyltransferases (PKMTs) play crucial roles in histone and nonhistone
modifications, and their dysregulation has been linked to the development and progression …

Combating castration-resistant prostate cancer by co-targeting the epigenetic regulators EZH2 and HDAC

AE Schade, R Kuzmickas, CL Rodriguez, K Mattioli… - PLoS …, 2023 - journals.plos.org
While screening and early detection have reduced mortality from prostate cancer, castration-
resistant disease (CRPC) is still incurable. Here, we report that combined EZH2/HDAC …

Circulating tumor extracellular vesicles to monitor metastatic prostate cancer genomics and transcriptomic evolution

I Casanova-Salas, D Aguilar, S Cordoba-Terreros… - Cancer Cell, 2024 - cell.com
Extracellular vesicles (EVs) secreted by tumors are abundant in plasma, but their potential
for interrogating the molecular features of tumors through multi-omic profiling remains widely …

A cryptic transactivation domain of EZH2 binds AR and AR's splice variant, promoting oncogene activation and tumorous transformation

J Wang, KS Park, X Yu, W Gong, HS Earp… - Nucleic acids …, 2022 - academic.oup.com
Abstract Enhancer of Zeste Homolog 2 (EZH2) and androgen receptor (AR) are crucial
chromatin/gene regulators involved in the development and/or progression of prostate …

EZH2 directly methylates PARP1 and regulates its activity in cancer

Q Meng, J Shen, Y Ren, Q Liu, R Wang, Q Li… - Science …, 2024 - science.org
DNA repair dysregulation is a key driver of cancer development. Understanding the
molecular mechanisms underlying DNA repair dysregulation in cancer cells is crucial for …

Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers

PJ Keller, EJ Adams, R Wu, A Côté, S Arora… - Cancer …, 2024 - aacrjournals.org
Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin
remodeling complex subunit ARID1A occur frequently in advanced urothelial, endometrial …

Histone demethylase JMJD3 downregulation protects against aberrant force-induced osteoarthritis through epigenetic control of NR4A1

Y **, Z Liu, Z Li, H Li, C Zhu, R Li, T Zhou… - International journal of …, 2022 - nature.com
Osteoarthritis (OA) is a prevalent joint disease with no effective treatment strategies.
Aberrant mechanical stimuli was demonstrated to be an essential factor for OA …

[HTML][HTML] Discovery of a peptide proteolysis-targeting chimera (PROTAC) drug of p300 for prostate cancer therapy

D Zhang, B Ma, D Liu, W Wu, T Zhou, Y Gao, C Yang… - …, 2024 - thelancet.com
Summary Background The E1A-associated protein p300 (p300) has emerged as a
promising target for cancer therapy due to its crucial role in promoting oncogenic signaling …

Lineage-specific canonical and non-canonical activity of EZH2 in advanced prostate cancer subtypes

VB Venkadakrishnan, AG Presser, R Singh… - Nature …, 2024 - nature.com
Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and emerging
therapeutic target that is overexpressed in most castration-resistant prostate cancers and …