Epigenetics-targeted drugs: current paradigms and future challenges

W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …

The roles of EZH2 in cancer and its inhibitors

Y Liu, Q Yang - Medical Oncology, 2023 - Springer
The enhancer of zeste homolog 2 (EZH2) is encoded by the Enhancer of zeste 2 polycomb
repressive complex 2 subunit gene. EZH2 is involved in the cell cycle, DNA damage repair …

DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic-and acquired-degrader resistance

M Schröder, M Renatus, X Liang, F Meili… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …

Triazole-fused pyrimidines in target-based anticancer drug discovery

XJ Dai, LP Xue, SK Ji, Y Zhou, Y Gao, YC Zheng… - European Journal of …, 2023 - Elsevier
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 …

Epigenetic therapies targeting histone lysine methylation: complex mechanisms and clinical challenges

S Gold, A Shilatifard - The Journal of Clinical Investigation, 2024 - jci.org
As epigenetic therapies continue to gain ground as potential treatment strategies for cancer
and other diseases, compounds that target histone lysine methylation and the enzyme …

Epigenetic regulation of bone remodeling and bone metastasis

G Sharma, A Sultana, KM Abdullah, R Pothuraju… - Seminars in Cell & …, 2024 - Elsevier
Bone remodeling is a continuous and dynamic process of bone formation and resorption to
maintain its integrity and homeostasis. Bone marrow is a source of various cell lineages …

EZH2: an accomplice of gastric cancer

W Yu, N Liu, X Song, L Chen, M Wang, G Xiao, T Li… - Cancers, 2023 - mdpi.com
Simple Summary Enhancer of zeste homolog 2 (EZH2) modifies the trimethylation of Lys-27
of histone 3, affecting downstream target genes' expression. It was reported that EZH2 is …

[HTML][HTML] Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs

Q Liao, J Yang, S Ge, P Chai, J Fan, R Jia - Journal of Pharmaceutical …, 2023 - Elsevier
The reversible and precise temporal and spatial regulation of histone lysine
methyltransferases (KMTs) is essential for epigenome homeostasis. The dysregulation of …

Structure-Based Design of the Indole-Substituted Triazolopyrimidines as New EED–H3K27me3 Inhibitors for the Treatment of Lymphoma

G Dong, J Zuo, J Yu, J Xu, G Gao, GB Li… - Journal of Medicinal …, 2022 - ACS Publications
Interrupting the embryonic ectoderm development (EED)–H3K27me3 interaction represents
a promising strategy to allosterically inhibit polycomb repressive complex 2 (PRC2) for …

Nicardipine is a putative EED inhibitor and has high selectivity and potency against chemoresistant prostate cancer in preclinical models

X Li, Y Chen, L Bai, R Zhao, Y Wu, ZR Xie… - British Journal of …, 2023 - nature.com
Background It is imperative to develop novel therapeutics to overcome chemoresistance, a
significant obstacle in the clinical management of prostate cancer (PCa) and other cancers …