Recent advances in EZH2-based dual inhibitors in the treatment of cancers
X Yang, L Xu, L Yang - European journal of medicinal chemistry, 2023 - Elsevier
The enhancer of zeste homolog 2 (EZH2) protein is the catalytic subunit of one of the histone
methyltransferases. EZH2 catalyzes the trimethylation of lysine 27 of histone H3 …
methyltransferases. EZH2 catalyzes the trimethylation of lysine 27 of histone H3 …
Dual target PARP1/EZH2 inhibitors inducing excessive autophagy and producing synthetic lethality for triple-negative breast cancer therapy
X Li, C Wang, S Li, F Yin, H Luo, Y Zhang, Z Luo… - European journal of …, 2023 - Elsevier
Currently available PARP inhibitors are mainly used for the treatment of BRCA-mutated
triple-negative breast cancer (TNBC), with a narrow application range of approximately 15 …
triple-negative breast cancer (TNBC), with a narrow application range of approximately 15 …
Discovery of a new-generation S-Adenosylmethionine-noncompetitive covalent inhibitor targeting the lysine methyltransferase enhancer of zeste homologue 2
Y Zhang, H Yang, B Li, J Li, H Li, Q Shi… - Journal of Medicinal …, 2023 - ACS Publications
The first-generation enhancer of zeste homologue 2 (EZH2) inhibitors suffer from several
limitations, such as high dosage, cofactor S-adenosylmethionine (SAM) competition, and …
limitations, such as high dosage, cofactor S-adenosylmethionine (SAM) competition, and …
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors
Y Zhao, B Jiang, Z Gu, T Chen, W Yu, S Liu… - European Journal of …, 2023 - Elsevier
Post-translational methylation of histone lysine or arginine residues by histone
methyltransferases (HMTs) plays crucial roles in gene regulation and diverse physiological …
methyltransferases (HMTs) plays crucial roles in gene regulation and diverse physiological …
A patent review of EZH2 inhibitors from 2017 and beyond
G Wan, H Feng, C Su, Y Zhu, L Zhang… - Expert Opinion on …, 2023 - Taylor & Francis
Introduction EZH2 is an important epigenetic regulator that forms the PRC2 complex with
SUZ12, EED and RbAp46/48. As the key catalytic subunit of PRC2, EZH2 regulates the …
SUZ12, EED and RbAp46/48. As the key catalytic subunit of PRC2, EZH2 regulates the …
EZH2 serves as a promising therapeutic target for fibrosis
Q Zhang, YX Wu, XQ Yu, BY Zhang, LY Ma - Bioorganic Chemistry, 2023 - Elsevier
Fibrosis affects the function of many organs and tissues, and its persistent development can
lead to tissue sclerosis and cancer, even leading to death further. Recent studies suggested …
lead to tissue sclerosis and cancer, even leading to death further. Recent studies suggested …
Identification and characterization of the rat in-vivo and in-vitro metabolites of tazemetostat using LC-QTOF-MS
In drug discovery, metabolite profiling unveils biotransformation pathways and potential
toxicant formation, guiding selection of candidates with optimal pharmacokinetics and safety …
toxicant formation, guiding selection of candidates with optimal pharmacokinetics and safety …
Design, synthesis, and evaluation of VHL-based EZH2 degraders for breast cancer
B Xiao, Z Shi, J Liu, Q Huang, K Shu, F Liu, C Zhi… - Bioorganic …, 2024 - Elsevier
EZH2 (enhancer of zeste homolog 2) is one of the most important histone
methyltransferases (HMTs), and overexpression of EZH2 can lead to proliferation, migration …
methyltransferases (HMTs), and overexpression of EZH2 can lead to proliferation, migration …
Design, synthesis and activity evaluation of quinolinone derivatives as EZH2 inhibitors
J Cai, H You, X Qin, Y Wang, W Li - Bioorganic & Medicinal Chemistry …, 2024 - Elsevier
The enhancer of zeste homologue 2 (EZH2) is the core catalytic subunit of polycomb
repressive complex 2, which catalyzes lysine 27 methylation of histone H3. Herein, a series …
repressive complex 2, which catalyzes lysine 27 methylation of histone H3. Herein, a series …
[HTML][HTML] Cantharidin suppresses hepatocellular carcinoma development by regulating EZH2/H3K27me3-dependent cell cycle progression and antitumour immune …
J Yan, X Deng, S Ma, Y hui Li, Y Gao, G Shi… - … Medicine and Therapies, 2023 - Springer
Background Cantharidin (CTD) is a major ingredient of cantharis (Mylabris phalerata Pallas)
and has been used extensively in traditional Chinese medicines. It has been shown to …
and has been used extensively in traditional Chinese medicines. It has been shown to …