Article
Chemistry, Medicinal
Bin Zhou, Beilei Wang, Fengming Zou, Husheng Mei, Qingwang Liu, Shuang Qi, Wenliang Wang, Rui Jin, Aoli Wang, Yongfei Chen, Feiyang Liu, Wenchao Wang, Jing Liu, Qingsong Liu
Summary: A novel covalent EZH2 degrader was discovered, which can reduce the expression of EZH2 in multiple types of cancer and exhibit antiproliferation activity. This study provides an opportunity for the development of new drug candidates.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Medicine, Research & Experimental
Mahshid Deldar Abad Paskeh, Atefeh Mehrabi, Mohammad Hossein Gholami, Amirhossein Zabolian, Ehsan Ranjbar, Hossein Saleki, Adnan Ranjbar, Mehrdad Hashemi, Yavuz Nuri Ertas, Kiavash Hushmandi, Sepideh Mirzaei, Milad Ashrafizadeh, Ali Zarrabi, Saeed Samarghandian
Summary: EZH2 plays a crucial role in brain tumors, promoting the proliferation and invasion of cancer cells while demonstrating tumor-suppressor activity in medulloblastoma. In addition to regulating gene expression, EZH2 can also influence the response of brain tumors to chemotherapy and radiotherapy.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biotechnology & Applied Microbiology
Liang Ai, Xiaojun Luo, Xiong Yan, Shan Jiang
Summary: The study found that miR-506-3p inhibited the progression of CRC by targeting EZH2 expression, providing a new molecular target for the clinical treatment of CRC in the future.
Article
Immunology
Deborah Mannino, Sarah Adriana Scuderi, Giovanna Casili, Valentina Bova, Laura Cucinotta, Marika Lanza, Alessia Filippone, Emanuela Esposito, Irene Paterniti
Summary: Parkinson's disease is characterized by degeneration of dopaminergic neurons and can cause motor disorders. The upregulation of EZH2 in the brains of PD patients suggests its possible role in PD pathogenesis. In this study, the neuroprotective effects of the EZH2 inhibitor GSK-343 were evaluated in an in vivo model of MPTP-induced dopaminergic degeneration. The results showed that GSK-343 treatment improved behavioral deficits and reduced PD hallmarks.
JOURNAL OF NEUROINFLAMMATION
(2023)
Article
Immunology
Chengmei He, Yanlei Yang, Zhilei Chen, Suying Liu, Taibiao Lyu, Liuting Zeng, Li Wang, Yongzhe Li, Mu Wang, Hua Chen, Fengchun Zhang
Summary: EZH2 is upregulated in CD4(+) T cells of pSS patients, promoting Tfh differentiation by enhancing STAT3 phosphorylation. EZH2 promotes Tfh differentiation and may be implicated in the pathogenesis of pSS.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Obstetrics & Gynecology
Ye Shang, Shujuan Wu, SaiJiao Li, Xiaolin Qin, Jiao Chen, Jinli Ding, Jing Yang
Summary: The study found a significant decrease in the expression of EZH2 in villi tissue from RSA patients compared to healthy controls. Inhibition of EZH2 expression or function in trophoblasts promoted M1 macrophage polarization, potentially contributing to the pathogenesis of RSA. Additionally, EZH2 suppression affected the secretion of immune and inflammatory cytokines in trophoblasts.
REPRODUCTIVE SCIENCES
(2022)
Article
Oncology
Kiyoshi Tone, Sachiyo Ohno, Masatake Honda, Akifumi Notsu, Keiko Sasaki, Takashi Sugino
Summary: The study evaluated the utility of EZH2 immunocytochemistry in bile cytology for diagnosing pancreatobiliary adenocarcinoma. EZH2 ICC significantly improved sensitivity in indeterminate cytology samples and may be useful as an initial assessment to ensure no cancer cells are missed.
CANCER CYTOPATHOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Johanna Barth, Ivonne Loeffler, Tzvetanka Bondeva, Marita Liebisch, Gunter Wolf
Summary: This study analyzed the impact of hypoxia and HIFs on epigenetic changes in podocytes, specifically affecting NIPP1, EZH2, and H3K27me3. It was found that hypoxic conditions and pharmacological HIFs activation significantly reduced the expression of NIPP1 and EZH2, and diminished H3K27 trimethylation.
Article
Biochemistry & Molecular Biology
Sarah Adriana Scuderi, Alessia Filippone, Rossella Basilotta, Deborah Mannino, Giovanna Casili, Anna Paola Capra, Giulia Chisari, Lorenzo Colarossi, Serena Sava, Michela Campolo, Emanuela Esposito, Irene Paterniti
Summary: This study investigated the effect of GSK343 on canonical/non-canonical NF-kappa B/I kappa B alpha pathways and immune response in GB. In vitro results showed that GSK343 significantly reduced GB cell viability and modulated pathway activation. In vivo, GSK343 reduced tumor mass and regulated oxidative stress levels. Ex vivo results confirmed the anti-proliferative effect of GSK343 and demonstrated its ability to regulate immune response.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Gastroenterology & Hepatology
Teng Ma, Jie Gu, Ye Zhao, Su Li, Duowu Zou, Di Ge
Summary: This study investigated the attenuated tight junction in PPI-refractory gastroesophageal reflux disease (RGERD) and revealed a potential mechanism by which EZH2-mediated H3K27me3 impairs esophageal epithelial barrier function through suppressing the transcription of CLDN1.
DIGESTIVE AND LIVER DISEASE
(2022)
Article
Biochemistry & Molecular Biology
Lea Scherschinski, Markus Prem, Irina Kremenetskaia, Ingeborg Tinhofer, Peter Vajkoczy, Anna-Gila Karbe, Julia Sophie Onken
Summary: The receptor tyrosine kinase AXL (RTK-AXL) plays a crucial role in therapy resistance in glioblastoma multiforme (GBM). The shedding product of RTK-AXL, CT-AXL, acts as a surrogate marker for radio-resistance. Overexpression of endogenous RTX-AXL leads to therapy resistance, but combination therapy of AXL TKI with standard treatments can increase therapeutic effects significantly.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Magdalena Mizerska-Kowalska, Adrianna Slawinska-Brych, Emilia Niedziela, Viktor Brodovskiy, Barbara Zdzisinska
Summary: As epigenetic abnormalities play a crucial role in cancerogenesis, natural substances are explored as potential therapeutic targets for gene expression regulation. Alpha-ketoglutarate (AKG) is a co-substrate for enzymes involved in histone and DNA demethylation with anti-cancer activity. This study investigated the potential effect of AKG on the expression of neutral endopeptidase (NEP) in cancer cells and normal cells and explored the synergistic activity of AKG with a NEP specific inhibitor. The results showed that AKG downregulated NEP expression in highly aggressive osteosarcoma cells and this downregulation was involved in AKG-induced growth inhibition. Additionally, the combination of AKG and the NEP inhibitor enhanced the growth inhibitory potential. This study also reported for the first time that AKG can influence the activity of histone methyltransferase EZH2, although further investigation is needed to elucidate the mechanisms.
Article
Andrology
Shan Xu, Chen Yao, Yanlin Jian, Yule Chen, Xinyang Wang, Hongjun Xie, Lei Li, Bohan Ma, Xiaoyu Feng
Summary: This study constructed an EZH2-regulated immune risk score prognostic model to predict the prognosis of ccRCC patients and provided a prospect for the clinical application of EZH2 inhibitors in fine-tuning T cell immune therapy.
TRANSLATIONAL ANDROLOGY AND UROLOGY
(2023)
Article
Medicine, Research & Experimental
Liang-Chun Shih, Chia-Wen Tsai, Tzu-Chieh Lin, Yun-Chi Wang, Jie-Long He, Che-Lun Hsu, Te-Chun Hsia, Fuu-Jen Tsai, Jai-Sing Yang, Yuan-Man Hsu, Da-Tian Bau, Wen-Shin Chang
Summary: The aim of this study was to evaluate the association of EZH2 genotypes with oral cancer risk among Taiwanese and analyze the interaction of EZH2 genotypes with personal behaviors.
Article
Oncology
Xuying Xu, Siyi Wang, Dongmei Zhou, Jianhua Qu, Cang Zhang, Yichuan Xu, Liyun Sun
Summary: This study investigated the protective effects of Haoqin-Huaban formula (HQHB) on UVB-induced skin damage and its regulatory mechanisms. The results showed that HQHB inhibited UVB-induced skin damage in a dose-dependent manner by eliminating oxidative stress. Moreover, HQHB upregulated the expression of HOXA11-AS by activating HIF-1α, which stabilized EZH2 protein and reduced oxidative stress. Consequently, HOXA11-AS promoted cell proliferation and inhibited apoptosis in HaCaT cells.
AMERICAN JOURNAL OF TRANSLATIONAL RESEARCH
(2022)