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
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
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
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)
Review
Physiology
Tingting Li, Chao Yu, Shougang Zhuang
Summary: EZH2, as a histone-modifying enzyme, plays a diverse role in kidney diseases and inhibiting it may provide therapeutic benefits in certain conditions while potentially exacerbating others.
FRONTIERS IN PHYSIOLOGY
(2021)
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
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
Pathology
Talha Anwar, Maria E. Gonzalez, Celina G. Kleer
Summary: EZH2, the catalytic subunit of PRC2, plays a critical role in determining cell identity by depositing trimethyl marks on histone H3. In addition to its well-defined role in transcriptional repression, EZH2 also exerts some histonemethyltransferaseeindependent functions, which are important for breast cancer progression.
AMERICAN JOURNAL OF PATHOLOGY
(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.
Review
Oncology
Wuhan Yu, Ning Liu, Xiaogang Song, Lang Chen, Mancai Wang, Guohui Xiao, Tengfei Li, Zheyuan Wang, Youcheng Zhang
Summary: This article focuses on the value of EZH2 research in gastric cancer by examining its crucial involvement in gastric cancer progression. The article first introduces the two main functions of EZH2: histone methylation modification and DNA methylation. It then provides a detailed description of the mechanisms of EZH2 in gastric cancer-related events, and concludes with a summary of the progress in the development of EZH2 inhibitors. This review article provides researchers studying the epigenetics of gastric cancer with new research ideas to find new targets for studying the pathogenesis of gastric cancer.
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
Lin Xu, Jiandong Gao, Di Huang, Pinglan Lin, Dongsheng Yao, Feng Yang, Yaheng Zhang, Xuejun Yang, Ming Wu, Chaoyang Ye
Summary: Emodin delays the progression of chronic renal failure and inhibits renal tubulointerstitial fibrosis by reducing extracellular collagen deposition and inhibiting pro-fibrotic signaling pathways, through down-regulation of EZH2.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Xufen Yu, Jun Wang, Weida Gong, Anqi Ma, Yudao Shen, Chengwei Zhang, Xijuan Liu, Ling Cai, Jing Liu, Gang Greg Wang, Jian Jin
Summary: This passage focuses on the noncanonical function of EZH2 in the development of multiple myeloma (MM), and proposes a novel therapeutic strategy, pharmacological degradation of EZH2, for treating EZH2-dependent MM.
Meeting Abstract
Gastroenterology & Hepatology
Olga Sarmento, Michelle Gonzalez, Manuel Braga, Joseph Gaballa, Adebowale Bamidele, Guilherme Piovezani Ramos, Mary Sagstetter, William Faubion
Meeting Abstract
Gastroenterology & Hepatology
Olga Sarmento, Michelle Gonzalez, Manuel Braga, Joseph Gaballa, Adebowale Bamidele, Guilherme Piovezani Ramos, Mary Sagstetter, William Faubion
INFLAMMATORY BOWEL DISEASES
(2019)
Article
Gastroenterology & Hepatology
Manuel B. Braga-Neto, Joseph M. Gaballa, Adebowale O. Bamidele, Olga F. Sarmento, Phyllis Svingen, Michelle Gonzalez, Guilherme Piovezani Ramos, Mary R. Sagstetter, Sayed Obaidullah Aseem, Zhifu Sun, William A. Faubion
JOURNAL OF CROHNS & COLITIS
(2020)
Article
Oncology
Guillermo Urrutia, Ann Salmonson, Jorge Toro-Zapata, Thiago M. de Assuncao, Angela Mathison, Nelson Dusetti, Juan Iovanna, Raul Urrutia, Gwen Lomberk
MOLECULAR CANCER RESEARCH
(2020)
Article
Multidisciplinary Sciences
Angela Mathison, Thiago Milech De Assuncao, Nikita R. Dsouza, Monique Williams, Michael T. Zimmermann, Raul Urrutia, Gwen Lomberk
Article
Oncology
Haijing Liu, Bo Zhang, Zhifu Sun
CANCER COMMUNICATIONS
(2020)
Article
Infectious Diseases
Wei-xia Xuan, Jin-jin Li, Qun-cheng Zhang, Guan-nan Sun, Zhi-wei Xu, Zhi-fu Sun, Xiao-ju Zhang
INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES
(2020)
Article
Genetics & Heredity
Xianfeng Chen, Zhifu Sun
Summary: This study utilized a novel lncRNA discovery pipeline and RNA-seq data resources to systematically discover novel lincRNAs in 30 major human tissue types, which defined the characteristics of each tissue type and demonstrated their reliability and tissue-specific expression. Tissue-specific genes were identified for each major tissue type, providing insight into each respective tissue's unique function and expanding interpretation of non-coding SNPs from genome-wide association studies.
Article
Genetics & Heredity
Reilly L. Allison, Jacob W. Adelman, Jenica Abrudan, Raul A. Urrutia, Michael T. Zimmermann, Angela J. Mathison, Allison D. Ebert
Summary: Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease with unclear mechanisms. A study found that glial-secreted factors may affect the expression and deposition of neurofilament proteins in motor neurons of ALS patients.
Article
Genetics & Heredity
Zhifu Sun, Saurabh Behati, Panwen Wang, Aditya Bhagwate, Samantha McDonough, Vivian Wang, William Taylor, Julie Cunningham, John Kisiel
Summary: Whole-genome methylation sequencing provides both DNA methylation and structural variant information. However, there is limited data on the reliability of obtaining this information simultaneously from low-input DNA using different library preparation and sequencing protocols. This study compared the performance of three protocols (EM-sequencing, QIA-sequencing, and Swift-sequencing) on CpG methylation measurement, SNV, and CNV detection. Results showed that at low DNA input, EM-sequencing was superior in most metrics except for CNV detection. EM-sequencing captured the highest number of CpGs and true SNVs, making it suitable for detecting methylation, SNVs, and CNVs from low-input DNA in a single sequencing.
Article
Medicine, Research & Experimental
Michelle M. Gonzalez, Adebowale O. Bamidele, Phyllis A. Svingen, Mary R. Sagstetter, Thomas C. Smyrk, Joseph M. Gaballa, Feda H. Hamdan, Robyn Laura Kosinsky, Hunter R. Gibbons, Zhifu Sun, Zhenqing Ye, Asha Nair, Guilherme P. Ramos, Manuel B. Braga Neto, Alexander Q. Wixom, Angela J. Mathison, Steven A. Johnsen, Raul Urrutia, William A. Faubion
Summary: Research has shown that BMI1 regulates the inflammatory enhancer network in Treg cells, and its loss leads to systemic inflammation and phenotypic conversion of Treg cells, which is relevant to CD4(+) T cells associated with Crohn's disease.
JOURNAL OF CLINICAL INVESTIGATION
(2021)
Meeting Abstract
Gastroenterology & Hepatology
Manuel Bonfim Braga Neto, Joseph M. Gaballa, Olga F. Sarmento, Guilherme Piovezani Ramos, Michelle Gonzalez, Adebowale O. Bamidele, Mary R. Sagstetter, Zhifu Sun, William Faubion
Meeting Abstract
Gastroenterology & Hepatology
Michelle Gonzalez, Phyllis Svingen, Olga F. Sarmento, Thomas Smyrk, Mary R. Sagstetter, Adebowale O. Bamidele, Manuel Bonfim Braga Neto, Guilherme Piovezani Ramos, Joseph M. Gaballa, Romica Kerketta, Raul Urrutia, William Faubion
Article
Gastroenterology & Hepatology
Adebowale O. Bamidele, Phyllis A. Svingen, Mary R. Sagstetter, Olga F. Sarmento, Michelle Gonzalez, Manuel B. Braga Neto, Subra Kugathasan, Gwen Lomberk, Raul A. Urrutia, William A. Faubion
CELLULAR AND MOLECULAR GASTROENTEROLOGY AND HEPATOLOGY
(2019)