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24 Results Found

  • Article
  • Open Access
19 Citations
5,507 Views
16 Pages

Evaluation of Tazemetostat as a Therapeutically Relevant Substance in Biliary Tract Cancer

  • Dino Bekric,
  • Daniel Neureiter,
  • Celina Ablinger,
  • Heidemarie Dobias and ,
  • Marlena Beyreis,
  • Markus Ritter,
  • Martin Jakab,
  • Johannes Bischof,
  • Ulrich Koller and
  • Christian Mayr
  • + 6 authors+ 1 author

2 March 2023

Biliary tract cancer (BTC) is a gastrointestinal malignancy associated with a poor survival rate. Current therapies encompass palliative and chemotherapeutic treatment as well as radiation therapy, which results in a median survival of only one year...

(This article belongs to the Special Issue New Insights in Biliary Tract Cancers Therapy)
  • Article
  • Open Access
13 Citations
3,675 Views
12 Pages

27 January 2025

Objectives: The primary aim of this phase 1 trial is to establish the recommended phase 2 dose (RP2D) of tazemetostat given with a fixed dose of pembrolizumab in patients with recurrent or metastatic head and neck squamous cell carcinomas (RM-HNSCCs)...

(This article belongs to the Section Clinical Research in Cancer)
  • Article
  • Open Access
7 Citations
3,239 Views
15 Pages

Isothiocyanates Potentiate Tazemetostat-Induced Apoptosis by Modulating the Expression of Apoptotic Genes, Members of Polycomb Repressive Complex 2, and Levels of Tri-Methylating Lysine 27 at Histone 3 in Human Malignant Melanoma Cells

  • Ioannis Anestopoulos,
  • Ioannis Paraskevaidis,
  • Sotiris Kyriakou,
  • Lambrini E. Giova and ,
  • Dimitrios T. Trafalis,
  • Sotiris Botaitis,
  • Rodrigo Franco,
  • Aglaia Pappa and
  • Mihalis I. Panayiotidis
  • + 4 authors+ 0 author

27 February 2024

In this study, we utilized an in vitro model consisting of human malignant melanoma as well as non-tumorigenic immortalized keratinocyte cells with the aim of characterizing the therapeutic effectiveness of the clinical epigenetic drug Tazemetostat a...

(This article belongs to the Special Issue Advances in Pathogenesis and Treatment of Skin Cancer)
  • Article
  • Open Access
25 Citations
5,488 Views
16 Pages

Dramatic In Vivo Efficacy of the EZH2-Inhibitor Tazemetostat in PBRM1-Mutated Human Chordoma Xenograft

  • Thibault Passeri,
  • Ahmed Dahmani,
  • Julien Masliah-Planchon,
  • Adnan Naguez and ,
  • Marine Michou,
  • Rania El Botty,
  • Sophie Vacher,
  • Rachida Bouarich,
  • André Nicolas and
  • Didier Decaudin
  • + 15 authors+ 10 authors

14 March 2022

Chordomas are rare neoplasms characterized by a high recurrence rate and a poor long-term prognosis. Considering their chemo-/radio-resistance, alternative treatment strategies are strongly required, but their development is limited by the paucity of...

  • Article
  • Open Access
2 Citations
3,134 Views
14 Pages

Validation of an LC-MS/MS Method for the Simultaneous Intracellular Quantification of the CDK4/6 Inhibitor Abemaciclib and the EZH2 Inhibitors GSK126 and Tazemetostat

  • Stefan Senekowitsch,
  • Thomas Freitag,
  • Daniel Dubinski,
  • Thomas M. Freiman and ,
  • Claudia Maletzki and
  • Burkhard Hinz
  • + 1 author+ 0 author

Background: Inhibitors of cyclin-dependent kinases (CDKs) and epigenetic modifier enhancer of zeste homolog 2 (EZH2) have emerged as promising options in the pharmacotherapy of malignant tumors. Recently, we demonstrated synergistic antitumor effects...

(This article belongs to the Section Pharmaceutical Technology, Manufacturing and Devices)
  • Article
  • Open Access
23 Citations
4,917 Views
25 Pages

Inhibition of the Histone Methyltransferase EZH2 Enhances Protumor Monocyte Recruitment in Human Mesothelioma Spheroids

  • Silvia Mola,
  • Giulia Pinton,
  • Marco Erreni,
  • Marco Corazzari and ,
  • Marco De Andrea,
  • Ambra A. Grolla,
  • Veronica Martini,
  • Laura Moro and
  • Chiara Porta
  • + 4 authors+ 0 author

Malignant pleural mesothelioma (MPM) is a highly aggressive cancer with a long latency period and dismal prognosis. Recently, tazemetostat (EPZ-6438), an inhibitor of the histone methyltransferase EZH2, has entered clinical trials due to the antiprol...

(This article belongs to the Special Issue Immune Response to Cancer: From Tumor Onset to Therapeutic Approach)
  • Review
  • Open Access
7 Citations
5,117 Views
19 Pages

Pharmacological Advancements of PRC2 in Cancer Therapy: A Narrative Review

  • Michael S. Wang,
  • Jonathan Sussman,
  • Jessica A. Xu,
  • Reema Patel and ,
  • Omar Elghawy and
  • Prashanth Rawla
  • + 1 author+ 0 author

11 December 2024

Polycomb repressive complex 2 (PRC2) is known to regulate gene expression and chromatin structure as it methylates H3K27, resulting in gene silencing. Studies have shown that PRC2 has dual functions in oncogenesis that allow it to function as both an...

(This article belongs to the Section Epidemiology)
  • Article
  • Open Access
1,284 Views
26 Pages

EZH2 Inhibition Restores Tumor Suppressor SFRP1 Activity by Reprogramming Extrachromosomal Circular DNA Dynamics in Ovarian Cancer

  • Tao Han,
  • Qingya Yan,
  • Yaqi Zhang,
  • Yu Gan and ,
  • Kaifan Li,
  • Liping Guan,
  • Changqin Jing,
  • Ciqing Yang,
  • Pengfei Li and
  • Qian Hao
  • + 7 authors+ 2 authors

15 February 2026

Extrachromosomal circular DNA (eccDNA) has emerged as a pivotal contributor to cancer progression, facilitating oncogene amplification, dysregulated gene expression, and tumor heterogeneity. Despite its significance in cancer, the interplay between e...

(This article belongs to the Special Issue Multi-Omics Data Integration in Complex Diseases (2nd Edition))
  • Article
  • Open Access
1 Citations
1,559 Views
30 Pages

Biological Evaluation of a Novel Compound with Predicted EZH2 and EED Binding Against Human Malignant Melanoma Cells

  • Sergei Gorbunov,
  • Sotiris Kyriakou,
  • Ioannis Anestopoulos,
  • Shahzaib Khoso and ,
  • Marcello Manfredi,
  • Rodrigo Franco,
  • Aglaia Pappa and
  • Mihalis I. Panayiotidis
  • + 3 authors+ 0 author

Enhancer of Zeste Homolog 2 (EZH2), the catalytic subunit of Polycomb Repressive Complex 2 (PRC2), mediates histone H3 lysine 27 trimethylation (H3K27me3), an epigenetic modification associated with transcriptional repression. EZH2 inhibitors (EZH2is...

(This article belongs to the Special Issue Protein Methyltransferases in Human Health and Diseases)
  • Review
  • Open Access
59 Citations
12,686 Views
19 Pages

Epithelioid Sarcoma—From Genetics to Clinical Practice

  • Anna M. Czarnecka,
  • Pawel Sobczuk,
  • Michal Kostrzanowski,
  • Mateusz Spalek and ,
  • Marzanna Chojnacka,
  • Anna Szumera-Cieckiewicz and
  • Piotr Rutkowski
  • + 2 authors+ 0 author

29 July 2020

Epithelioid sarcoma is a mesenchymal soft tissue sarcoma often arising in the extremities, usually in young adults with a pick of incidence at 35 years of age. Epithelioid sarcoma (ES) is characterized by the loss of SMARCB1/INI1 (integrase in...

(This article belongs to the Special Issue Bone and Soft Tissue Tumors)
  • Review
  • Open Access
25 Citations
6,876 Views
11 Pages

24 August 2022

Epithelioid sarcoma (ES) is a very rare and aggressive mesenchymal tumor of unclear origin and uncertain lineage characterized by a prevalent epithelioid morphology. The only recurrent genetic alteration reported in ES as yet is the functional inacti...

(This article belongs to the Collection Feature Papers in ‘Cellular Pathology’)
  • Systematic Review
  • Open Access
39 Citations
7,485 Views
15 Pages

SMARCB1 (INI-1)-Deficient Sinonasal Carcinoma: A Systematic Review and Pooled Analysis of Treatment Outcomes

  • Victor Ho-Fun Lee,
  • Raymond King-Yin Tsang,
  • Anthony Wing Ip Lo,
  • Sum-Yin Chan and ,
  • Joseph Chun-Kit Chung,
  • Chi-Chung Tong,
  • To-Wai Leung and
  • Dora Lai-Wan Kwong
  • + 3 authors+ 0 author

5 July 2022

(1) Background: SMARCB1 (INI-1)-deficient sinonasal carcinoma is a rare sinonasal malignancy; since its discovery and description in 2014, less than 200 cases have been identified. It is almost impossible to perform randomized-controlled trials on no...

(This article belongs to the Special Issue Diagnostic, Prognostic, Predictive Biomarkers and New Targets for Treatment in Head and Neck Cancers)
  • Article
  • Open Access
2 Citations
1,283 Views
19 Pages

EZH2 Inhibition in Mesothelioma Cells Increases the Release of Extracellular Vesicles That Skew Neutrophils Toward a Protumor Phenotype

  • Giulia Pinton,
  • Elia Bari,
  • Silvia Fallarini,
  • Valentina Gigliotti and ,
  • Veronica De Giorgis,
  • Fausto Chiazza,
  • Maria Luisa Torre,
  • Marcello Manfredi and
  • Laura Moro
  • + 4 authors+ 0 author

23 October 2025

We previously demonstrated that in BAP1-proficient pleural mesothelioma cells, CDKN2A is critical for mediating the response to selective EZH2 inhibition and highlighted a complex interplay between epigenetic regulation and the tumor immune microenvi...

(This article belongs to the Section Molecular Oncology)
  • Article
  • Open Access
1,185 Views
25 Pages

EZH2 Regulates the Proliferation-Senescence Balance and Tumor–Stromal Signaling in Lung Adenocarcinoma

  • Kamil Saramowicz,
  • Matylda Piesiewicz,
  • Angelika A. Adamus-Grabicka,
  • Pengyu Zhao and ,
  • Joanna Sikora and
  • Wioletta Rozpędek-Kamińska
  • + 1 author+ 0 author

Enhancer of zeste homolog 2 (EZH2), the catalytic component of the polycomb repressive complex 2, is frequently overexpressed in lung adenocarcinoma and contributes to transcriptional programs that support tumor proliferation and cellular plasticity....

(This article belongs to the Special Issue Challenges and Future Perspectives in Treatment for Lung Cancer: 2nd Edition)
  • Article
  • Open Access
34 Citations
4,999 Views
14 Pages

HDAC Inhibition Increases HLA Class I Expression in Uveal Melanoma

  • Zahra Souri,
  • Aart G. Jochemsen,
  • Mieke Versluis,
  • Annemijn P.A. Wierenga and ,
  • Fariba Nemati,
  • Pieter A. van der Velden,
  • Wilma G.M. Kroes,
  • Robert M. Verdijk,
  • Gregorius P.M. Luyten and
  • Martine J. Jager
  • + 5 authors+ 0 author

9 December 2020

The treatment of uveal melanoma (UM) metastases or adjuvant treatment may imply immunological approaches or chemotherapy. It is to date unknown how epigenetic modifiers affect the expression of immunologically relevant targets, such as the HLA Class...

  • Article
  • Open Access
7 Citations
4,858 Views
14 Pages

EZH2 Inhibition Sensitizes IDH1R132H-Mutant Gliomas to Histone Deacetylase Inhibitor

  • Lisa Sprinzen,
  • Franklin Garcia,
  • Angeliki Mela,
  • Liang Lei and ,
  • Pavan Upadhyayula,
  • Aayushi Mahajan,
  • Nelson Humala,
  • Lisa Manier,
  • Richard Caprioli and
  • Peter Canoll
  • + 7 authors+ 2 authors

25 January 2024

Isocitrate Dehydrogenase-1 (IDH1) is commonly mutated in lower-grade diffuse gliomas. The IDH1R132H mutation is an important diagnostic tool for tumor diagnosis and prognosis; however, its role in glioma development, and its impact on response to the...

  • Communication
  • Open Access
33 Citations
6,985 Views
11 Pages

The Role of the Histone Methyltransferase EZH2 in Liver Inflammation and Fibrosis in STAM NASH Mice

  • Seul Lee,
  • Dong-Cheol Woo,
  • Jeeheon Kang,
  • Moonjin Ra and ,
  • Ki Hyun Kim,
  • Seoung Rak Lee,
  • Dong Kyu Choi,
  • Heejin Lee,
  • Ki Bum Hong and
  • Ji Hoon Yu
  • + 7 authors+ 2 authors

Non-alcoholic fatty liver disease (NAFLD) is a leading form of chronic liver disease, with few biomarkers and treatment options currently available. Non-alcoholic steatohepatitis (NASH), a progressive disease of NAFLD, may lead to fibrosis, cirrhosis...

(This article belongs to the Section Cell Biology)
  • Review
  • Open Access
1 Citations
4,070 Views
16 Pages

Small-Molecule Drugs in Pediatric Neuro-Oncology

  • Stephanie Vairy and
  • George Michaiel

Advances in molecular diagnostics have enabled precision medicine approaches in pediatric neuro-oncology, with small-molecule drugs emerging as promising therapeutic candidates targeting specific genetic and epigenetic alterations in central nervous...

(This article belongs to the Special Issue Clinical Outcomes and New Treatments in Pediatric Brain Tumors)
  • Review
  • Open Access
1,164 Views
21 Pages

Epithelioid Sarcoma: A Review and Update

  • Jun Nishio,
  • Shizuhide Nakayama and
  • Mikiko Aoki

21 August 2026

Epithelioid sarcoma (EPS) is an ultra-rare malignant mesenchymal neoplasm of uncertain differentiation that comprises two distinct clinicopathological subtypes: classic and proximal. Classic EPS most commonly occurs in the distal upper extremity of a...

(This article belongs to the Special Issue Challenges and New Developments in the Diagnosis and Treatment of Sarcoma)
  • Review
  • Open Access
31 Citations
3,137 Views
25 Pages

Unraveling the Epigenetic Landscape of Mature B Cell Neoplasia: Mechanisms, Biomarkers, and Therapeutic Opportunities

  • Nawar Maher,
  • Francesca Maiellaro,
  • Joseph Ghanej,
  • Silvia Rasi and ,
  • Riccardo Moia and
  • Gianluca Gaidano
  • + 1 author+ 0 author

22 August 2025

Epigenetic regulation is critical to B cell development, guiding gene expression via DNA methylation, histone modifications, chromatin remodeling, and noncoding RNAs. In mature B cell neoplasms, particularly diffuse large B cell lymphoma (DLBCL), fol...

(This article belongs to the Section Molecular Oncology)
  • Review
  • Open Access
22 Citations
9,468 Views
30 Pages

Novel Therapeutics in Soft Tissue Sarcoma

  • Leonidas Mavroeidis,
  • Andrea Napolitano,
  • Paul Huang and
  • Robin L. Jones

24 December 2024

There has been noteworthy progress in molecular characterisation and therapeutics in soft tissue sarcomas. Novel agents have gained regulatory approval by the FDA. Examples are the tyrosine kinase inhibitors avapritinib and ripretinib in gastrointest...

(This article belongs to the Special Issue Advances in Cancer Therapeutics)
  • Article
  • Open Access
427 Views
16 Pages

An Ex Vivo 3D Co-Culture Model of the Bone Marrow Niche Better Predicts Clinically Relevant Epigenetic Target Modulation to Improve Immunotherapy in Multiple Myeloma

  • Christine Greil,
  • Johannes Jung,
  • Julia Felthaus,
  • Dagmar Wider and ,
  • Monika Engelhardt and
  • Ralph Wäsch
  • + 1 author+ 0 author

23 September 2026

Background: In the last decade, treatment options for multiple myeloma have increased remarkably, including antibodies or CAR-T cells targeting myeloma surface markers with unprecedented efficacy. To enhance immunomodulation and clinical efficacy eve...

(This article belongs to the Section Methods and Technologies Development)
  • Article
  • Open Access
1 Citations
1,259 Views
12 Pages

EZH2-Mediated PTEN Silencing Promotes AKT-Dependent Afatinib Resistance in Radiation-Resistant Cervical Cancer Cells

  • Won-Hyoek Lee,
  • Seong Cheol Kim,
  • Sungchan Park,
  • Jeong Woo Park and
  • Sang-Hun Lee

17 October 2025

Background: Cervical cancer remains a major global health burden, and treatment failure due to radioresistance and secondary drug resistance severely limits clinical outcomes. Enhancer of zeste homolog 2 (EZH2) is a key epigenetic regulator implicate...

(This article belongs to the Section Obstetrics & Gynecology)
  • Review
  • Open Access
2 Citations
6,288 Views
18 Pages

Background: Rhabdoid tumours (RTs) are aggressive neoplasms most often characterised by biallelic loss of the SMARCB1 gene, encoding a core subunit of the SWI/SNF chromatin-remodelling complex. Despite their relative genetic stability, RTs exhibit a...

(This article belongs to the Section Cell Metabolism)