EZH2: a novel target for cancer treatment

Autor: Wenfang Du, Ran Duan, Weijian Guo
Rok vydání: 2020
Předmět:
0301 basic medicine
Cancer Research
Adenosine
H3K27me3
EZH2 inhibitor
Review
Metastasis
Histones
0302 clinical medicine
Neoplasms
Gene expression
Tumor Microenvironment
Multicenter Studies as Topic
Neoplasm Metastasis
Cancer
Clinical Trials as Topic
biology
Cell Cycle
EZH2
Polycomb Repressive Complex 2
lcsh:Diseases of the blood and blood-forming organs
Hematology
lcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogens
Combined Modality Therapy
Neoplasm Proteins
Histone Code
Cell Transformation
Neoplastic

Histone
Oncology
030220 oncology & carcinogenesis
Benzamides
PRC2
Transcriptional Activation
Senescence
Pyridones
Morpholines
Antineoplastic Agents
macromolecular substances
Epigenetic Repression
lcsh:RC254-282
Methylation
Structure-Activity Relationship
03 medical and health sciences
medicine
Humans
Enhancer of Zeste Homolog 2 Protein
Molecular Biology
Gene
lcsh:RC633-647.5
Biphenyl Compounds
medicine.disease
030104 developmental biology
Drug Resistance
Neoplasm

biology.protein
Cancer research
Zdroj: Journal of Hematology & Oncology
Journal of Hematology & Oncology, Vol 13, Iss 1, Pp 1-12 (2020)
ISSN: 1756-8722
DOI: 10.1186/s13045-020-00937-8
Popis: Enhancer of zeste homolog 2 (EZH2) is enzymatic catalytic subunit of polycomb repressive complex 2 (PRC2) that can alter downstream target genes expression by trimethylation of Lys-27 in histone 3 (H3K27me3). EZH2 could also regulate gene expression in ways besides H3K27me3. Functions of EZH2 in cells proliferation, apoptosis, and senescence have been identified. Its important roles in the pathophysiology of cancer are now widely concerned. Therefore, targeting EZH2 for cancer therapy is a hot research topic now and different types of EZH2 inhibitors have been developed. In this review, we summarize the structure and action modes of EZH2, focusing on up-to-date findings regarding the role of EZH2 in cancer initiation, progression, metastasis, metabolism, drug resistance, and immunity regulation. Furtherly, we highlight the advance of targeting EZH2 therapies in experiments and clinical studies.
Databáze: OpenAIRE