Last update 01 Nov 2024

EZH2 x SUZ12 x EED

Last update 01 Nov 2024

Basic Info

Related Targets

EZH2SUZ12EED

Drugs associated with EZH2 x SUZ12 x EED

E-3P-MDM2

Target

EED x EZH2 x SUZ12

Mechanism

EED inhibitors [+2]

Active Org.

Shenyang Pharmaceutical University [+1]

Originator Org.

Shenyang Pharmaceutical University [+1]

Active Indication

Lymphoma

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

UNC6846

Target

EED x EZH2 x SUZ12

Mechanism

EED inhibitors [+2]

Active Org.-

Originator Org.-

Active Indication-

Inactive Indication-

Drug Highest Phase-

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

UNC6851

Target

EED x EZH2 x SUZ12

Mechanism

EED inhibitors [+2]

Active Org.-

Originator Org.-

Active Indication-

Inactive Indication-

Drug Highest Phase-

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with EZH2 x SUZ12 x EED

100 Translational Medicine associated with EZH2 x SUZ12 x EED

0 Patents (Medical) associated with EZH2 x SUZ12 x EED

154

Literatures (Medical) associated with EZH2 x SUZ12 x EED

01 Oct 2024·Clinical Genetics

EZH2‐associated tumor malignancy: A prominent target for cancer treatment

Review

Author: Biray‐Avci, Cigir ; Sabour‐Takanlou, Maryam ; Sabour‐Takanlou, Leila

AbstractThe discussion in this review centers around the significant relationships between EZH2 and the initiation, progression, metastasis, metabolism, drug resistance, and immune regulation of cancer. Polycomb group (PcG) proteins, which encompass two primary Polycomb repressor complexes (PRC1 and PRC2), have been categorized. PRC2 consists mainly of four subunits, namely EZH2, EED, SUZ12, and RbAp46/48. As the crucial catalytic component within the PRC2 complex, EZH2 plays a pivotal role in controlling a wide range of biological processes. Overexpression/mutations of EZH2 have been detected in a wide variety of tumors. Several mechanisms of EZH regulation have been identified, including regulation EZH2 mRNA by miRNAs, LncRNAs, accessibility to DNA via DNA‐binding proteins, post‐translational modifications, and transcriptional regulation. EZH2 signaling triggers cancer progression and may intervene with anti‐tumor immunity; therefore it has charmed attention as an effective therapeutic target in cancer therapy. Numerous nucleic acid‐based therapies have been used in the modification of EZH2. In addition to gene therapy approaches, pharmaceutical compounds can be used to target the EZH2 signaling pathway in the treatment of cancer. EZH2‐associated tumor cells and immune cells enhance the effects of the immune response in a variety of human malignancies. The combination of epigenetic modifying agents, such as anti‐EZH2 compounds with immunotherapy, could potentially be efficacious even in the context of immunosuppressive tumors. Summary, understanding the mechanisms underlying resistance to EZH2 inhibitors may facilitate the development of novel drugs to prevent or treat relapse in treated patients.

01 Oct 2024·American Journal of Medical Genetics Part A

Biallelic loss‐of‐function variants of EZH1 cause a novel developmental disorder with central precocious puberty

Article

Author: Yanagi, Kumiko ; Okamoto, Nobuhiko ; Kaname, Tadashi ; Ogitani, Ayako ; Yoshida, Sayaka ; Etani, Yuri

AbstractPathogenic variants of polycomb repressive complex‐2 (PRC2) subunits are associated with overgrowth syndromes and neurological diseases. EZH2 is a major component of PRC2 and mediates the methylation of H3K27 trimethylation (H3K27me3). Germline variants of EZH2 have been identified as a cause of Weaver syndrome (WS), an overgrowth/intellectual disability (OGID) syndrome characterized by overgrowth, macrocephaly, accelerated bone age, intellectual disability (ID), and characteristic facial features. Germline variants of SUZ12 and EED, other components of PRC2, have also been reported in the WS or Weaver‐like syndrome. EZH1 is a homolog of EZH2 that interchangeably associates with SUZ12 and EED. Recently, pathogenic variants of EZH1 have been reported in individuals with dominant and recessive neurodevelopmental disorders. We herein present sisters with biallelic loss‐of‐function variants of EZH1. They showed developmental delay, ID, and central precocious puberty, but not the features of WS or other OGID syndromes.

01 Mar 2024·Theriogenology

Exposure to the extremely low-frequency electromagnetic field induces changes in the epigenetic regulation of gene expression in the endometrium

Article

Author: Wydorski, Pawel Jozef ; Kozlowska, Wiktoria ; Zmijewska, Agata ; Franczak, Anita

Increasing technological development results in more sources of the extremely low-frequency electromagnetic field (ELF-EMF), which is recognized as an environmental risk factor. The results of the past study indicate that the ELF-EMF can affect the level of DNA methylation. The study aimed to determine whether the ELF-EMF induces changes in epigenetic regulation of gene expression in the endometrium of pigs during the peri-implantation period. Endometrial slices (100 ± 5 mg) collected on days 15-16 of pregnancy were exposed in vitro to the ELF-EMF at a frequency of 50 Hz for 2 h of treatment duration. To determine the impact of the ELF-EMF on elements of epigenetic regulations involved in DNA methylation, histone modification, and microRNA biogenesis in the endometrium, the DNMT1 and DNMT3a; EZH2, UHRF1, and MBD1; DICER1 and DGCR8 mRNA transcript and protein abundance were analyzed using Real-Time PCR and Western blot, respectively. Moreover, EED and SUZ12 mRNA transcript, global DNA methylation, and the activity of histone deacetylase (HDAC) were analyzed. The changes in the abundance of DNMT1 and DNMT3a, EZH2 mRNA transcript and protein, EED and SUZ12 mRNA transcript, global DNA methylation level, HDAC activity, and the abundance of proteins involved in microRNA biogenesis evoked by the ELF-EMF in the endometrium were observed. The ELF-EMF possesses the potential to alter epigenetic regulation of gene expression in the porcine endometrium. Observed alterations may be the reason for changes in the transcriptomic profile of the endometrium exposed to the ELF-EMF which in turn may disrupt biological processes in the uterus during peri-implantation.

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