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Target not currently curated in GtoImmuPdb
Target id: 2835
Nomenclature: enhancer of zeste 1 polycomb repressive complex 2 subunit
Abbreviated Name: EZH1
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 747 | 17q21.2 | EZH1 | enhancer of zeste 1 polycomb repressive complex 2 subunit | 1 |
| Mouse | - | 747 | 11 64.37 cM | Ezh1 | enhancer of zeste 1 polycomb repressive complex 2 subunit | |
| Rat | - | 747 | 10q32.1 | Ezh1 | enhancer of zeste 1 polycomb repressive complex 2 subunit | |
| Previous and Unofficial Names |
| enhancer of zeste homolog 1 (Drosophila) | KMT6B |
| Database Links |
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| Alphafold | Q92800 (Hs), P70351 (Mm) |
| ChEMBL Target | CHEMBL2189116 (Hs) |
| Ensembl Gene | ENSG00000108799 (Hs), ENSMUSG00000006920 (Mm), ENSRNOG00000020336 (Rn) |
| Entrez Gene | 2145 (Hs), 14055 (Mm), 303547 (Rn) |
| Human Protein Atlas | ENSG00000108799 (Hs) |
| KEGG Gene | hsa:2145 (Hs), mmu:14055 (Mm), rno:303547 (Rn) |
| OMIM | 601674 (Hs) |
| Pharos | Q92800 (Hs) |
| RefSeq Nucleotide | NM_001991 (Hs), NM_007970 (Mm), NM_001107051 (Rn) |
| RefSeq Protein | NP_001982 (Hs), NP_031996 (Mm), NP_001100521 (Rn) |
| UniProtKB | Q92800 (Hs), P70351 (Mm) |
| Wikipedia | EZH1 (Hs) |
Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| General Comments |
| EZH1/2 inhibitors have anti-proliferative effects that have anti-cancer potential. In addition, pharmacological inhibition of EZH1 and EZH2 has been shown to induce multiple inflammatory, stress, and antipathogen pathways, and to enhance recruitment of immune cells to virally infected cells in vitro, thereby creating a cellular antiviral state that was suppressive to infection by a range of DNA and RNA viruses [2]. EZH1/2 inhibitors exhibiting this experimental effect were GSK126, GSK343 and UNC1999. This work suggests that EZH1/2 inhibitors can induce a general antiviral defense mechanism. |
1. Abel KJ, Brody LC, Valdes JM, Erdos MR, McKinley DR, Castilla LH, Merajver SD, Couch FJ, Friedman LS, Ostermeyer EA et al.. (1996) Characterization of EZH1, a human homolog of Drosophila Enhancer of zeste near BRCA1. Genomics, 37 (2): 161-71. [PMID:8921387]
2. Arbuckle JH, Gardina PJ, Gordon DN, Hickman HD, Yewdell JW, Pierson TC, Myers TG, Kristie TM. (2017) Inhibitors of the Histone Methyltransferases EZH2/1 Induce a Potent Antiviral State and Suppress Infection by Diverse Viral Pathogens. MBio, 8 (4). [PMID:28811345]
3. Bradley WD. (2022) Ezh2 inhibition in combination therapies for the treatment of cancers. Patent number: US20220257577A1. Assignee: Constellation Pharmaceuticals Inc. Priority date: 23/07/2020. Publication date: 18/08/2022.
4. Honma D, Kanno O, Watanabe J, Kinoshita J, Hirasawa M, Nosaka E, Shiroishi M, Takizawa T, Yasumatsu I, Horiuchi T et al.. (2017) Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor. Cancer Sci, 108 (10): 2069-2078. [PMID:28741798]
5. Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA et al.. (2012) Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett, 3 (12): 1091-6. [PMID:24900432]
2.1.1.43 Histone methyltransferases (HMTs): enhancer of zeste 1 polycomb repressive complex 2 subunit. Last modified on 19/04/2023. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2835.
