enhancer of zeste 1 polycomb repressive complex 2 subunit

Target id: 2835

Nomenclature: enhancer of zeste 1 polycomb repressive complex 2 subunit

Abbreviated Name: EZH1

Family: 2.1.1.43 Histone methyltransferases (HMTs)

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for enhancer of zeste 1 polycomb repressive complex 2 subunit in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 747 17q21.1-q21.3 EZH1 enhancer of zeste 1 polycomb repressive complex 2 subunit 1
Mouse - 750 11 C-D 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
KMT6B | enhancer of zeste homolog 1 (Drosophila)
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
GSK343 Hs Inhibition 6.6 pIC50 3
pIC50 6.6 (IC50 2.4x10-7 M) [3]
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.

References

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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. Genomics37 (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. MBio8 (4). [PMID:28811345]

3. 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 Lett3 (12): 1091-6. [PMID:24900432]

How to cite this page

2.1.1.43 Histone methyltransferases (HMTs): enhancer of zeste 1 polycomb repressive complex 2 subunit. Last modified on 18/08/2017. Accessed on 18/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2835.