embryonic ectoderm development | Neutral sphingomyelinase coupling factors | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

embryonic ectoderm development

Target not currently curated in GtoImmuPdb

Target id: 2487

Nomenclature: embryonic ectoderm development

Family: Neutral sphingomyelinase coupling factors

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 441 11q14.2-q22.3 EED embryonic ectoderm development
Mouse - 441 7 E1 Eed embryonic ectoderm development
Rat - 441 1q32 Eed embryonic ectoderm development
Previous and Unofficial Names
Polycomb protein EED | WAIT-1 | WD protein associating with integrin cytoplasmic tails 1
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
A-395 Hs Binding 9.4 pKi 2
pKi 9.4 (Ki 4x10-10 M) [2]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
MAK683 Hs Negative 8.2 pIC50 1
pIC50 8.2 (IC50 5.8x10-9 M) [1]
Description: Measuring test compound-mediated inhibition of EED-H3K27Me3 binding in a peptide competition binding assay using AlphaScreen technology.
General Comments
The EED protein is an essential subunit of the polycomb repressive complex 2 (PRC2). PRC2 trimethylates histone H3 at lysine 27 (H3K27me3) causing gene silencing. H3K27me3 marks are recognised, and the trimethyllysine bound by EED. The small molecule probe A-395 prevents EED binding to H3K27me3 histone marks and this blocks activation of the catalytic activity of PRC2.

References

Show »

1. Chan HM, Gu X-JJ, Huang Y, Li L, Mi Y, Qi W, Sendzik M, Sun Y, Wang L, Yu Z et al.. (2016) Triazolopyrimidine compounds and uses thereof. Patent number: WO2016103155A1. Assignee: Novartis Ag. Priority date: 23/12/2014. Publication date: 20/06/2016.

2. He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM et al.. (2017) The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat. Chem. Biol., 13 (4): 389-395. [PMID:28135237]

How to cite this page

Select citation format: