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embryonic ectoderm development

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Target not currently curated in GtoImmuPdb

Target id: 2487

Nomenclature: embryonic ectoderm development

Family: Neutral sphingomyelinase coupling factors

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

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
A-395 Small molecule or natural product Hs Binding 9.4 pKi 3
pKi 9.4 (Ki 4x10-10 M) [3]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
FTX-6058 Small molecule or natural product Hs Negative >8.6 pKd 2
pKd >8.6 (Kd <2.5x10-9 M) [2]
Description: Binding affinity by SPR
MAK683 Small molecule or natural product Ligand has a PDB structure 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.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:1990830 cellular response to leukemia inhibitory factor IEA
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

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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. Efremov IV, Kazmirski S, Li q, Thompson LA III, Wallace OW, Johnstone SD, Zhou F, Rahl P. (2020) MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS. Patent number: WO2020190754. Assignee: FULCRUM THERAPEUTICS, INC. Priority date: 15/03/2019. Publication date: 24/09/2020.

3. 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]

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