Details of the Target

General Information of Target

Target ID LDTP05916
Target Name Eukaryotic translation initiation factor 4E-binding protein 2 (EIF4EBP2)
Gene Name EIF4EBP2
Gene ID 1979
Synonyms
Eukaryotic translation initiation factor 4E-binding protein 2; 4E-BP2; eIF4E-binding protein 2
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MSSSAGSGHQPSQSRAIPTRTVAISDAAQLPHDYCTTPGGTLFSTTPGGTRIIYDRKFLL
DRRNSPMAQTPPCHLPNIPGVTSPGTLIEDSKVEVNNLNNLNNHDRKHAVGDDAQFEMDI
Target Type
Clinical trial
Target Bioclass
Other
Family
EIF4E-binding protein family
Function
Repressor of translation initiation involved in synaptic plasticity, learning and memory formation. Regulates EIF4E activity by preventing its assembly into the eIF4F complex: hypophosphorylated form of EIF4EBP2 competes with EIF4G1/EIF4G3 and strongly binds to EIF4E, leading to repress translation. In contrast, hyperphosphorylated form dissociates from EIF4E, allowing interaction between EIF4G1/EIF4G3 and EIF4E, leading to initiation of translation. EIF4EBP2 is enriched in brain and acts as a regulator of synapse activity and neuronal stem cell renewal via its ability to repress translation initiation. Mediates the regulation of protein translation by hormones, growth factors and other stimuli that signal through the MAP kinase and mTORC1 pathways.
TTD ID
T80011
Uniprot ID
Q13542
DrugMap ID
TTNBTCW
Ensemble ID
ENST00000373218.5
HGNC ID
HGNC:3289

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C-Sul
 Probe Info  		16.51  LDD0066  [1]
DBIA
 Probe Info  		C35(1.96)  LDD3401  [2]
5E-2FA
 Probe Info  		H74(0.00); H9(0.00); H32(0.00)  LDD2235  [3]
m-APA
 Probe Info  		H74(0.00); H9(0.00); H32(0.00)  LDD2231  [3]
IA-alkyne
 Probe Info  		N.A.  LDD0177  [4]
NAIA_4
 Probe Info  		C35(0.00); C73(0.00)  LDD2226  [5]
NAIA_5
 Probe Info  		N.A.  LDD2224  [5]
Compound 10
 Probe Info  		N.A.  LDD2216  [6]
Compound 11
 Probe Info  		N.A.  LDD2213  [6]
IPM
 Probe Info  		C35(0.00); C73(0.00)  LDD2156  [7]
VSF
 Probe Info  		C35(0.00); C73(0.00)  LDD0007  [8]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0634  CY-0357 Hep-G2 C35(0.77)  LDD2228  [5]
 LDCM0625  F8 Ramos C35(1.06)  LDD2187  [10]
 LDCM0572  Fragment10 Ramos C35(0.94)  LDD2189  [10]
 LDCM0573  Fragment11 Ramos C35(0.41)  LDD2190  [10]
 LDCM0574  Fragment12 Ramos C35(0.81)  LDD2191  [10]
 LDCM0575  Fragment13 Ramos C35(0.75)  LDD2192  [10]
 LDCM0576  Fragment14 Ramos C35(0.53)  LDD2193  [10]
 LDCM0579  Fragment20 Ramos C35(0.89)  LDD2194  [10]
 LDCM0580  Fragment21 Ramos C35(1.04)  LDD2195  [10]
 LDCM0582  Fragment23 Ramos C35(1.93)  LDD2196  [10]
 LDCM0578  Fragment27 Ramos C35(1.22)  LDD2197  [10]
 LDCM0586  Fragment28 Ramos C35(0.44)  LDD2198  [10]
 LDCM0588  Fragment30 Ramos C35(1.01)  LDD2199  [10]
 LDCM0589  Fragment31 Ramos C35(0.93)  LDD2200  [10]
 LDCM0590  Fragment32 Ramos C35(1.04)  LDD2201  [10]
 LDCM0468  Fragment33 Ramos C35(1.00)  LDD2202  [10]
 LDCM0596  Fragment38 Ramos C35(1.02)  LDD2203  [10]
 LDCM0566  Fragment4 Ramos C35(1.13)  LDD2184  [10]
 LDCM0610  Fragment52 Ramos C35(0.71)  LDD2204  [10]
 LDCM0614  Fragment56 Ramos C35(1.01)  LDD2205  [10]
 LDCM0569  Fragment7 Ramos C35(0.64)  LDD2186  [10]
 LDCM0571  Fragment9 Ramos C35(1.12)  LDD2188  [10]
 LDCM0022  KB02 Ramos C35(1.02)  LDD2182  [10]
 LDCM0023  KB03 Ramos C35(0.86)  LDD2183  [10]
 LDCM0024  KB05 RD C35(1.96)  LDD3401  [2]
 LDCM0131  RA190 MM1.R C35(0.75)  LDD0304  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Eukaryotic translation initiation factor 4E (EIF4E) Eukaryotic initiation factor 4E family P06730

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis-eif4e Antisense drug D08HQI
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 232828 Antisense drug D0FI9M
Isis 347573 Antisense drug D0W3RV
Isis 347577 Antisense drug D0QE7H

References

1 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
4 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
5 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
6 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
7 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
8 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
9 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
10 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
11 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.