General Information of Target

Target ID LDTP06065
Target Name Inhibitor of nuclear factor kappa-B kinase subunit epsilon (IKBKE)
Gene Name IKBKE
Gene ID 9641
Synonyms
IKKE; IKKI; KIAA0151; Inhibitor of nuclear factor kappa-B kinase subunit epsilon; I-kappa-B kinase epsilon; IKK-E; IKK-epsilon; IkBKE; EC 2.7.11.10; Inducible I kappa-B kinase; IKK-i
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQSTANYLWHTDDLLGQGATASVYKARNKKSGELVAVKVFNTTSYLRPREVQVREFEVLR
KLNHQNIVKLFAVEETGGSRQKVLVMEYCSSGSLLSVLESPENAFGLPEDEFLVVLRCVV
AGMNHLRENGIVHRDIKPGNIMRLVGEEGQSIYKLTDFGAARELDDDEKFVSVYGTEEYL
HPDMYERAVLRKPQQKAFGVTVDLWSIGVTLYHAATGSLPFIPFGGPRRNKEIMYRITTE
KPAGAIAGAQRRENGPLEWSYTLPITCQLSLGLQSQLVPILANILEVEQAKCWGFDQFFA
ETSDILQRVVVHVFSLSQAVLHHIYIHAHNTIAIFQEAVHKQTSVAPRHQEYLFEGHLCV
LEPSVSAQHIAHTTASSPLTLFSTAIPKGLAFRDPALDVPKFVPKVDLQADYNTAKGVLG
AGYQALRLARALLDGQELMFRGLHWVMEVLQATCRRTLEVARTSLLYLSSSLGTERFSSV
AGTPEIQELKAAAELRSRLRTLAEVLSRCSQNITETQESLSSLNRELVKSRDQVHEDRSI
QQIQCCLDKMNFIYKQFKKSRMRPGLGYNEEQIHKLDKVNFSHLAKRLLQVFQEECVQKY
QASLVTHGKRMRVVHETRNHLRLVGCSVAACNTEAQGVQESLSKLLEELSHQLLQDRAKG
AQASPPPIAPYPSPTRKDLLLHMQELCEGMKLLASDLLDNNRIIERLNRVPAPPDV
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family, I-kappa-B kinase subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine kinase that plays an essential role in regulating inflammatory responses to viral infection, through the activation of the type I IFN, NF-kappa-B and STAT signaling. Also involved in TNFA and inflammatory cytokines, like Interleukin-1, signaling. Following activation of viral RNA sensors, such as RIG-I-like receptors, associates with DDX3X and phosphorylates interferon regulatory factors (IRFs), IRF3 and IRF7, as well as DDX3X. This activity allows subsequent homodimerization and nuclear translocation of the IRF3 leading to transcriptional activation of pro-inflammatory and antiviral genes including IFNB. In order to establish such an antiviral state, IKBKE forms several different complexes whose composition depends on the type of cell and cellular stimuli. Thus, several scaffolding molecules including IPS1/MAVS, TANK, AZI2/NAP1 or TBKBP1/SINTBAD can be recruited to the IKBKE-containing-complexes. Activated by polyubiquitination in response to TNFA and interleukin-1, regulates the NF-kappa-B signaling pathway through, at least, the phosphorylation of CYLD. Phosphorylates inhibitors of NF-kappa-B thus leading to the dissociation of the inhibitor/NF-kappa-B complex and ultimately the degradation of the inhibitor. In addition, is also required for the induction of a subset of ISGs which displays antiviral activity, may be through the phosphorylation of STAT1 at 'Ser-708'. Phosphorylation of STAT1 at 'Ser-708' seems also to promote the assembly and DNA binding of ISGF3 (STAT1:STAT2:IRF9) complexes compared to GAF (STAT1:STAT1) complexes, in this way regulating the balance between type I and type II IFN responses. Protects cells against DNA damage-induced cell death. Also plays an important role in energy balance regulation by sustaining a state of chronic, low-grade inflammation in obesity, wich leads to a negative impact on insulin sensitivity. Phosphorylates AKT1.
Uniprot ID
Q14164
Ensemble ID
ENST00000581977.7
HGNC ID
HGNC:14552
ChEMBL ID
CHEMBL3529

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AU565 SNV: p.R706W .
CCK81 Deletion: p.F335SfsTer45 .
HCT15 SNV: p.G208Ter .
HEC1 SNV: p.Y568S .
MEWO SNV: p.L654F .
MOLT4 SNV: p.R143C .
NCIH716 SNV: p.A630G .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C33(2.31)  LDD3313  [1]
IA-alkyne
 Probe Info 
C545(5.26); C546(0.00)  LDD1703  [2]
ATP probe
 Probe Info 
N.A.  LDD0199  [3]
ATP probe
 Probe Info 
N.A.  LDD0035  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell C545(5.26); C546(0.00)  LDD1703  [2]
 LDCM0023  KB03 A3-KAW C33(1.79)  LDD2674  [1]
 LDCM0024  KB05 Hs 936.T C33(2.31)  LDD3313  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
ATP-dependent RNA helicase DDX3X (DDX3X) DEAD box helicase family O00571
Interferon-induced helicase C domain-containing protein 1 (IFIH1) Helicase family Q9BYX4
Ubiquitin carboxyl-terminal hydrolase isozyme L1 (UCHL1) Peptidase C12 family P09936
Serine/threonine-protein kinase TBK1 (TBK1) Ser/Thr protein kinase family Q9UHD2
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hsp90 co-chaperone Cdc37 (CDC37) CDC37 family Q16543
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Interferon regulatory factor 3 (IRF3) IRF family Q14653
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid protein-binding protein 2 (APPBP2) . Q92624
Mitochondrial antiviral-signaling protein (MAVS) . Q7Z434
TANK-binding kinase 1-binding protein 1 (TBKBP1) . A7MCY6
TRAF family member-associated NF-kappa-B activator (TANK) . Q92844

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010

References

1 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
2 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
3 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
4 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096