Details of the Target

General Information of Target

Target ID LDTP07923
Target Name Serine/threonine-protein kinase/endoribonuclease IRE2 (ERN2)
Gene Name ERN2
Gene ID 10595
Synonyms
IRE2; Serine/threonine-protein kinase/endoribonuclease IRE2; Endoplasmic reticulum-to-nucleus signaling 2; Inositol-requiring protein 2; hIRE2p; Ire1-beta; IRE1b) [Includes: Serine/threonine-protein kinase; EC 2.7.11.1; Endoribonuclease; EC 3.1.26.-)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASAVRGSRPWPRLGLQLQFAALLLGTLSPQVHTLRPENLLLVSTLDGSLHALSKQTGDL
KWTLRDDPVIEGPMYVTEMAFLSDPADGSLYILGTQKQQGLMKLPFTIPELVHASPCRSS
DGVFYTGRKQDAWFVVDPESGETQMTLTTEGPSTPRLYIGRTQYTVTMHDPRAPALRWNT
TYRRYSAPPMDGSPGKYMSHLASCGMGLLLTVDPGSGTVLWTQDLGVPVMGVYTWHQDGL
RQLPHLTLARDTLHFLALRWGHIRLPASGPRDTATLFSTLDTQLLMTLYVGKDETGFYVS
KALVHTGVALVPRGLTLAPADGPTTDEVTLQVSGEREGSPSTAVRYPSGSVALPSQWLLI
GHHELPPVLHTTMLRVHPTLGSGTAETRPPENTQAPAFFLELLSLSREKLWDSELHPEEK
TPDSYLGLGPQDLLAASLTAVLLGGWILFVMRQQQPQVVEKQQETPLAPADFAHISQDAQ
SLHSGASRRSQKRLQSPSKQAQPLDDPEAEQLTVVGKISFNPKDVLGRGAGGTFVFRGQF
EGRAVAVKRLLRECFGLVRREVQLLQESDRHPNVLRYFCTERGPQFHYIALELCRASLQE
YVENPDLDRGGLEPEVVLQQLMSGLAHLHSLHIVHRDLKPGNILITGPDSQGLGRVVLSD
FGLCKKLPAGRCSFSLHSGIPGTEGWMAPELLQLLPPDSPTSAVDIFSAGCVFYYVLSGG
SHPFGDSLYRQANILTGAPCLAHLEEEVHDKVVARDLVGAMLSPLPQPRPSAPQVLAHPF
FWSRAKQLQFFQDVSDWLEKESEQEPLVRALEAGGCAVVRDNWHEHISMPLQTDLRKFRS
YKGTSVRDLLRAVRNKKHHYRELPVEVRQALGQVPDGFVQYFTNRFPRLLLHTHRAMRSC
ASESLFLPYYPPDSEARRPCPGATGR
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family
Subcellular location
Endoplasmic reticulum membrane
Function Induces translational repression through 28S ribosomal RNA cleavage in response to ER stress. Pro-apoptotic. Appears to play no role in the unfolded-protein response, unlike closely related proteins.
Uniprot ID
Q76MJ5
Ensemble ID
ENST00000256797.9
HGNC ID
HGNC:16942
ChEMBL ID
CHEMBL4105932

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C816(2.72)  LDD3319  [1]
NAIA_5
 Probe Info  		C664(20.00)  LDD2227  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C664(20.00)  LDD2227  [2]
 LDCM0022  KB02 AGS C579(1.32)  LDD2263  [1]
 LDCM0023  KB03 AGS C579(1.29)  LDD2680  [1]
 LDCM0024  KB05 MEWO C816(2.72)  LDD3319  [1]

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 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
3 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