Details of the Target

General Information of Target

Target ID LDTP10900
Target Name P2X purinoceptor 4 (P2RX4)
Gene Name P2RX4
Gene ID 5025
Synonyms
P2X purinoceptor 4; P2X4; ATP receptor; Purinergic receptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGNQLAGIAPSQILSVESYFSDIHDFEYDKSLGSTRFFKVARAKHREGLVVVKVFAIQDP
TLPLTSYKQELEELKIRLNSAQNCLPFQKASEKASEKAAMLFRQYVRDNLYDRISTRPFL
NNIEKRWIAFQILTAVDQAHKSGVRHGDIKTENVMVTSWNWVLLTDFASFKPTYLPEDNP
ADFNYFFDTSRRRTCYIAPERFVDGGMFATELEYMRDPSTPLVDLNSNQRTRGELKRAMD
IFSAGCVIAELFTEGVPLFDLSQLLAYRNGHFFPEQVLNKIEDHSIRELVTQMIHREPDK
RLEAEDYLKQQRGNAFPEIFYTFLQPYMAQFAKETFLSADERILVIRKDLGNIIHNLCGH
DLPEKAEGEPKENGLVILVSVITSCLQTLKYCDSKLAALELILHLAPRLSVEILLDRITP
YLLHFSNDSVPRVRAEALRTLTKVLALVKEVPRNDINIYPEYILPGIAHLAQDDATIVRL
AYAENIALLAETALRFLELVQLKNLNMENDPNNEEIDEVTHPNGNYDTELQALHEMVQQK
VVTLLSDPENIVKQTLMENGITRLCVFFGRQKANDVLLSHMITFLNDKNDWHLRGAFFDS
IVGVAAYVGWQSSSILKPLLQQGLSDAEEFVIVKALYALTCMCQLGLLQKPHVYEFASDI
APFLCHPNLWIRYGAVGFITVVARQISTADVYCKLMPYLDPYITQPIIQIERKLVLLSVL
KEPVSRSIFDYALRSKDITSLFRHLHMRQKKRNGSLPDCPPPEDPAIAQLLKKLLSQGMT
EEEEDKLLALKDFMMKSNKAKANIVDQSHLHDSSQKGVIDLAALGITGRQVDLVKTKQEP
DDKRARKHVKQDSNVNEEWKSMFGSLDPPNMPQALPKGSDQEVIQTGKPPRSESSAGICV
PLSTSSQVPEVTTVQNKKPVIPVLSSTILPSTYQIRITTCKTELQQLIQQKREQCNAERI
AKQMMENAEWESKPPPPGWRPKGLLVAHLHEHKSAVNRIRVSDEHSLFATCSNDGTVKIW
NSQKMEGKTTTTRSILTYSRIGGRVKTLTFCQGSHYLAIASDNGAVQLLGIEASKLPKSP
KIHPLQSRILDQKEDGCVVDMHHFNSGAQSVLAYATVNGSLVGWDLRSSSNAWTLKHDLK
SGLITSFAVDIHQCWLCIGTSSGTMACWDMRFQLPISSHCHPSRARIRRLSMHPLYQSWV
IAAVQGNNEVSMWDMETGDRRFTLWASSAPPLSELQPSPHSVHGIYCSPADGNPILLTAG
SDMKIRFWDLAYPERSYVVAGSTSSPSVSYYRKIIEGTEVVQEIQNKQKVGPSDDTPRRG
PESLPVGHHDIITDVATFQTTQGFIVTASRDGIVKVWK
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
P2X receptor family
Subcellular location
Membrane
Function
ATP-gated nonselective transmembrane cation channel permeable to potassium, sodium and calcium. Activated by extracellularly released ATP, it plays multiple role in immunity and central nervous system physiology. Plays a key role in initial steps of T-cell activation and Ca(2+) microdomain formation. Participates also in basal T-cell activity without TCR/CD3 stimulation. Promotes the differentiation and activation of Th17 cells via expression of retinoic acid-related orphan receptor C/RORC. Upon activation, drives microglia motility via the PI3K/Akt pathway. Could also function as an ATP-gated cation channel of lysosomal membranes.
TTD ID
T60330
Uniprot ID
Q99571
DrugMap ID
TT1NLOA
Ensemble ID
ENST00000337233.9
HGNC ID
HGNC:8535
ChEMBL ID
CHEMBL2104

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A431 Insertion: p.Y359LfsTer15 .
EFO27 SNV: p.P176H .
HEC1B SNV: p.H286Y .
IGR1 SNV: p.S59F DBIA    Probe Info 
MOLT4 SNV: p.Y378F .
NCIH2172 SNV: p.G147C .

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
YN-1
 Probe Info  		100.00  LDD0444  [1]
DBIA
 Probe Info  		C286(2.24)  LDD3312  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [3]
NAIA_5
 Probe Info  		N.A.  LDD2223  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2058 C286(2.46)  LDD2253  [2]
 LDCM0023  KB03 COLO-679 C286(3.54)  LDD2722  [2]
 LDCM0024  KB05 HMCB C286(2.24)  LDD3312  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin-associated protein 1-1 (KRTAP1-1) KRTAP type 1 family Q07627
Keratin-associated protein 12-3 (KRTAP12-3) KRTAP type 12 family P60328
Keratin-associated protein 5-9 (KRTAP5-9) KRTAP type 5 family P26371
Notch homolog 2 N-terminal-like protein A (NOTCH2NLA) NOTCH family Q7Z3S9
Notch homolog 2 N-terminal-like protein C (NOTCH2NLC) NOTCH family P0DPK4
Dynein axonemal assembly factor 6 (DNAAF6) PIH1 family Q9NQM4

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Eslicarbazepine Small molecular drug DB14575
Eslicarbazepine Acetate Small molecular drug DB09119
Promethazine Small molecular drug DB01069
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mrs-2160 Small molecular drug D0U0KJ

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
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 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
4 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