Details of the Target

General Information of Target

Target ID LDTP10675
Target Name Adhesion G protein-coupled receptor A2 (ADGRA2)
Gene Name ADGRA2
Gene ID 25960
Synonyms
GPR124; KIAA1531; TEM5; Adhesion G protein-coupled receptor A2; G-protein coupled receptor 124; Tumor endothelial marker 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKTLIAAYSGVLRGERQAEADRSQRSHGGPALSREGSGRWGTGSSILSALQDLFSVTWLN
RSKVEKQLQVISVLQWVLSFLVLGVACSAILMYIFCTDCWLIAVLYFTWLVFDWNTPKKG
GRRSQWVRNWAVWRYFRDYFPIQLVKTHNLLTTRNYIFGYHPHGIMGLGAFCNFSTEATE
VSKKFPGIRPYLATLAGNFRMPVLREYLMSGGICPVSRDTIDYLLSKNGSGNAIIIVVGG
AAESLSSMPGKNAVTLRNRKGFVKLALRHGADLVPIYSFGENEVYKQVIFEEGSWGRWVQ
KKFQKYIGFAPCIFHGRGLFSSDTWGLVPYSKPITTVVGEPITIPKLEHPTQQDIDLYHT
MYMEALVKLFDKHKTKFGLPETEVLEVN
Target Bioclass
GPCR
Family
G-protein coupled receptor 2 family, Adhesion G-protein coupled receptor (ADGR) subfamily
Subcellular location
Cell membrane
Function
Endothelial receptor which functions together with RECK to enable brain endothelial cells to selectively respond to Wnt7 signals (WNT7A or WNT7B). Plays a key role in Wnt7-specific responses, such as endothelial cell sprouting and migration in the forebrain and neural tube, and establishment of the blood-brain barrier. Acts as a Wnt7-specific coactivator of canonical Wnt signaling: required to deliver RECK-bound Wnt7 to frizzled by assembling a higher-order RECK-ADGRA2-Fzd-LRP5-LRP6 complex. ADGRA2-tethering function does not rely on its G-protein coupled receptor (GPCR) structure but instead on its combined capacity to interact with RECK extracellularly and recruit the Dishevelled scaffolding protein intracellularly. Binds to the glycosaminoglycans heparin, heparin sulfate, chondroitin sulfate and dermatan sulfate.
Uniprot ID
Q96PE1
Ensemble ID
ENST00000315215.11
HGNC ID
HGNC:17849
ChEMBL ID
CHEMBL4523909

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 Deletion: p.P1086LfsTer217
SNV: p.R1205C		 .
CCK81 Deletion: p.A525PfsTer12 .
COLO829 SNV: p.E863K .
CORL23 SNV: p.P958L .
DU145 SNV: p.A542V .
HCC15 SNV: p.G392W .
HCT15 SNV: p.R974M .
HDMYZ SNV: p.C1084S .
HT SNV: p.D462G .
IGR1 SNV: p.W724Ter .
IGROV1 Deletion: p.P1086LfsTer217 .
IM95 Deletion: p.A525PfsTer12 .
KARPAS299 SNV: p.E1245G .
KPL1 SNV: p.P434L .
KYSE30 SNV: p.A1151E .
KYSE510 SNV: p.A1195S .
MFE319 SNV: p.L237F .
MOLT4 Deletion: p.A525PfsTer12 .
NCIH1793 SNV: p.G854C .
NCIH2172 SNV: p.I480N .
NCIH2286 SNV: p.H814Q .
REH SNV: p.H1068D .
RKO SNV: p.S1011G .
RL952 Deletion: p.P1086LfsTer217
SNV: p.C783Y		 .
SHP77 Deletion: p.A242PfsTer72 .
SKMEL24 SNV: p.P708L .
SW1783 SNV: p.K1184R .
SW480 SNV: p.C1070S .
TOV21G SNV: p.G893W .
U118MG SNV: p.K1184R .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C979(2.21)  LDD3423  [1]
YN-1
 Probe Info  		N.A.  LDD0447  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A673 C979(2.42)  LDD2261  [1]
 LDCM0023  KB03 A673 C979(2.55)  LDD2678  [1]
 LDCM0024  KB05 SK-ES1 C979(2.21)  LDD3423  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Disks large homolog 1 (DLG1) MAGUK family Q12959
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-D1-binding protein 1 (CCNDBP1) CCNDBP1 family O95273

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 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.