Details of the Target

General Information of Target

Target ID LDTP04277
Target Name C-X-C chemokine receptor type 3 (CXCR3)
Gene Name CXCR3
Gene ID 2833
Synonyms
GPR9; C-X-C chemokine receptor type 3; CXC-R3; CXCR-3; CKR-L2; G protein-coupled receptor 9; Interferon-inducible protein 10 receptor; IP-10 receptor; CD antigen CD183
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVLEVSDHQVLNDAEVAALLENFSSSYDYGENESDSCCTSPPCPQDFSLNFDRAFLPALY
SLLFLLGLLGNGAVAAVLLSRRTALSSTDTFLLHLAVADTLLVLTLPLWAVDAAVQWVFG
SGLCKVAGALFNINFYAGALLLACISFDRYLNIVHATQLYRRGPPARVTLTCLAVWGLCL
LFALPDFIFLSAHHDERLNATHCQYNFPQVGRTALRVLQLVAGFLLPLLVMAYCYAHILA
VLLVSRGQRRLRAMRLVVVVVVAFALCWTPYHLVVLVDILMDLGALARNCGRESRVDVAK
SVTSGLGYMHCCLNPLLYAFVGVKFRERMWMLLLRLGCPNQRGLQRQPSSSRRDSSWSET
SEASYSGL
Target Type
Preclinical
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
[Isoform 1]: Receptor for the C-X-C chemokine CXCL9, CXCL10 and CXCL11 and mediates the proliferation, survival and angiogenic activity of human mesangial cells (HMC) through a heterotrimeric G-protein signaling pathway. Binds to CCL21. Probably promotes cell chemotaxis response.; [Isoform 2]: Receptor for the C-X-C chemokine CXCL4 and also mediates the inhibitory activities of CXCL9, CXCL10 and CXCL11 on the proliferation, survival and angiogenic activity of human microvascular endothelial cells (HMVEC) through a cAMP-mediated signaling pathway. Does not promote cell chemotaxis respons. Interaction with CXCL4 or CXCL10 leads to activation of the p38MAPK pathway and contributes to inhibition of angiogenesis. Overexpression in renal cancer cells down-regulates expression of the anti-apoptotic protein HMOX1 and promotes apoptosis.; [Isoform 3]: Mediates the activity of CXCL11.
TTD ID
T25315
Uniprot ID
P49682
DrugMap ID
TT1UCIJ
Ensemble ID
ENST00000373691.4
HGNC ID
HGNC:4540
ChEMBL ID
CHEMBL4441

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
Ishikawa (Heraklio) 02 ER SNV: p.V274A .
MOLM16 SNV: p.R326Q .
OVCAR5 SNV: p.R161L .
SKNSH SNV: p.Y160S .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C338(9.69)  LDD1703  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell C338(9.69)  LDD1703  [1]
 LDCM0024  KB05 T cell C338(12.26)  LDD1705  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transmembrane protein 14A (TMEM14A) TMEM14 family Q9Y6G1
Phospholipid transfer protein C2CD2L (C2CD2L) . O14523
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
C-X-C chemokine receptor type 4 (CXCR4) G-protein coupled receptor 1 family P61073
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Fetal and adult testis-expressed transcript protein (FATE1) . Q969F0

The Drug(s) Related To This Target

Preclinical
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jt07 Antibody DBJ36R
Dioscin Small molecular drug D0F2AD
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hypoglaucin A Small molecular drug D0T1PA
Kallstroemin D Small molecular drug D09LGT
Nbi-74330 Small molecular drug D0A8PV
Sch-900875 . D0EK9K
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
T487 Small molecular drug D0E6DI

References

1 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.