Tchem CXCR3 C-X-C chemokine receptor type 3

Protein Summary

Description

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 (PubMed:12782716). 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 (PubMed:12782716). 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. This gene encodes a G protein-coupled receptor with selectivity for three chemokines, termed CXCL9/Mig (monokine induced by interferon-g), CXCL10/IP10 (interferon-g-inducible 10 kDa protein) and CXCL11/I-TAC (interferon-inducible T cell a-chemoattractant). Binding of chemokines to this protein induces cellular responses that are involved in leukocyte traffic, most notably integrin activation, cytoskeletal changes and chemotactic migration. Alternatively spliced transcript variants encoding different isoforms have been found for this gene. One of the isoforms (CXCR3-B) shows high affinity binding to chemokine, CXCL4/PF4 (PMID:12782716). [provided by RefSeq, Jun 2011]

Uniprot Accession IDs

• P49682
• B2R982
• O15185
• Q7Z710
• Q9P2T4
• Q9P2T5
• CXC-R3

Gene Name

• CXCR3

Ensembl ID

• ENST00000373691
• ENSP00000362795
• ENSG00000186810
• ENST00000373693
• ENSP00000362797

Symbol

• GPR9
• GPR9
• MigR
• CD182
• CD183
• Mig-R
• CKR-L2
• CMKAR3
• IP10-R

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (protein)	1
biological term	0.98
gene perturbation	0.69
cell type or tissue	0.68
molecular function	0.6

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Chemokine Receptor / C-x-c Chemokine Receptor / C-x-c Chemokine Receptor Type 3

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1152.13   (req: < 5)

Gene RIFs: 288   (req: <= 3)

Antibodies: 966   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1152.13   (req: >= 5)

Gene RIFs: 288   (req: > 3)

Antibodies: 966   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 32

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 739

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0