Tclin CXCR4 C-X-C chemokine receptor type 4

Protein Summary

Description

Receptor for the C-X-C chemokine CXCL12/SDF-1 that transduces a signal by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation (PubMed:10452968, PubMed:28978524, PubMed:18799424, PubMed:24912431). Involved in the AKT signaling cascade (PubMed:24912431). Plays a role in regulation of cell migration, e.g. during wound healing (PubMed:28978524). Acts as a receptor for extracellular ubiquitin; leading to enhanced intracellular calcium ions and reduced cellular cAMP levels (PubMed:20228059). Binds bacterial lipopolysaccharide (LPS) et mediates LPS-induced inflammatory response, including TNF secretion by monocytes (PubMed:11276205). Involved in hematopoiesis and in cardiac ventricular septum formation. Also plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Involved in cerebellar development. In the CNS, could mediate hippocampal-neuron survival (By similarity). (Microbial infection) Acts as a coreceptor (CD4 being the primary receptor) for human immunodeficiency virus-1/HIV-1 X4 isolates and as a primary receptor for some HIV-2 isolates. Promotes Env-mediated fusion of the virus (PubMed:8849450, PubMed:8929542, PubMed:9427609, PubMed:10074122, PubMed:10756055). This gene encodes a CXC chemokine receptor specific for stromal cell-derived factor-1. The protein has 7 transmembrane regions and is located on the cell surface. It acts with the CD4 protein to support HIV entry into cells and is also highly expressed in breast cancer cells. Mutations in this gene have been associated with WHIM (warts, hypogammaglobulinemia, infections, and myelokathexis) syndrome. Alternate transcriptional splice variants, encoding different isoforms, have been characterized. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P61073
• B2R5N0
• O60835
• P30991
• P56438
• Q53S69
• Q9BXA0
• Q9UKN2
• CXC-R4

Gene Name

• CXCR4

Ensembl ID

• ENST00000241393
• ENSP00000241393
• ENSG00000121966
• ENST00000409817
• ENSP00000386884

Symbol

• FB22
• HM89
• LAP3
• LCR1
• NPYR
• WHIM
• CD184
• LAP-3
• LESTR
• NPY3R
• NPYRL
• WHIMS
• HSY3RR
• NPYY3R
• D2S201E

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	0.99
PubMedID	0.99
transcription factor perturbation	0.99
gene perturbation	0.98
virus perturbation	0.97

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 4

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: 4274.44   (req: < 5)

Gene RIFs: 1605   (req: <= 3)

Antibodies: 1625   (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: 4274.44   (req: >= 5)

Gene RIFs: 1605   (req: > 3)

Antibodies: 1625   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 35

Tchem

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

Active Ligands: 386

Tclin

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

Active Drug: 1