Tchem PTAFR Platelet-activating factor receptor

Protein Summary

Description

Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth-muscle contractile and hypotensive activity. Seems to mediate its action via a G protein that activates a phosphatidylinositol-calcium second messenger system. This gene encodes a seven-transmembrane G-protein-coupled receptor for platelet-activating factor (PAF) that localizes to lipid rafts and/or caveolae in the cell membrane. PAF (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine) is a phospholipid that plays a significant role in oncogenic transformation, tumor growth, angiogenesis, metastasis, and pro-inflammatory processes. Binding of PAF to the PAF-receptor (PAFR) stimulates numerous signal transduction pathways including phospholipase C, D, A2, mitogen-activated protein kinases (MAPKs), and the phosphatidylinositol-calcium second messenger system. Following PAFR activation, cells become rapidly desensitized and this refractory state is dependent on PAFR phosphorylation, internalization, and down-regulation. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Aug 2011]

Uniprot Accession IDs

• P25105
• A3KMC8
• A8K2H5
• PAF-R

Gene Name

• PTAFR

Ensembl ID

• ENST00000305392
• ENSP00000301974
• ENSG00000169403
• ENST00000373857
• ENSP00000362965
• ENST00000539896
• ENSP00000442658

Symbol

• PAFR
• PAFR

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	0.95
molecular function	0.79
cell type or tissue	0.69
biological term	0.67
tissue	0.66

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Platelet-activating Factor Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Platelet-activating Factor Receptor

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: 180.56   (req: < 5)

Gene RIFs: 60   (req: <= 3)

Antibodies: 173   (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: 180.56   (req: >= 5)

Gene RIFs: 60   (req: > 3)

Antibodies: 173   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 42

Tchem

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

Active Ligands: 229

Tclin

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

Active Drug: 1