| Tchem | Platelet-activating factor receptor |
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]
Comments
Property Summary
| NCBI Gene PubMed Count | 81 |
| Grant Count | 79 |
| R01 Count | 50 |
| Funding | $10,082,811.63 |
| PubMed Score | 105.96 |
| PubTator Score | 254.01 |
| Disease | log2 FC | p |
|---|---|---|
| hepatocellular carcinoma | 1.300 | 0.000 |
| pancreatic cancer | 1.900 | 0.000 |
| psoriasis | 1.500 | 0.006 |
| osteosarcoma | -1.401 | 0.008 |
| medulloblastoma, large-cell | -1.300 | 0.000 |
| fascioscapulohumeral muscular dystrophy | -1.100 | 0.001 |
| juvenile dermatomyositis | -1.143 | 0.000 |
| Amyotrophic Lateral Sclerosis | -1.089 | 0.001 |
| tuberculosis and treatment for 3 months | 1.300 | 0.000 |
| ulcerative colitis | 1.400 | 0.000 |
| interstitial cystitis | 1.200 | 0.002 |
| cystic fibrosis | 1.100 | 0.000 |
| pancreatic carcinoma | 1.900 | 0.000 |
| gastric carcinoma | 1.300 | 0.018 |
| mucosa-associated lymphoid tissue lympho... | 1.052 | 0.008 |
| ovarian cancer | -1.400 | 0.000 |
CHEMBL33139
pIC50 7.00
CHEMBL300463
pIC50 7.00
CHEMBL283152
pIC50 7.00
CHEMBL20141
pIC50 7.00
CHEMBL36269
pIC50 7.00
CHEMBL37809
pIC50 7.00
CHEMBL143914
pIC50 7.00
CHEMBL20591
pIC50 7.00
CHEMBL288098
pIC50 7.00
CHEMBL369194
pIC50 7.00
CHEMBL52821
pIC50 7.00
CHEMBL280164
pIC50 7.03
CHEMBL160571
pIC50 7.04
CHEMBL328833
pIC50 7.05
CHEMBL20690
pIC50 7.05
CHEMBL57510
pIC50 7.07
CHEMBL286229
pIC50 7.10
CHEMBL296169
pIC50 7.10
CHEMBL281780
pIC50 7.10
CHEMBL21026
pIC50 7.13
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 686924 | other |
0 / 0 / 1 | ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound) |
| 686925 | other |
0 / 0 / 1 | ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound) |
| 686926 | other |
0 / 0 / 1 | ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound) |
| 686927 | other |
0 / 0 / 1 | ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound) |
| 743249 | screening |
1 / 0 / 0 | Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM) |
| 743250 | screening |
1 / 0 / 0 | Discovery and characterization of a small molecule allosteric agonists of mas-related G-Protein coupled receptor X1 ( MrgX1) |
| 743251 | screening |
1 / 0 / 0 | Development of a novel orthosteric Muscarinic 5 (M5) antagonist possessing a hig degree of muscarinic subtype selectivity |
| 743252 | screening |
1 / 0 / 0 | Development of the first CNS penetrant Muscarinic 5 (M5) Positive Allosteric Modulator based on a novel non-isatin core |
| 743435 | other |
0 / 0 / 0 | Development of inhibitors for Dopamine D4 Receptors: Eurofin Panel Assay Results |
| 743437 | other |
0 / 0 / 0 | Development of inhibitors for PLD2 (Eurofin Panel Assay Results) |
| PMID | Text |
|---|---|
| 26359459 | PAFR is overexpressed in NSCLC as well as in breast, colorectal, and gastric carcinomas. PAFR expression correlates with clinical stages, survival time, and distant metastasis. PAF/PAFR signaling also upregulated IL6 expression and STAT3 activation. |
| 25639872 | we made the first demonstration that dysregulation of PAFR and the positive regulatory loop between PAFR and pAKT contribute to malignant progression of esophageal squamous cell carcinoma |
| 25182608 | Data support an important role for PAFR in tumor growth and suggest that engagement of PAFR interferes with selected pathways in macrophages, changing their phenotype into that of a regulatory with suppressor activities. [review] |
| 25143722 | Epithelial PAFr expression is upregulated in smokers, especially in those with COPD, and is not obviously affected by inhaled corticosteroid therapy. |
| 24921917 | PAFR may have an important role in modulating the cisplatin sensitivity of ovarian cancer cells. |
| 24886678 | Results suggest that WEB2086 and AG1478 are synergistic in ovarian cancer cells with high expression of both platelet-activating factor receptor (PAFR) and epidermal growth factor receptor (EGFR). |
| 24824933 | patients presenting elevated PAFR expression had significantly longer survival times compared to those with low PAFR expression (log-rank test, p<0.001). |
| 24289152 | Data suggest PAF/PAF receptor signaling exerts proinflammatory effect on neutrophil via down-regulation of LXRa (liver X receptor alpha) and target genes (ATP-binding cassette transporter (ABC) A1, ABC G1, sterol response element binding protein 1c). |
| 24130805 | oxLDL induces the recruitment of PAFR and CD36 into the same lipid rafts, which is important for oxLDL uptake and IL-10 production |
| 24062612 | oxLDL induces alternative macrophage activation by mechanisms involving CD36 and PAFR |
| More... |
MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLTMADMLFLITL 1 - 70 PLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVTRPIKTAQANTRKRGISLSLV 71 - 140 IWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKGSVPVLIIHIFIVFSFFLVFLIILFCNLVII 141 - 210 RTLLMQPVQQQRNAEVKRRALWMVCTVLAVFIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLC 211 - 280 LLSTNCVLDPVIYCFLTKKFRKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN 281 - 342 //
| PMID | Year | Title |
|---|---|---|
| 26359459 | 2015 | Feed-Forward Reciprocal Activation of PAFR and STAT3 Regulates Epithelial-Mesenchymal Transition in Non-Small Cell Lung Cancer. |
| 25639872 | 2015 | Platelet-activating factor receptor-mediated PI3K/AKT activation contributes to the malignant development of esophageal squamous cell carcinoma. |
| 25182608 | 2014 | PAF receptor and tumor growth. |
| 25143722 | 2014 | Airway epithelial platelet-activating factor receptor expression is markedly upregulated in chronic obstructive pulmonary disease. |
| 24921917 | 2014 | The expression of platelet-activating factor receptor modulates the cisplatin sensitivity of ovarian cancer cells: a novel target for combination therapy. |
| 24886678 | 2014 | Synergistic effects of combined platelet-activating factor receptor and epidermal growth factor receptor targeting in ovarian cancer cells. |
| 24824933 | 2014 | Platelet-activating factor (PAF) receptor expression is associated with histopathological stage and grade and patients' survival in gastric adenocarcinoma. |
| 24289152 | 2014 | Platelet-activating factor downregulates the expression of liver X receptor-? and its target genes in human neutrophils. |
| 24130805 | 2013 | Uptake of oxLDL and IL-10 production by macrophages requires PAFR and CD36 recruitment into the same lipid rafts. |
| 24062612 | 2013 | Oxidized LDL induces alternative macrophage phenotype through activation of CD36 and PAFR. |
| More... |
