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

Knowledge Summary

Patent (8,806)

Expression

Synonym

Accession P25105 A3KMC8 A8K2H5 PAF-R
Symbols PAFR

Gene

PANTHER Protein Class (2)

PDB

2B0X  

  TechDev Info (1)

MLP Assay (10)

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)

Gene RIF (52)

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
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AA Sequence

MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLTMADMLFLITL      1 - 70
PLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVTRPIKTAQANTRKRGISLSLV     71 - 140
IWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKGSVPVLIIHIFIVFSFFLVFLIILFCNLVII    141 - 210
RTLLMQPVQQQRNAEVKRRALWMVCTVLAVFIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLC    211 - 280
LLSTNCVLDPVIYCFLTKKFRKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN            281 - 342
//

Text Mined References (82)

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...