Platelet-activating Factor GPCR Assays
Background of PAFR
Platelet-activating factor (PAF) is a unique phospholipid compound, mainly produced by cell membranes. PAF exerts a variety of biological functions by activating its cognate receptor, the PAF receptor (PAFR), which is a member of the G protein-coupled receptor superfamily. Studies revealed that the PAF/PAFR system contributes to the regulation of peripheral tissues and the nervous system.
Roles of PAFR
PAFR is expressed on the surface of various cells and tissues over the body, such as the central nervous system, muscle, and inflammatory cells. PAFR is closely related to immune responses as well as cardiovascular, reproductive, respiratory, and nervous system regulation. Furthermore, PAFR is involved in diverse disease processes. Growing evidence suggests that PAFRs are attractive drug targets for therapy, inflammation, asthma, and cardiovascular disease.
Fig.1 PAFR signaling pathway through Gq and Gi protein. (Singh, 2013)
PAFR Signaling Pathways
PAFR is a Gq/G11-coupled protein receptor that functions in numerous biological processes. PAFR is involved in multiple intracellular signaling pathways, including the p38 MAPK and PI 3-K pathways.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| PAFR | PTAFR |
|
|
|
Assay List of Platelet-activating Factor Receptor
Creative Biolabs can provide a range of assays of platelet-activating factor receptor. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| cAMP Assay | ||||
| S01YF-1122-KX811 | Magic™ Human PTAFR In Vitro cAMP Assay | CHO-K1 | cAMP Assay | |
| Calcium Flux Assay | ||||
| S01YF-0722-KX184 | Magic™ Human PTAFR In Vitro Calcium Assay & Reporter Assay, HEK293-NFAT-βla | HEK293-NFAT-βla | Calcium Assay; Reporter Assay | |
Published Data
| Paper Title | Progress in the Development of Platelet-Activating Factor Receptor (PAFr) Antagonists and Applications in the Treatment of Inflammatory Diseases |
| Journal | ChemMedChem |
| Published | 2018 |
| Abstract | PAF and its receptor PAFR are closely related to a variety of diseases arising from the activation of inflammatory pathways. Although the exact structure of the binding site on PAFR remains unclear, PAFR is considered to be a mature and attractive therapeutic target and a series of structurally distinct PAFR antagonists have been identified. These include compounds structurally similar to natural PAF ligands, synthetic heterocycles, complex polycyclic natural products, and various metal complexes. |
| Result |
PAF and PAFR are closely associated with a variety of different disease states, such as cancer, lung disease, and neurodegenerative diseases. A series of structurally diverse molecules have been demonstrated to act as PAFR antagonists. Nonetheless, specific therapeutic applications of PAFR antagonists have some limitations. In recent years, synthetic strategies for the construction of more complex antagonists have been developed, and new and efficient methods have been developed. Many metal-based complexes have recently demonstrated potent PAFR antagonistic activity. Structurally related synthetic PAF derivatives show good potency and selectivity, but suffer from toxicity and bioavailability concerns. Recently, heterocyclic compounds that do not contain a diazide core have emerged as potent antagonists. PAF and PAFR and their roles in biological functions have been elucidated in detail, laying the foundation for exploring related therapeutic strategies.
|
Fig.2 Metal complexes 12-15. (Hyland, 2018)
References
- Singh, P.; Singh, I. N. Platelet-activating factor (PAF)-antagonists of natural origin. Fitoterapia. 2013, 84: 180-201.
- Hyland, I.K.; et al. Progress in the Development of Platelet-Activating Factor Receptor (PAFr) Antagonists and Applications in the Treatment of Inflammatory Diseases. ChemMedChem. 2018, 13(18): 1873-1884.
