P2Y Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
In the early stages of evolution, nucleotides were likely among the earliest transmitters utilized for cell communication. All cell types in the human body contain their receptors. The broad class of G-protein-coupled receptors, which includes the purine- and pyrimidine-sensitive P2Y receptors, is the target of around one-third of the pharmaceuticals currently utilized in clinical settings. The ADP-sensitive P2Y1, P2Y12, and P2Y13, the UTP- and ATP-sensitive P2Y2 and P2Y4, the UDP-sensitive P2Y6, the ATP-sensitive P2Y11, and the UDP and UDP-glucose sensitive P2Y14 have all been cloned.
Fig.1. Genomic clustering of P2Y receptors. (Jacobson, 2020)
Creative Biolabs organized a professional bioinformatics team to provide our customers with P2Y family drug discovery assays and related products:
Overview of P2Y Family
- P2Y1 receptor
The cloned P2Y1 receptor was discovered to respond favorably to both ADP and ATP. The pharmacological characteristics were comparable to the functionally described P2Y receptor's ability to elevate intracellular calcium concentration in a range of tissues, such as smooth muscle, endothelium, and neuronal tissue.
- P2Y2 receptor
Like the functionally characterized P2U-receptor, the receptor is activated by both ATP and UTP. Gq and phospholipase C activation are the primary signaling mechanisms used by the P2Y2 receptor. Selective P2Y2 receptor agonists include analogues of 2-thio-UTP and similar compounds. In addition to Up4U, the P2Y2 receptor reacts to dinucleoside polyphosphates.
- P2Y4 receptor
UTP activates the human P2Y4 receptor. ATP, UDP and ADP are inactive. In actuality, ATP functions at the human receptor as a competitive antagonist. Gq/phospholipase C-β is the primary signaling pathway for the P2Y4 receptor. Effects on M-type K+ channels and N-type Ca2+ channels have also been shown.
- P2Y6 receptor
Adenine nucleotides are virtually inactive at the P2Y6 receptor, which prefers uridine diphosphate, with UDP being far more powerful than UTP. Through the use of phospholipase C-β isozymes, the receptor forms a coupling with Gq and triggers inositol lipid signaling.
- P2Y11 receptor
The human P2Y11 receptor's main physiological agonist is ATP. In 1321N1 human astrocytoma cells, the recombinant human receptor binds to Gq and activates inositol lipid hydrolysis. Adenylyl cyclase activity rose as a result of this receptor's activation.
- P2Y12 receptor
The natural agonist of the P2Y12 receptor is ADP. Members of the Gi family of heterotrimeric G proteins couple with the P2Y12 receptor. This prevents the buildup of cyclic AMP and triggers additional downstream signaling activities.
- P2Y13 receptor
ADP is preferred by the P2Y13 receptor. In terms of efficacy at the P2Y13 receptor, ATP and 2-methylthio-ATP seem to be partial agonists. The P2Y13 receptor cooperates with Gi-proteins to inhibit adenylyl cyclase and to support further Gidependent cell signaling reactions.
- P2Y14 receptor
The P2Y14 receptor is activated by UDP and UDP-glucose. The P2Y14 receptor couples to Gi/o and shares 47% of its genetic makeup with the P2Y12 and P2Y13 receptors.
Reference
- Jacobson, K.A.; et al. Update of P2Y receptor pharmacology: IUPHAR Review 27. British Journal of Pharmacology. 2020, 177(11): 2413-2433.
