Prostanoid 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.
Initiated by the cyclooxygenase-mediated degradation of the unsaturated 20-carbon fatty acid arachidonic acid to PGG/H2, prostaglandins (PGs) are a broad family of metabolites that produce five main bioactive prostanoids: PGE2, PGF2α, PGD2, PGI2, and TxA2. The traditional and new applications of cyclooxygenase-inhibiting nonsteroidal anti-inflammatory medications, which nonselectively inhibit the synthesis of all of these chemicals, highlight the significance of this pathway in a wide range of disorders, including cancer, inflammation, and hypertension. Each prostanoid is created by distinct synthases in certain locations throughout the body.
Fig.1. The prostanoids. (Bos, 2004)
Creative Biolabs provides professional prostanoid family in vitro assays and related products to facilitate our customers' research, development, and applications of membrane protein drugs:
Overview of Prostanoid Family
Prostanoids may interact with the heterotrimeric G-protein-coupled, rhodopsin-type receptors that make up their distinct seven transmembrane domain receptor family. The prostanoid receptors are a subfamily of this family with remarkably low overall homology.
Fig.2. Identification of conserved residues in the EP3 receptor. (Breyerá, 2001)
- TP receptors
TxA2 production is linked to the development of atherosclerosis and myocardial infarctions because it is a potent activator of platelet aggregation and smooth muscle constriction, which results in vasoconstriction. The first eicosanoid receptor to be cloned was the human TxA2 receptor, dubbed "TP". The heterotrimeric Gq-protein is functionally linked to TP receptors. A group of signaling cascades, including the activation of phospholipase C (PLC), calcium release, and protein kinase C (PKC), are triggered by the activation of these components. This longer-lasting effects of TxA2, such as smooth muscle enlargement, may be explained by the TxA2-dependent, TP-mediated PKC enzymatic activity.
- FP receptors
PGF2α is typically linked to physiological activities like luteolysis, uterine contraction, interleukin production, hypertrophic cell development, and so forth. PGF2α has a strong affinity for the EP1 and EP3 receptors in addition to its FP receptor. Although the precise signaling mechanisms underlying PGF2α and FP effects on the MAP kinase pathway are still unclear, they almost certainly involve both Gq- and Gi-dependent signal transduction, with the relative contributions of the two pathways to the signal being highly dependent on the specific cell types and environmental factors used.
- EP receptors
PGE2 promotes inflammation, produces vasodilatation, and controls the production of several cytokines. The inflammatory lipid PGE2 activates a pleiotropic effect on signal transduction, and the actual cellular effects it has depend heavily on the receptor subtypes expressed. PGE2 had a variety of effects on different organs, pointing to the possibility of several receptor subtypes. These receptors were given the names EP1, EP2, EP3, and EP4, and each one was encoded by a different gene. Despite having a stronger affinity for PGE2 than other prostanoids, all four cloned EP receptors are not closely related to one another based on amino acid homology.
- IP receptors
Prostacyclin, commonly known as PGI2, which prevents platelet aggregation and induces vasodilatation, works in this manner to inhibit TxA2. It has been demonstrated that PGI2's interaction with its receptor IP increases Gs, and as a result, the response triggered comprises the production of cAMP, followed by the activation of PKA, but it has also been observed that Gq and Gi are activated. Gq-dependent PGI2 signaling in particular has been commonly seen.
- DP receptors
The prostanoid PGD2 is made in a variety of tissues and suppresses platelet aggregation while relaxing both vascular and non-vascular smooth muscle cells. It has been demonstrated that PGD2 binds to and activates the DP and DP2 receptors. The DP receptor is activated in a PGD2-dependent manner and mediates or promotes a number of physiological processes, including the induction of sleep, cell survival, and allergy reactions. It is still unclear what the DP2 receptor does physiologically.
References
- Bos, C. L.; et al. Prostanoids and prostanoid receptors in signal transduction. The international journal of biochemistry & cell biology. 2004, 36(7): 1187-1205.
- Breyer, R.M.; et al. Prostanoid receptors: subtypes and signaling. Annual review of pharmacology and toxicology. 2001, 41(1): 661-690.
