Adenosine 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 has developed a comprehensive list of membrane protein tools to support the development of antibody and other therapeutic. We are dedicated to bringing more value to our clients by providing stock products, more technical resources and custom protein production services.
Creative Biolabs' membrane preparations are useful for membrane protein research. We offer membrane preparations to study the role of membrane proteins in diseases. Membrane preparations from Creative Biolabs are quality-assured frozen membranes from cells expressing recombinant or natural receptors.
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.
Adenosine receptors are evolutionarily well conserved subgroup of G protein-coupled receptors. They are designated A1, A2A, A2B, and A3. The first and the last couple primarily to G proteins of the Gi family, whereas the two A2 receptors couple primarily to members of the Gs family. However, the receptors have the potential to connect to additional G protein pathways, particularly when overexpressed. Creative Biolabs offers high-quality, innovative tools and solutions to help research groups accelerate drug discovery and development projects of adenosine family.
Fig.1 Local amplification of adenosine signaling in response to insults or hypoxia. (Chen,
2013)
To meet our customers' specific requirements, Creative Biolabs provides a full range of assays and products in adenosine family drug discovery:
Overview of Adenosine Receptors
The A1 receptor is the most commonly expressed adenosine receptor subtype across all species, and it is concentrated in the brain, particularly at excitatory nerve terminals. Inhibiting adenylyl cyclase activity, activating potassium channels, blocking transient calcium channels, and increasing intracellular calcium and inositol-1,4,5-triphosphate (Ins(1,4,5)P3) levels through the activation of phospholipase C are all effects of A1 receptor activation (PLC).
The striatum of the brain, immune cells in the spleen, thymus, leukocytes, and blood platelets, as well as the heart, lung, and blood arteries, all contain high concentrations of the A2A receptor. By connecting to either the Gs protein in peripheral tissues or the Golf protein in the brain, A2A receptor activation activates the cyclic AMP-protein kinase A (PKA) pathway. Several neurotransmitters interact with A2A receptors in the brain to control motor activity, psychiatric behaviors, the sleep-wake cycle, and neuronal cell death. A2A receptors are essential for the control of cancer etiology, angiogenesis, myocardial oxygen consumption, coronary blood flow, and inflammation in peripheral tissues.
Although A2B receptors are expressed broadly, they are often not abundant. The A2B receptor is the least adenosine-sensitive of the four adenosine receptors, necessitating micromolar adenosine concentrations, which are rarely reached under physiological conditions. Despite stimulating mitogen-activated protein kinase (MAPK) activity with a similar affinity to A2A receptors in cultured cells, the A2B receptor is the most adenosine-insensitive. Functional roles of the A2B receptor signaling have been described in genetic and pharmacological studies during situations where adenosine levels are elevated, such as hypoxia, ischaemia, or inflammation; these roles include tissue adaptation to hypoxia, increased ischaemia tolerance, or attenuation of acute inflammation.
The pharmacology, location, and hence function, of A3 receptors, vary significantly between species. A3 receptor signaling has been connected to mast cell degranulation in mice, but things might be different in people. When compared to healthy individuals, blood cells from patients with rheumatoid arthritis, Crohn's disease, and colon cancer had higher levels of A3 receptor expression, which was correlated with higher levels of nuclear factor-κB (NF-κB) signaling and the phosphoinositide 3-kinase (PI3K)-PKB-AKT signaling pathways.
Targeting Adenosine Receptors
The process of finding new drugs has been facilitated by the introduction of suitable radioligands targeting adenosine receptors. Unlike certain other GPCRs, adenosine receptor research and medication development are not constrained by a lack of selective ligands. Additionally, ongoing efforts in medicinal chemistry are being made to create novel adenosine ligands with enhanced in vivo biodistribution, tissue selectivity, and structure-activity correlations, all of which are essential for druggability.
Reference
- Chen, J.F.; et al. Adenosine receptors as drug targets-what are the challenges? Nature reviews Drug discovery. 2013, 12(4): 265-286.
