This site features trending Adenosine Receptors-linked items from the web for 5 of August 2019.
Trending Adenosine Receptors news item:
iTeos Therapeutics Initiates Phase 1/1b Trial with Differentiated Adenosine A2A Antagonist in Patients with Advanced Cancer Gosselies, Belgium and Cambridge, MA – April 17, 2019 – iTeos Therapeutics SA, a privately-held biotechnology company developing novel cancer immunotherapies, announced today the first cohort of patients has been dosed in its Phase 1/1b study with EOS100850, the Company’s investigational A2A receptor antagonist and lead program candidate.“I am tremendously excited to announce that patient dosing in our innovative, adaptive Phase 1/1b trial is now underway with EOS100850, our unique and specific A2A receptor antagonist. We believe we have a potential best-in-class compound, which was carefully designed with differentiating features to maximize the therapeutic window,” said Michel Detheux, Ph.D., Co-Founder, President and Chief Executive Officer of iTeos… read the entire news item (from GlobeNewswire)
Featured recent scientific publication on Adenosine Receptors:
Adenosine receptor agonist NECA increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation Conventional methods for therapeutic blood-brain barrier (BBB) disruption facilitate drug delivery but are cumbersome to perform. A previous study demonstrated that adenosine receptor (AR) stimulation by 5′-N-ethylcarboxamide adenosine (NECA) increased the extravasation of intravascular tracers into the brain and proposed that AR agonism may be an effective method for therapeutic BBB disruption. We attempted to confirm the extravasation of tracers into the brain and also investigated tracer extravasation into peripheral organs and tracer retention in the blood. We found that NECA not only increased the extravasation of intravascular fluorescein and low molecular weight dextran into the brain of mice but also increased the concentrations of these tracers in the blood. In fact, the brain:blood ratio-normalized BBB permeability for either tracer is actually decreased by NECA administration. Elevated blood urea nitrogen levels in mice following NECA treatment suggested that renal function impairment was a probable cause of tracer retention. Therefore, NECA has almost no effect on the extravasation of intravascular Evans blue dye (EBD), an albumin-binding tracer with little renal clearance. Rather than inducing BBB disruption, our study demonstrated that NECA increased tracer extravasation into the brain by increasing the concentration gradient of the tracer across the BBB… read the entire scientific publication (from Scientific Reports)
Trending tweet on #adenosinereceptors:
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Background knowledge on Adenosine Receptors:
Adenosine Receptors Adenosine is a purine nucleoside that serves as a link between energy metabolism and cell signaling. Adenosine is a physiologic regulator of all cell types that binds to G protein coupled receptors (GPCRs) that exist as four subtypes (A1, A2A, A2B, and A3). The receptor-mediated actions of adenosine have been extensively studied in the central nervous system, cardiac muscle, blood vessels, gastrointestinal tract, kidneys, lung, liver, immune system, and other tissues. In light of the clear therapeutic potential of selective adenosine receptor subtypeselective agonists or antagonists, new therapeutic candidates are being intensely pursued by the pharmaceutical industry. Naturally occurring xanthines are nonselective antagonists of adenosine receptors. One such compound, caffeine, is the most widely used psychotropic drug in the world. Adenosine, FORMATION: Adenosine is a purine nucleoside that is formed within cells from the breakdown of adenosine monophosphate (AMP), which, in turn, is formed from adenosine triphosphate (ATP) and adenosine diphosphate (ADP) in the course of utilizing energy for cellular functions. Adenine nucleotides released from nerves, mast cells, platelets, endothelial cells, and dying cells also can be dephosphorylated in the extracellular space by ectonucleotidases. Increased energy utilization or hypoxia enhances the cellular formation of AMP, which is dephosphorylated by a 50-nucleotidase in the ratelimiting step for adenosine production. The signaling molecule cyclic AMP (cAMP) can also be a source of AMP for adenosine production. Under resting conditions, a sizable fraction of adenosine is formed by the hydrolysis of S-adenosyl-homocysteine. LOCATION: Adenosine is produced in either the intracellular or extracellular spaces and can be transported across cell membranes in either direction by a family of nucleoside transporters that allow for equilibration of adenosine concentrations by facilitated diffusion or sodium-dependent active transport. REGULATION OF PRODUCTION: Production of adenosine is increased during periods of high metabolic activity or ischemia, when there is increased cellular demand for ATP or decreased delivery of oxygen. Adenosine also is derived from adenine nucleotides released from nerves, platelets, mast cells, or other cells. In the brain, adenosine release has been observed experimentally following various manipulations (e.g., hypoxia, ischemia, hypoglycemia, seizures, electrical stimulation, prolonged wakefulness, and application of free radicals). Changes in extracellular levels of adenosine of up to 100-fold have been observed following oxidative or ischemic stress… read more (from Encyclopedia of Biological Chemistry, 1st Edition)
Keywords: Adenosine Receptors, #adenosinereceptors, S-adenosyl-homocysteine, ectonucleotidases, adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), caffeine, naturally occurring xanthines, G protein coupled receptors (GPCRs), 5′-N-ethylcarboxamide adenosine (NECA), blood-brain barrier (BBB), EOS100850, Adenosine A2A Antagonist, iTeos Therapeutics SA.
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