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  • cardiac
  • The study provides the first proof for the new concept that an increased expression of the human A3 receptor in the cardiac myocyte can be an important cardioprotective therapeutic approach. (garvan.org.au)
  • Agonists
  • In this review, we showcase selected modeling-based and guided strategies that were applied to elucidate the binding of agonists to the A 3 AR and discuss the challenges associated with an accurate prediction of the receptor extracellular vestibule through homology modeling from the available X-ray templates. (mdpi.com)
  • The selective A 3 adenosine receptor agonists IB-MECA (0.05 mg/kg, 0.1 mg/kg, or 0.3 mg/kg) and MRS3558 (0.05 mg/kg or 0.1 mg/kg) were administered before reperfusion. (springer.com)
  • Thus, increasing the receptor level improves the myocyte sensitivity to the endogenous adenosine, which in turn causes all of the cardioprotective effects found for exogenously administered adenosine agonists. (garvan.org.au)
  • Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein A, a, R2, and R3 are as defined in the specification. (nih.gov)
  • extracellular
  • In mice in which extracellular adenosine production was impaired by CD73 KO, TAC caused greater hypertrophy and dysfunction and increased myocardial 3′-nitrotyrosine. (ahajournals.org)
  • Recently, we demonstrated that genetic deletion of CD73 (an ectonucleotidase that produces extracellular adenosine) exacerbated myocardial hypertrophy and heart failure resulting from left ventricular (LV) pressure overload produced by transverse aortic constriction (TAC), 1 suggesting that endogenous extracellular adenosine can protect against maladaptive hypertrophy. (ahajournals.org)
  • The A3 receptor activation also led to an increase in extracellular levels of MMP9 in the supernatants of glioblastoma cells as evaluated by ELISA and gelatine zymography assays. (unife.it)
  • This is the first example showing that it is feasible to modulate and even enhance the pharmacological profile of a ligand of a GPCR based on conjugation to a nanocarrier and the precise structure of the linking group, which was designed to interact with distal extracellular regions of the 7 transmembrane-spanning receptor. (biomedcentral.com)
  • ligands have confirmed
  • even supposing the A receptor is more and more being well-known for three its expanding variety of organic roles in the course of the physique and plenty of A receptor three ligands have confirmed precious in elucidating peripheral and valuable pathologies, many matters stay unresolved. (b-construction.ru)
  • The A 3 receptor is more and more being well-known for its organic roles through the physique, and lots of A 3 receptor ligands have confirmed important in elucidating peripheral and principal pathologies. (stainlessqa.com)
  • membrane
  • Adenosine released from cells interacts with membrane receptors (adenosine receptors, ARs). (mybiosource.com)
  • The cooperation of gB, the heterodimer gH/gL, as well as gD and the gD receptor are required in entering the plasma or endosomal membrane of host cells [5, (schwitzbiotech.com)
  • Another significant thermodynamic aspect, which characterizes the membrane receptors is the linearity of the van't Hoff plots in the temperature range usually investigated (0-35°C) indicating that the heat capacity value (DCp°) of the binding equilibrium is nearly zero, a phenomenon which is not usual in reactions involving biomacromolecules in solution (Sturtevant 1977). (stainlessqa.com)
  • exerts
  • Several studies in literature and obtained in our laboratory have shown that adenosine exerts important modulatory function in the growth of tumors, giving an essential role in this to the A3 receptor. (unife.it)
  • Human
  • The objective of the present study was to investigate whether genetic manipulation of the cardiac myocyte, achieved by gene transfer and overexpression of the human A3 receptor cDNA, renders the myocytes resistant to the deleterious effect of ischemia. (garvan.org.au)
  • During simulated ischemia, cultured myocytes with enhanced expression of the human A3 receptor and showed significantly higher ATP content, fewer cells killed, and less creatine kinase released into the medium than either control or mock-transfected myocytes. (garvan.org.au)
  • protective
  • Although we and others have demonstrated that adenosine protects against LV hypertrophy and maladaptive remodeling during pressure overload, the distinct contributions of the A 1 R and A 3 R to this protective effect are not known. (ahajournals.org)
  • cardiac function
  • 13 On the other hand, transgenic overexpression of the A 1 R 14 or A 3 R 15,16 promotes cardiac dilation and dysfunction, suggesting that these receptors may also exert adverse effects on cardiac function. (ahajournals.org)
  • regulation
  • Therefore the aim of this study was to evaluate the involvement of adenosine on the regulation of metalloproteinases and in particular of MMP9 in U87MG glioblastoma cells. (unife.it)
  • Receptors of adenosine A 2a that are localized in a relatively higher number in the striatum, show functional interaction with dopamine receptors in the regulation of synaptic conduction. (russianpatents.com)
  • pharmaceutical
  • methods of their production, new intermediate compounds of described methods of production, a pharmaceutical composition containing these compounds, and application of compounds of common formula (I) and their pharmaceutical acceptable salts as ligands of adenosine A3 receptor in treatment of different diseases. (russianpatents.com)
  • Biological
  • Although the A receptor is increasingly being recognized for 3 its increasing number of biological roles throughout the body and many A receptor 3 ligands have proven useful in elucidating peripheral and central pathologies, many issues remain unresolved. (foyles.co.uk)
  • diseases
  • The number of growing diseases and increasing concern and awareness about health are the factors contributing to the growth of Adenosine Receptor A3 industry and its allied industries. (mononews.ca)
  • Molecular
  • Detailed understanding of the physico-chemical aspects and molecular biology of the A receptor provides a solid basis for its future development as a target for 3 adenosine-based pharmacotherapies (Chapters 2 and 3). (foyles.co.uk)
  • distinctive knowing of the physico-chemical elements and molecular biology of the A receptor presents a fantastic foundation for its destiny improvement as a aim for three adenosine-based pharmacotherapies (Chapters 2 and 3). (b-construction.ru)
  • study
  • This report is a systematic research study based on the market and analyzes the competitive framework of the global Adenosine Receptor A3 industry. (mononews.ca)
  • The company profiles, trends, tactics, merger & acquisitions, business strategies, financial metrics of the major participants operating in the global Adenosine Receptor A3 market have been reviewed in this study. (mononews.ca)