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Researchers at National Institute of Diabetes, Digestive and Kidney Diseases Report Findings in Adenosine Therapy (Structure-based approaches to...

July 9, 2014



Researchers at National Institute of Diabetes, Digestive and Kidney Diseases Report Findings in Adenosine Therapy (Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates)

By a News Reporter-Staff News Editor at Biotech Week -- Researchers detail new data in Drugs and Therapies. According to news reporting originating in Bethesda, Maryland, by NewsRx editors, the research stated, "Adenosine receptor (ARs) and P2Y receptors (P2YRs) that respond to extracellular nucleosides/nucleotides are associated with new directions for therapeutics. The X-ray structures of the A2AAR complexes with agonists and antagonists are examined in relationship to the G-protein-coupled receptor (GPCR) superfamily and applied to drug discovery."

The news reporters obtained a quote from the research from the National Institute of Diabetes, Digestive and Kidney Diseases, "Much of the data on AR ligand structure from early SAR studies now are explainable from the A2AAR X-ray crystallography. The ligand-receptor interactions in related GPCR complexes can be identified by means of modeling approaches, e.g., molecular docking. Thus, molecular recognition in binding and activation processes has been studied effectively using homology modeling and applied to ligand design. Virtual screening has yielded new nonnucleoside AR antagonists, and existing ligands have been improved with knowledge of the receptor interactions. New agonists are being explored for central nervous system and peripheral therapeutics based on in vivo activity, such as chronic neuropathic pain. Ligands for receptors more distantly related to the X-ray template, i.e., P2YRs, have been introduced and are mainly used as pharmacological tools for elucidating the physiological role of extracellular nucleotides."

According to the news reporters, the research concluded: "Other ligand tools for drug discovery include fluorescent probes, radioactive probes, multivalent probes, and functionalized nanoparticles."

For more information on this research see: Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates. Journal of Medicinal Chemistry, 2013;56(10):3749-67. (American Chemical Society - www.acs.org; Journal of Medicinal Chemistry - www.pubs.acs.org/journal/jmcmar)

Our news correspondents report that additional information may be obtained by contacting K.A. Jacobson, Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States (see also Drugs and Therapies).

Keywords for this news article include: Antiarrhythmic Agents, Pharmaceuticals, Bethesda, Maryland, Adenosine, United States, Radiologic Agents, Drugs and Therapies, Radiologic Adjuncts, Cardiovascular Agents, Cardiac Stressing Agents, North and Central America.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Biotech Week


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