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Nucleoside-based adenosine A3 receptor antagonists as drug candidates

Title
Nucleoside-based adenosine A3 receptor antagonists as drug candidates
Authors
Tosh D.K.Jacobson K.A.Jeong L.S.
Ewha Authors
정낙신
Issue Date
2009
Journal Title
Drugs of the Future
ISSN
0377-8282JCR Link
Citation
vol. 34, no. 1, pp. 43 - 52
Indexed
SCIE; SCOPUS WOS scopus
Abstract
Purine nucleoside derivatives that are selective ligands for the A 3 adenosine receptor (AR) have been structurally modified such that their ability to activate the receptor is lost while retaining high binding affinity. This loss of efficacy in otherwise selectively binding nucleosides has been shown to result in antagonism of the effects of known agonists in functional assays. Modification of the ribose moiety has been the most effective strategy to accomplish this aim. Steric constraints have been introduced, as well as replacement of the various hydrogen bond-donating groups, to achieve a reduction in efficacy. High selectivity has recently been achieved for such nucleoside-based A3 AR antagonists. Thus, it is now possible to compare nucleoside-based A3 AR antagonists with well-characterized heterocyclic nonpurine antagonists as clinical candidates for the treatment of glaucoma, asthma and inflammation. Copyright © 2009 Prous Science, S.A.U. or its licensors. All rights reserved.
DOI
10.1358/dof.2009.034.01.1286494
Appears in Collections:
약학대학 > 약학과 > Journal papers
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