Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 정낙신 | - |
dc.contributor.author | 이상국 | - |
dc.date.accessioned | 2016-08-28T11:08:00Z | - |
dc.date.available | 2016-08-28T11:08:00Z | - |
dc.date.issued | 2006 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.other | OAK-3113 | - |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/219661 | - |
dc.description.abstract | We have established structure-activity relationships of novel 4′-thionucleoside analogues as the A3 adenosine receptor (AR) agonists. Binding affinity, selectivity toward other AR subtypes, and efficacy in inhibition of adenylate cyclase were studied. From this study, 2-chloro-N 6-methyl-4′-thioadenosine-5′-methyluronamide (36a) emerged as the most potent and selective agonist at the human A3 AR. We have also revealed that, similar to 4′-oxoadenosine analogues, at least one hydrogen on the 5′-uronamide moiety was necessary for high-affinity binding at the human A3 AR, presumably to allow this group to donate a H bond within the binding site. Furthermore, bulky substituents on the 5′-uronamide reduced binding affinity, but in some cases large 5′-uronamide substituents, such as substituted benzyl and 2-phenylethyl groups, maintained moderate affinity with reduced efficacy, leading to A 3 AR partial agonists or antagonists. In several cases for which the corresponding 4′-oxonucleosides have been studied, the 4′-thionucleosides showed higher binding affinity to the A3 AR. © 2006 American Chemical Society. | - |
dc.language | English | - |
dc.title | Structure-activity relationships of 2-chloro-N6-substituted- 4′-thioadenosine-5′-uronamides as highly potent and selective agonists at the human A3 adenosine receptor | - |
dc.type | Article | - |
dc.relation.issue | 1 | - |
dc.relation.volume | 49 | - |
dc.relation.index | SCI | - |
dc.relation.index | SCIE | - |
dc.relation.index | SCOPUS | - |
dc.relation.startpage | 273 | - |
dc.relation.lastpage | 281 | - |
dc.relation.journaltitle | Journal of Medicinal Chemistry | - |
dc.identifier.doi | 10.1021/jm050595e | - |
dc.identifier.wosid | WOS:000234575300028 | - |
dc.identifier.scopusid | 2-s2.0-30444439867 | - |
dc.author.google | Jeong L.S. | - |
dc.author.google | Lee H.W. | - |
dc.author.google | Jacobson K.A. | - |
dc.author.google | Kim H.O. | - |
dc.author.google | Shin D.H. | - |
dc.author.google | Lee J.A. | - |
dc.author.google | Gao Z.-G. | - |
dc.author.google | Lu C. | - |
dc.author.google | Duong H.T. | - |
dc.author.google | Gunaga P. | - |
dc.author.google | Lee S.K. | - |
dc.author.google | Jin D.Z. | - |
dc.author.google | Chun M.W. | - |
dc.author.google | Moon H.R. | - |
dc.contributor.scopusid | 정낙신(16028528200) | - |
dc.contributor.scopusid | 이상국(36067620500) | - |
dc.date.modifydate | 20211210153309 | - |