Correlation study between A(3) adenosine receptor binding affinity and anti-renal interstitial fibrosis activity of truncated adenosine derivatives
- 주제(키워드) A(3) adenosine receptor , Antagonist , Binding affinity , Truncated adenosine , Renal fibrosis
- 주제(기타) Chemistry, Medicinal
- 주제(기타) Pharmacology & Pharmacy
- 등재 SCIE, SCOPUS, KCI등재
- 발행기관 PHARMACEUTICAL SOC KOREA
- 발행년도 2019
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000161410
- 본문언어 영어
- Published As http://dx.doi.org/10.1007/s12272-018-1079-2
- PubMed https://pubmed.ncbi.nlm.nih.gov/30264323
- 저작권 이화여자대학교 논문은 저작권에 의해 보호받습니다.
초록/요약
Truncated 4 '-thionucleosides 1-4 and 4 '-oxonucleosides 5-8 as potent and selective A(3)AR antagonists were synthesized from d-mannose and d-erythronic acid gamma-lactone, respectively. These nucleosides were evaluated for their anti-fibrotic renoprotective activity in TGF-beta 1-treated murine proximal tubular (mProx) cells. Their antagonistic activities for A(3)AR were proportional to their inhibitory activities against TGF-beta 1-induced collagen I upregulation in mProx cells. This result suggests that the binding affinity of A(3)AR antagonists is closely correlated with their anti-fibrotic activity. Thus, A(3)AR antagonists might be novel therapeutic candidates for treating chronic kidney disease.
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