Correlation study between A3 adenosine receptor binding affinity and anti-renal interstitial fibrosis activity of truncated adenosine derivatives

被引：0
|
作者：
Jinha Yu
Gyudong Kim
Dnyandev B. Jarhad
Hyuk Woo Lee
Jiyoun Lee
Chong Woo Park
Hunjoo Ha
Lak Shin Jeong
机构：
[1] Seoul National University,Research Institute of Pharmaceutical Sciences, College of Pharmacy
[2] Future Medicine Co.,College of Pharmacy
[3] Ltd.,undefined
[4] Ewha Womans University,undefined
来源：
Archives of Pharmacal Research | 2019年 / 42卷
关键词：
A; adenosine receptor; Antagonist; Binding affinity; Truncated adenosine; Renal fibrosis;
D O I：
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中图分类号：
学科分类号：
摘要：
Truncated 4′-thionucleosides 1–4 and 4′-oxonucleosides 5–8 as potent and selective A3AR antagonists were synthesized from d-mannose and d-erythronic acid γ-lactone, respectively. These nucleosides were evaluated for their anti-fibrotic renoprotective activity in TGF-β1-treated murine proximal tubular (mProx) cells. Their antagonistic activities for A3AR were proportional to their inhibitory activities against TGF-β1-induced collagen I upregulation in mProx cells. This result suggests that the binding affinity of A3AR antagonists is closely correlated with their anti-fibrotic activity. Thus, A3AR antagonists might be novel therapeutic candidates for treating chronic kidney disease.
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页码：773 / 779
页数：6
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