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

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 γ-lactone, respectively. These nucleosides were evaluated for their anti-fibrotic renoprotective activity in TGF-β1-treated murine proxima...

Full description

Saved in:
Bibliographic Details
Published in:Archives of pharmacal research 2019, 42(9), , pp.773-779
Main Authors: Yu, Jinha, Kim, Gyudong, Jarhad, Dnyandev B., Lee, Hyuk Woo, Lee, Jiyoun, Park, Chong Woo, Ha, Hunjoo, Jeong, Lak Shin
Format: Article
Language:English
Subjects:
Medicine
Pharmacology/Toxicology
Pharmacy
Research Article
약학
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 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 A 3 AR were proportional to their inhibitory activities against TGF-β1-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.
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-018-1079-2