|
KMID : 0043320190420090773
|
|
Archives of Pharmacal Research
2019 Volume.42 No. 9 p.773 ~ p.779
|
|
|
Correlation study between A3 adenosine receptor binding affinity and anti-renal interstitial fibrosis activity of truncated adenosine derivatives
|
|
Yu Jin-Ha
Kim Gyu-Dong
Jarhad Dnyandev B.
Lee Hyuk-Woo
Lee Ji-Youn
Park Chong-Woo
Ha Hun-Joo
Jeong Lak-Shin
|
|
|
Abstract
|
|
|
|
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.
|
|
|
KEYWORD
|
|
|
A3 adenosine receptor, Antagonist, Binding affinity, Truncated adenosine, Renal fibrosis
|
|
|
FullTexts / Linksout information
|
|
|
|
|
Listed journal information
|
|
  
|