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Correlation study between A(3) adenosine receptor binding affinity and anti-renal interstitial fibrosis activity of truncated adenosine derivatives
- Title
- Correlation study between A(3) adenosine receptor binding affinity and anti-renal interstitial fibrosis activity of truncated adenosine derivatives
- Authors
- Yu, Jinha; Kim, Gyudong; Jarhad, Dnyandev B.; Lee, Hyuk Woo; Lee, Jiyoun; Park, Chong Woo; Ha, Hunjoo; Jeong, Lak Shin
- Ewha Authors
- 하헌주
- SCOPUS Author ID
- 하헌주
- Issue Date
- 2019
- Journal Title
- ARCHIVES OF PHARMACAL RESEARCH
- ISSN
- 0253-6269
1976-3786
- Citation
- ARCHIVES OF PHARMACAL RESEARCH vol. 42, no. 9, pp. 773 - 779
- Keywords
- A(3) adenosine receptor; Antagonist; Binding affinity; Truncated adenosine; Renal fibrosis
- Publisher
- PHARMACEUTICAL SOC KOREA
- Indexed
- SCIE; SCOPUS; KCI
- Document Type
- Article
- Abstract
- 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.
- DOI
- 10.1007/s12272-018-1079-2
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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