論文

査読有り 筆頭著者 責任著者
2012年

Feasibility of structural modification of retinoid X receptor agonists to separate blood glucose-lowering action from adverse effects: studies in KKA(y) type 2 diabetes model mice

Biological & pharmaceutical bulletin
  • Hiroki Kakuta, Fuminori Ohsawa, Shoya Yamada, Makoto Makishima, Akihiro Tai, Hiroyuki Yasui, Yutaka Yoshikawa

35
4
開始ページ
629
終了ページ
633
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1248/bpb.35.629
出版者・発行元
PHARMACEUTICAL SOC JAPAN

Retinoid X receptor (RXR) agonists are reported to exhibit blood glucose-lowering action owing to peroxisome proliferator-activated receptor (PPAR)/RXR or liver X receptor (LXR)/RXR activation, but may also cause adverse effects such as blood triglyceride elevation. In order to examine the feasibility of separating the glucose-lowering action from the adverse effects, we examined the effects of RXR agonists (NEt-TMN), NEt-3IB, and NEt-3IP, which have different heterodimer-activating patterns, in KKA(y) type 2 diabetes model mice. We found that NEt-3IB induced lower degrees of hepatomegaly and blood triglyceride (TG) elevation than the other RXR agonists, even though all of them showed similar blood glucose-lowering action on repeated administration. These findings indicate that structural modification of RXR agonists is a potentially effective strategy to reduce adverse effects while retaining desired activities.

リンク情報
DOI
https://doi.org/10.1248/bpb.35.629
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/22466572
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000302200900028&DestApp=WOS_CPL
ID情報
  • DOI : 10.1248/bpb.35.629
  • ISSN : 0918-6158
  • ORCIDのPut Code : 51294777
  • PubMed ID : 22466572
  • Web of Science ID : WOS:000302200900028

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