RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists
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- 作者：Hiroki Kakuta ; Nobumasa Yakushiji ; Ryosuke Shinozaki ; Fuminori Ohsawa ; Shoya Yamada ; Yui Ohta ; Kohei Kawata ; Mariko Nakayama ; Manabu Hagaya ; Chisa Fujiwara ; Makoto Makishima ; Shigeyuki Uno ; Akihiro Tai ; Ami Maehara ; Masaru Nakayama ; Toshitaka Oohashi ; Hiroyuki Yasui ; Yutaka Yoshikawa
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：May 10, 2012
- 年：2012
- 卷：3
- 期：5
- 页码：427-432
- 全文大小：353K
- 年卷期：v.3,no.5(May 10, 2012)
- ISSN：1948-5875
文摘
Treating insulin resistance and type 2 diabetes in rodents, currently known retinoid X receptor (RXR) agonists induce significant adverse effects. Here we introduce a novel RXR partial agonist CBt-PMN (11b), which shows a potent glucose-lowering effect and improvements of insulin secretion and glucose tolerance without the serious adverse effects caused by RXR full agonists. We suggest that RXR partial agonists may be a new class of antitype 2 diabetes drug candidates.