RXR部分激动剂CBt-PMN对2型糖尿病具有治疗作用，且无RXR完全激动剂的副作用。
RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists.
作者信息
Kakuta Hiroki, Yakushiji Nobumasa, Shinozaki Ryosuke, Ohsawa Fuminori, Yamada Shoya, Ohta Yui, Kawata Kohei, Nakayama Mariko, Hagaya Manabu, Fujiwara Chisa, Makishima Makoto, Uno Shigeyuki, Tai Akihiro, Maehara Ami, Nakayama Masaru, Oohashi Toshitaka, Yasui Hiroyuki, Yoshikawa Yutaka
机构信息
Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1 Tsushima-Naka, Okayama 700-8530, Japan.
Division of Biochemistry, Department of Biomedical Sciences, Nihon University School of Medicine , 30-1 Oyaguchi-kamicho, Itabashi-ku, Tokyo 173-8610, Japan.
出版信息
ACS Med Chem Lett. 2012 Apr 9;3(5):427-32. doi: 10.1021/ml300055n. eCollection 2012 May 10.
Abstract
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.
摘要
在啮齿动物中治疗胰岛素抵抗和2型糖尿病时，目前已知的视黄酸X受体（RXR）激动剂会引发显著的不良反应。在此，我们介绍一种新型的RXR部分激动剂CBt-PMN（11b），它具有强效的降糖作用，能改善胰岛素分泌和葡萄糖耐量，且不会产生RXR完全激动剂所引起的严重不良反应。我们认为RXR部分激动剂可能是一类新型的抗2型糖尿病候选药物。
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