RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists.
RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists.
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DOI：
10.1021/ml300055n
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发表时间：
2012-04
影响因子：
4.2
通讯作者：
H. Kakuta;Nobumasa Yakushiji;Ryosuke Shinozaki;Fuminori Ohsawa;S. Yamada;Yui Ohta;Kohei Kawata;Mariko Nakayama;Manabu Hagaya;Chisa Fujiwara;M. Makishima;S. Uno;A. Tai;Ami Maehara;Masaru Nakayama;T. Oohashi;H. Yasui;Y. Yoshikawa
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文献类型：
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作者：
H. Kakuta;Nobumasa Yakushiji;Ryosuke Shinozaki;Fuminori Ohsawa;S. Yamada;Yui Ohta;Kohei Kawata;Mariko Nakayama;Manabu Hagaya;Chisa Fujiwara;M. Makishima;S. Uno;A. Tai;Ami Maehara;Masaru Nakayama;T. Oohashi;H. Yasui;Y. Yoshikawa
在啮齿类动物中治疗胰岛素抵抗和2型糖尿病，目前已知的类维生素A X受体（RXR）激动剂诱导显著的副作用。在这里，我们介绍了一种新的RXR部分激动剂CBt-PMN（11b），它显示出有效的降糖作用，改善胰岛素分泌和葡萄糖耐量，而没有RXR完全激动剂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的抗2型糖尿病候选药物。
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.