- Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5- carboxylic acid and structural development to increase potency
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We have reported that retinoid X receptor (RXR) partial agonist 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5- carboxylic acid (CBt-PMN, 4a) shows a significant antidiabetes effect in the KK-Ay type 2 diabetes model
- Ohsawa, Fuminori,Yamada, Shoya,Yakushiji, Nobumasa,Shinozaki, Ryosuke,Nakayama, Mariko,Kawata, Kohei,Hagaya, Manabu,Kobayashi, Toshiki,Kohara, Kazutaka,Furusawa, Yuuki,Fujiwara, Chisa,Ohta, Yui,Makishima, Makoto,Naitou, Hirotaka,Tai, Akihiro,Yoshikawa, Yutaka,Yasui, Hiroyuki,Kakuta, Hiroki
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p. 1865 - 1877
(2013/05/09)
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- RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists
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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.
- 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
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supporting information; experimental part
p. 427 - 432
(2012/06/30)
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