RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists

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 gluco...

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Veröffentlicht in:ACS medicinal chemistry letters 2012-05, Vol.3 (5), p.427-432
Hauptverfasser: 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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container_end_page 432
container_issue 5
container_start_page 427
container_title ACS medicinal chemistry letters
container_volume 3
creator 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
description 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.
doi_str_mv 10.1021/ml300055n
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title RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists
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