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
Format:	Artikel
Sprache:	eng
Schlagworte:	Letter
Online-Zugang:	Volltext
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Zusammenfassung:	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.
ISSN:	1948-5875 1948-5875
DOI:	10.1021/ml300055n