RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists

Hiroki Kakuta; Nobumasa Yakushiji; Ryosuke Shinozaki; Fuminori Ohsawa; Shoya Yamada; Yui Ohta; Kohei Kawata; Mariko Nakayama; Manabu Hagaya; Chisa Fujiwara; Makoto Makishima; Shigeyuki Uno; Akihiro Tai; Ami Maehara; Masaru Nakayama; Toshitaka Oohashi; Hiroyuki Yasui; Yutaka Yoshikawa

doi:10.1021/ml300055n

RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists

Hiroki Kakuta, Nobumasa Yakushiji, Ryosuke Shinozaki, Fuminori Ohsawa, Shoya Yamada, Yui Ohta, Kohei Kawata, Mariko Nakayama, Manabu Hagaya, Chisa Fujiwara, Makoto Makishima, Shigeyuki Uno, Akihiro Tai, Ami Maehara, Masaru Nakayama, Toshitaka Oohashi, Hiroyuki Yasui, Yutaka Yoshikawa

Research output: Contribution to journal › Article › peer-review

43 Citations (Scopus)

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.

Original language	English
Pages (from-to)	427-432
Number of pages	6
Journal	ACS Medicinal Chemistry Letters
Volume	3
Issue number	5
DOIs	https://doi.org/10.1021/ml300055n
Publication status	Published - May 10 2012

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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Kakuta, H., Yakushiji, N., Shinozaki, R., Ohsawa, F., Yamada, S., Ohta, Y., Kawata, K., Nakayama, M., Hagaya, M., Fujiwara, C., Makishima, M., Uno, S., Tai, A., Maehara, A., Nakayama, M., Oohashi, T., Yasui, H., & Yoshikawa, Y. (2012). RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists. ACS Medicinal Chemistry Letters, 3(5), 427-432. https://doi.org/10.1021/ml300055n

Kakuta, H, Yakushiji, N, Shinozaki, R, Ohsawa, F, Yamada, S, Ohta, Y, Kawata, K, Nakayama, M, Hagaya, M, Fujiwara, C, Makishima, M, Uno, S, Tai, A, Maehara, A, Nakayama, M, Oohashi, T, Yasui, H & Yoshikawa, Y 2012, 'RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists', ACS Medicinal Chemistry Letters, vol. 3, no. 5, pp. 427-432. https://doi.org/10.1021/ml300055n

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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.",

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AU - Kakuta, Hiroki

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AU - Shinozaki, Ryosuke

AU - Ohsawa, Fuminori

AU - Yamada, Shoya

AU - Ohta, Yui

AU - Kawata, Kohei

AU - Nakayama, Mariko

AU - Hagaya, Manabu

AU - Fujiwara, Chisa

AU - Makishima, Makoto

AU - Uno, Shigeyuki

AU - Tai, Akihiro

AU - Maehara, Ami

AU - Nakayama, Masaru

AU - Oohashi, Toshitaka

AU - Yasui, Hiroyuki

AU - Yoshikawa, Yutaka

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RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists

Abstract

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