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

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34 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 languageEnglish
Pages (from-to)427-432
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume3
Issue number5
DOIs
Publication statusPublished - 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