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 journalArticle

32 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

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Retinoid X Receptors
Therapeutic Uses
Medical problems
Type 2 Diabetes Mellitus
Insulin
Glucose
Insulin Resistance
Rodentia
1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

Cite this

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

In: ACS Medicinal Chemistry Letters, Vol. 3, No. 5, 10.05.2012, p. 427-432.

Research output: Contribution to journalArticle

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
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. / RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists. In: ACS Medicinal Chemistry Letters. 2012 ; Vol. 3, No. 5. pp. 427-432.
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