4.5 Article

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

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 3, Issue 5, Pages 427-432

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ml300055n

Keywords

Nuclear receptors; RXR; partial agonists; type 2 diabetes

Funding

  1. Ministry of Health, Labour, and Welfare of Japan [23080401]
  2. Ministry of Education, Science, Culture and Sports of Japan
  3. Takeda Science Foundation

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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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