Retinoid X Receptor Ligands with Anti-Type 2 Diabetic Activity

Author(s): Ken-ichi Morishita , Hiroki Kakuta .

Journal Name: Current Topics in Medicinal Chemistry

Volume 17 , Issue 6 , 2017

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Graphical Abstract:


Peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-dependent transcription factor that plays an important role in regulating glucose metabolism. Agonists of PPARγ, such as thiazolidinediones, have anti-hyperglycemic activity, and are therefore used to treat type 2 diabetes. However, the functional activity of PPARγ is manifested by heterodimers of PPARγ with retinoid X receptors (RXRs). Since RXR/PPARγ heterodimers can be activated not only by PPARγ agonists, but also by RXR agonists, RXR agonists are also attractive candidates for treatment of type 2 diabetes. However, RXR full agonists have side effects, such as triglyceride elevation and hypothyroidism. Therefore, RXR partial agonists have been developed as new anti-type 2 diabetes agent candidates with reduced side effects. In addition, RXR antagonists also show therapeutic potency in type 2 diabetes patients. Here, we review RXR full agonists, RXR antagonists, and RXR modulators (partial agonists) with reported anti-diabetic effects, and we discuss their potential suitability as anti-diabetic agents.

Keywords: Retinoid X receptors, Agonists, Antagonists, Partial-agonists, Diabetes, Glucose-lowering effects.

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Article Details

Year: 2017
Page: [696 - 707]
Pages: 12
DOI: 10.2174/1568026616666160617085545
Price: $58

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