PMID- 27320332
OWN - NLM
STAT- MEDLINE
DCOM- 20170208
LR  - 20190907
IS  - 1873-4294 (Electronic)
IS  - 1568-0266 (Linking)
VI  - 17
IP  - 6
DP  - 2017
TI  - Retinoid X Receptor Ligands with Anti-Type 2 Diabetic Activity.
PG  - 696-707
AB  - Peroxisome proliferator-activated receptor gamma (PPARgamma) is a ligand-dependent 
      transcription factor that plays an important role in regulating glucose 
      metabolism. Agonists of PPARgamma, such as thiazolidinediones, have 
      anti-hyperglycemic activity, and are therefore used to treat type 2 diabetes. 
      However, the functional activity of PPARgamma is manifested by heterodimers of PPARgamma 
      with retinoid X receptors (RXRs). Since RXR/PPARgamma heterodimers can be activated 
      not only by PPARgamma 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.
FAU - Morishita, Ken-Ichi
AU  - Morishita KI
FAU - Kakuta, Hiroki
AU  - Kakuta H
AD  - Division of Pharmaceutical Sciences, Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences, 1-1-1 Tsushima-Naka, Kita-ku, 
      Okayama 700- 8530, Japan.
LA  - eng
PT  - Journal Article
PT  - Review
PL  - United Arab Emirates
TA  - Curr Top Med Chem
JT  - Current topics in medicinal chemistry
JID - 101119673
RN  - 0 (Ligands)
RN  - 0 (Retinoid X Receptors)
SB  - IM
MH  - Diabetes Mellitus, Type 2/*drug therapy
MH  - Humans
MH  - Ligands
MH  - Retinoid X Receptors/*drug effects
EDAT- 2016/06/21 06:00
MHDA- 2017/02/09 06:00
CRDT- 2016/06/21 06:00
PHST- 2015/10/14 00:00 [received]
PHST- 2016/01/11 00:00 [revised]
PHST- 2016/01/11 00:00 [accepted]
PHST- 2016/06/21 06:00 [pubmed]
PHST- 2017/02/09 06:00 [medline]
PHST- 2016/06/21 06:00 [entrez]
AID - CTMC-EPUB-76609 [pii]
AID - 10.2174/1568026616666160617085545 [doi]
PST - ppublish
SO  - Curr Top Med Chem. 2017;17(6):696-707. doi: 10.2174/1568026616666160617085545.