PMID- 27320331
OWN - NLM
STAT- MEDLINE
DCOM- 20170208
LR  - 20190907
IS  - 1873-4294 (Electronic)
IS  - 1568-0266 (Linking)
VI  - 17
IP  - 6
DP  - 2017
TI  - Recent Progress in the Design and Discovery of RXR Modulators Targeting Alternate 
      Binding Sites of the Receptor.
PG  - 663-675
AB  - Retinoid X receptors (RXRs) occupy a central position within the nuclear receptor 
      superfamily. They not only function as important transcriptional factors but also 
      exhibit diverse nongenomic biological activities. The pleiotropic actions of RXRs 
      under both physiological and pathophysiological conditions confer RXRs important 
      drug targets for the treatment of cancer, and metabolic and neurodegenerative 
      diseases. RXR modulators have been studied for the purpose of developing both 
      drug molecules and chemical tools for biological investigation of RXR. 
      Development of RXR modulators has focused on small molecules targeting the 
      canonical ligand-binding pocket. However, accumulating results have demonstrated 
      that there are other binding mechanisms by which small molecules interact with 
      RXR to act as RXR modulators. This review discusses the recent development in the 
      design and discovery of RXR modulators with a focus on those targeting novel 
      binding sites on RXR.
FAU - Su, Ying
AU  - Su Y
AD  - Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Road, 
      La Jolla, California 92037, United States.
FAU - Zeng, Zhiping
AU  - Zeng Z
FAU - Chen, Ziwen
AU  - Chen Z
FAU - Xu, Dan
AU  - Xu D
FAU - Zhang, Weidong
AU  - Zhang W
FAU - Zhang, Xiao-Kun
AU  - Zhang XK
AD  - School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, China.
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  - Animals
MH  - Binding Sites
MH  - *Drug Design
MH  - *Drug Discovery
MH  - Humans
MH  - Ligands
MH  - Retinoid X Receptors/*chemistry/metabolism
EDAT- 2016/06/21 06:00
MHDA- 2017/02/09 06:00
CRDT- 2016/06/21 06:00
PHST- 2015/11/13 00:00 [received]
PHST- 2015/12/16 00:00 [revised]
PHST- 2015/12/16 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-76615 [pii]
AID - 10.2174/1568026616666160617092241 [doi]
PST - ppublish
SO  - Curr Top Med Chem. 2017;17(6):663-675. doi: 10.2174/1568026616666160617092241.