PMID- 22242853
OWN - NLM
STAT- MEDLINE
DCOM- 20120925
LR  - 20190907
IS  - 1873-4294 (Electronic)
IS  - 1568-0266 (Linking)
VI  - 12
IP  - 6
DP  - 2012
TI  - Retinoid receptors and therapeutic applications of RAR/RXR modulators.
PG  - 505-27
AB  - Retinoic acid receptors (RARs) are ligand-controlled transcription factors that 
      function as heterodimers with retinoid X receptors (RXRs) to regulate cell 
      growth, differentiation, survival and death. Due to their regulatory potential, 
      these nuclear receptors (NRs) are major drug targets for a variety of 
      pathologies, including cancer and metabolic diseases. A large amount of RAR- and 
      RXR-selective ligands, ranging from (partial) agonists to antagonists and inverse 
      agonists, have been designed and the corresponding structural and functional 
      analyses have provided deep insight into the molecular basis of ligand action. 
      Ligands regulate, via allosteric conformational changes, the ability of these NRs 
      to interact with different sets of coregulators, which in turn recruit 
      enzymatically active complexes/machineries. Here, we describe strategies in the 
      design of selective RXR and RAR modulators and review the structural mechanisms 
      by which the diverse pharmacological classes of compounds modulate receptor 
      functions. Finally, we discuss the perspectives for retinoid- and rexinoid-based 
      therapies.
FAU - le Maire, Albane
AU  - le Maire A
AD  - Institut National de la Sante et de la Recherche Medicale, U1054, Montpellier, 
      France.
FAU - Alvarez, Susana
AU  - Alvarez S
FAU - Shankaranarayanan, Pattabhiraman
AU  - Shankaranarayanan P
FAU - Lera, Angel R de
AU  - Lera AR
FAU - Bourguet, William
AU  - Bourguet W
FAU - Gronemeyer, Hinrich
AU  - Gronemeyer H
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - United Arab Emirates
TA  - Curr Top Med Chem
JT  - Current topics in medicinal chemistry
JID - 101119673
RN  - 0 (Ligands)
RN  - 0 (Receptors, Retinoic Acid)
RN  - 0 (Retinoid X Receptors)
SB  - IM
MH  - Animals
MH  - Disease
MH  - Drug Design
MH  - Humans
MH  - Ligands
MH  - Models, Molecular
MH  - Receptors, Retinoic Acid/*agonists/*antagonists & inhibitors/metabolism
MH  - Retinoid X Receptors/*agonists/*antagonists & inhibitors/metabolism
EDAT- 2012/01/17 06:00
MHDA- 2012/09/26 06:00
CRDT- 2012/01/17 06:00
PHST- 2011/11/11 00:00 [received]
PHST- 2011/12/02 00:00 [accepted]
PHST- 2012/01/17 06:00 [entrez]
PHST- 2012/01/17 06:00 [pubmed]
PHST- 2012/09/26 06:00 [medline]
AID - CTMC-EPUB-20120113-003 [pii]
AID - 10.2174/156802612799436687 [doi]
PST - ppublish
SO  - Curr Top Med Chem. 2012;12(6):505-27. doi: 10.2174/156802612799436687.