PMID- 31359388
OWN - NLM
STAT- MEDLINE
DCOM- 20200330
LR  - 20200330
IS  - 1940-6029 (Electronic)
IS  - 1064-3745 (Linking)
VI  - 2019
DP  - 2019
TI  - Ligand Design for Modulation of RXR Functions.
PG  - 51-72
LID - 10.1007/978-1-4939-9585-1_4 [doi]
AB  - Retinoid X receptors (RXRs) are promiscuous partners of heterodimeric 
      associations with other members of the Nuclear Receptor (NR) superfamily. RXR 
      ligands ("rexinoids") either transcriptionally activate the "permissive" subclass 
      of heterodimers or synergize with partner ligands in the "nonpermissive" subclass 
      of heterodimers. The rationale for rexinoid design with a wide structural 
      diversity going from the structures of existing complexes with RXR determined by 
      X-Ray, to natural products and other ligands discovered by high-throughput 
      screening (HTS), mere serendipity, and rationally designed based on Molecular 
      Modeling, will be described. Included is the new generation of ligands that 
      modulate the structure of specific receptor surfaces that serve to communicate 
      with other regulators. The panel of the known RXR agonists, partial 
      (ant)agonists, and/or heterodimer-selective rexinoids require the exploration of 
      their therapeutic potential in order to overcome some of the current limitations 
      of rexinoids in therapy.
FAU - Martinez, Claudio
AU  - Martinez C
AD  - Departamento de Quimica Organica, Facultade de Quimica, CINBIO and IBIV, 
      Universidade de Vigo, Vigo, Spain.
FAU - Souto, Jose A
AU  - Souto JA
AD  - Departamento de Quimica Organica, Facultade de Quimica, CINBIO and IBIV, 
      Universidade de Vigo, Vigo, Spain.
FAU - de Lera, Angel R
AU  - de Lera AR
AD  - Departamento de Quimica Organica, Facultade de Quimica, CINBIO and IBIV, 
      Universidade de Vigo, Vigo, Spain. qolera@uvigo.es.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Methods Mol Biol
JT  - Methods in molecular biology (Clifton, N.J.)
JID - 9214969
RN  - 0 (Ligands)
RN  - 0 (Pharmaceutical Preparations)
RN  - 0 (Retinoid X Receptors)
SB  - IM
MH  - Animals
MH  - Drug Design
MH  - Humans
MH  - Ligands
MH  - Models, Molecular
MH  - Molecular Structure
MH  - Pharmaceutical Preparations/*chemistry
MH  - Protein Multimerization
MH  - Retinoid X Receptors/*chemistry/*metabolism
MH  - Structure-Activity Relationship
OTO - NOTNLM
OT  - (Virtual) ligand design
OT  - Agonists
OT  - Antagonists
OT  - Computer-assisted RXR ligand discovery
OT  - RXR
OT  - RXR heterodimers
OT  - Rexinoids
EDAT- 2019/07/31 06:00
MHDA- 2020/03/31 06:00
CRDT- 2019/07/31 06:00
PHST- 2019/07/31 06:00 [entrez]
PHST- 2019/07/31 06:00 [pubmed]
PHST- 2020/03/31 06:00 [medline]
AID - 10.1007/978-1-4939-9585-1_4 [doi]
PST - ppublish
SO  - Methods Mol Biol. 2019;2019:51-72. doi: 10.1007/978-1-4939-9585-1_4.