Natural ligands of RXR receptors.

Agonists Natural ligands RXR RXR heterodimers Rexinoids Synthesis

Journal

Methods in enzymology
ISSN: 1557-7988
Titre abrégé: Methods Enzymol
Pays: United States
ID NLM: 0212271

Informations de publication

Date de publication:
2020
Historique:
entrez: 4 5 2020
pubmed: 4 5 2020
medline: 24 6 2021
Statut: ppublish

Résumé

Given the role of retinoid X receptors (RXRs) as promiscuous partners of heterodimeric complexes with other members of the Nuclear Receptor (NR) superfamily, RXR ligands (rexinoids) play fundamental roles in gene transcription, since upon ligand binding either transcriptionally activate the "permissive" subclass of heterodimers or synergize with partner ligands in the "non-permissive" subclass of heterodimers. The collection of natural products thus far reported to bind RXR are described, including those discovered by high-throughput screening (HTS), mere serendipity, and a combination of those. Detailed protocols for the diastereo- and enantioselective synthesis of (R)-9-cis-13,14-dihydroretinoic acid, a putative natural RXR ligand, are provided.

Identifiants

pubmed: 32359646
pii: S0076-6879(20)30084-7
doi: 10.1016/bs.mie.2020.02.006
pii:
doi:

Substances chimiques

Ligands 0
Retinoid X Receptors 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

209-234

Informations de copyright

© 2020 Elsevier Inc. All rights reserved.

Auteurs

Patricia García (P)

Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain.

Paula Lorenzo (P)

Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain.

Angel R de Lera (AR)

Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain. Electronic address: qolera@uvigo.es.

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Classifications MeSH