Natural ligands of RXR receptors

Patricia García; Paula Lorenzo; Angel R de Lera

doi:10.1016/bs.mie.2020.02.006

Natural ligands of RXR receptors

Methods Enzymol. 2020:637:209-234. doi: 10.1016/bs.mie.2020.02.006. Epub 2020 Mar 19.

Authors

Patricia García¹, Paula Lorenzo¹, Angel R de Lera²

Affiliations

¹ Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain.
² Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain. Electronic address: qolera@uvigo.es.

PMID: 32359646
DOI: 10.1016/bs.mie.2020.02.006

Abstract

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.

Keywords: Agonists; Natural ligands; RXR; RXR heterodimers; Rexinoids; Synthesis.

Publication types

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

MeSH terms

Ligands
Retinoid X Receptors* / genetics

Substances

Ligands
Retinoid X Receptors