PMID- 32359646 OWN - NLM STAT- MEDLINE DCOM- 20210623 LR - 20210623 IS - 1557-7988 (Electronic) IS - 0076-6879 (Linking) VI - 637 DP - 2020 TI - Natural ligands of RXR receptors. PG - 209-234 LID - S0076-6879(20)30084-7 [pii] LID - 10.1016/bs.mie.2020.02.006 [doi] AB - 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. CI - (c) 2020 Elsevier Inc. All rights reserved. FAU - Garcia, Patricia AU - Garcia P AD - Departamento de Quimica Organica, Facultade de Quimica, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain. FAU - Lorenzo, Paula AU - Lorenzo P AD - Departamento de Quimica Organica, Facultade de Quimica, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, 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, Campus As Lagoas-Marcosende, Vigo, Spain. Electronic address: qolera@uvigo.es. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20200319 PL - United States TA - Methods Enzymol JT - Methods in enzymology JID - 0212271 RN - 0 (Ligands) RN - 0 (Retinoid X Receptors) SB - IM MH - Ligands MH - *Retinoid X Receptors/genetics OTO - NOTNLM OT - Agonists OT - Natural ligands OT - RXR OT - RXR heterodimers OT - Rexinoids OT - Synthesis EDAT- 2020/05/04 06:00 MHDA- 2021/06/24 06:00 CRDT- 2020/05/04 06:00 PHST- 2020/05/04 06:00 [entrez] PHST- 2020/05/04 06:00 [pubmed] PHST- 2021/06/24 06:00 [medline] AID - S0076-6879(20)30084-7 [pii] AID - 10.1016/bs.mie.2020.02.006 [doi] PST - ppublish SO - Methods Enzymol. 2020;637:209-234. doi: 10.1016/bs.mie.2020.02.006. Epub 2020 Mar 19.