(-)-Epicatechin Is a Biased Ligand of Apelin Receptor

Andrés Portilla-Martínez, Miguel Ángel Ortiz-Flores, Eduardo Meaney, Francisco Villarreal, Nayelli Nájera, Guillermo Ceballos

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

(-)-Epicatechin (EC) is part of a large family of biomolecules called flavonoids and is widely distributed in the plant kingdom. Several studies have shown the beneficial effects of EC consumption. Many of these reported effects are exerted by activating the signaling pathways associated with the activation of two specific receptors: the G protein-coupled estrogen receptor (GPER), a transmembrane receptor, and the pregnane X receptor (PXR), which is a nuclear receptor. However, the effects of EC are so diverse that these two receptors cannot describe the complete phenomenon. The apelin receptor or APLNR is classified within the G protein-coupled receptor (GPCR) family, and is capable of activating the G protein canonical pathways and the β-arrestin transducer, which participates in the phenomenon of receptor desensitization and internalization. β-arrestin gained interest in selective pharmacology and mediators of the so-called “biased agonism”. With molecular dynamics (MD) and in vitro assays, we demonstrate how EC can recruit the β-arrestin in the active conformation of the APLN receptor acting as a biased agonist.

Original languageEnglish
Article number8962
JournalInternational Journal of Molecular Sciences
Volume23
Issue number16
DOIs
StatePublished - Aug 2022

Keywords

  • (-)-epicatechin
  • APLNR
  • bias ligand
  • molecular dynamics
  • β-arrestin

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