Liver X receptors conserve the therapeutic target potential for the treatment of rheumatoid arthritis

Pharmacol Res. 2021 Aug:170:105747. doi: 10.1016/j.phrs.2021.105747. Epub 2021 Jun 26.

Abstract

Rheumatoid arthritis (RA) is a chronic multi-system autoimmune disease with extremely complex pathogenesis. Significantly altered lipid paradox related to the inflammatory burden is reported in RA patients, inducing 50% higher cardiovascular risks. Recent studies have also demonstrated that lipid metabolism can regulate many functions of immune cells in which metabolic pathways have altered. The nuclear liver X receptors (LXRs), including LXRα and LXRβ, play a central role in regulating lipid homeostasis and inflammatory responses. Undoubtedly, LXRs have been considered as an attractive therapeutic target for the treatment of RA. However, there are some contradictory effects of LXRs agonists observed in previous animal studies where both pro-inflammatory role and anti-inflammatory role were revealed for LXRs activation in RA. Therefore, in addition to updating the knowledge of LXRs as the prominent regulators of lipid homeostasis, the purpose of this review is to summarize the effects of LXRs agonists in RA-associated immune cells, to explore the underlying reasons for the contradictory therapeutic effects of LXRs agonists observed in RA animal models, and to discuss future strategy for the treatment of RA with LXRs modulators.

Keywords: Immune cells; LXRs agonist; Liver X receptors; Rheumatoid arthritis.

Publication types

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

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / toxicity
  • Antirheumatic Agents / pharmacology*
  • Antirheumatic Agents / toxicity
  • Arthritis, Rheumatoid / drug therapy*
  • Arthritis, Rheumatoid / immunology
  • Arthritis, Rheumatoid / metabolism
  • Disease Models, Animal
  • Humans
  • Joints / drug effects*
  • Joints / immunology
  • Joints / metabolism
  • Lipid Metabolism / drug effects
  • Liver / drug effects
  • Liver / metabolism
  • Liver X Receptors / agonists*
  • Liver X Receptors / metabolism
  • Molecular Targeted Therapy
  • Signal Transduction

Substances

  • Anti-Inflammatory Agents
  • Antirheumatic Agents
  • Liver X Receptors