REV-ERB and ROR nuclear receptors as drug targets

Area of Science:

• Endocrinology and Molecular Biology

Background:

• Nuclear receptors REV-ERB (REV-ERBα/β) and RORs (RORα/β/γ) are crucial regulators of metabolism, development, immunity, and circadian rhythms.
• These receptors were initially termed 'orphan' due to the lack of identified endogenous ligands.

Purpose of the Study:

• To review the latest advancements in the pharmacology of ROR and REV-ERB nuclear receptors.
• To highlight the therapeutic potential of targeting these receptors for various diseases.

Main Methods:

• Literature review of recent developments in ROR and REV-ERB research.
• Analysis of studies on endogenous and synthetic ligand characterization.
• Evaluation of pharmacological data and therapeutic implications.

Main Results:

• Endogenous ligands for RORs and REV-ERBs have been identified, validating them as druggable targets.
• Development of synthetic ligands has accelerated, showing therapeutic potential.
• ROR and REV-ERB targeting is being explored for diseases like diabetes, atherosclerosis, autoimmunity, and cancer.

Conclusions:

• ROR and REV-ERB nuclear receptors are validated as druggable targets.
• Pharmacological targeting of RORs and REV-ERBs offers a promising therapeutic strategy for multiple disorders.
• Further research into ROR and REV-ERB ligands could lead to novel treatments.