RAR-related orphan receptor

The RAR-related orphan receptors (RORs) are members of the

Melatonin has been claimed to be an endogenous ligand for ROR-α while CGP 52608 has been identified as a ROR-α selective synthetic ligand.^[9]

Tissue distribution

RORα, RORβ, and RORγ are primarily expressed the following tissues:^[7]

• ROR-α – widely expressed in liver, skeletal muscle, skin, lung, adipose tissue, kidney, thymus, and brain.
• ROR-β – expression restricted to the brain and retina.
• ROR-γ – highly expressed in thymus (the thymus-specific isoform is referred to as RORγt), muscle, testis, pancreas, prostate, heart, and liver.

Function

The three forms of RORs fulfill a number of critical roles^[10] including:

• ROR-α – Involved in the maintenance of the
  BMAL1.^[5] Development of the cerebellum and lymph nodes, lipid metabolism, immune response, maintenance of bone.^[11]
• ROR-β – Circadian rhythm, bone metabolism, and retinal neurogenesis.[12]
• ROR-γ – Lymph node development and immune response, survival of T helper 17 cells.

As drug targets

A number of synthetic RORγt inverse agonists are in various stages of drug development for the treatment of

• Retinoid receptor

References