GPR183 (also known as Epstein-Barr virus-induced gene 2) is an orphan G protein-coupled receptor (GPCR) that is highly expressed in spleen and is required for humoral immune responses, including B cell migration and T cell-dependent antibody production. 7α,25-dihydroxy Cholesterol (7α,25-DHC) is a potent agonist of GPR183 that induces specific activation of the receptor with an EC50 value of 50 nM (Kd = 450 pM). At concentrations below 3 μM, it does not show any appreciable binding activity when tested against eight different nuclear hormone receptors including LXR and thirty-one different G protein-coupled receptors in a panel of reporter gene assays. 7α,25-DHC can act as a potent chemokine, affecting migration of immune cells expressing GPR183 both in vitro (EC50 = 500 pM) and in vivo.[Cayman Chemical]
일반 설명
7α,25-dihydroxycholesterol (7α,25-OHC) is synthesized by the hydroxylation of cholesterol by the action of enzyme cholesterol 25-hydroxylase (CH25H) and cytochrome P450, family 7, subfamily b, polypeptide 1 (CYP7B1). The catabolic breakdown of 7α,25-OHC to bile acid precursors is catalyzed by the enzymes hydroxy-Δ-5-steroid dehydrogenase, 3β- and steroid Δ-isomerase 7 (HSD3B7).
Biochem/physiol Actions
7α,25-dihydroxycholesterol (7α,25-OHC) serves as an endogenous ligand for G-protein-coupled receptor 183 (GPR183) or Epstein-Barr virus-induced gene 2 (EBI2). It plays a key role in the migration of type 3 innate lymphoid cells (ILC3) in the small intestine and colon. 7α,25-OHC mediates immune cell migration functionality by their chemoattractant property. Inhibition of 7α,25-OHC synthesis leads to impairment in the migration of B cells.
