Irving Andrew, Abdulrazzaq Ghayth, Chan Sue L F, Penman June, Harvey Jenni, Alexander Stephen P H
The Conway Institute, School of Biomolecular and Biomedical Science, University College Dublin, Dublin, Ireland.
Life Sciences, University of Nottingham Medical School, Nottingham, United Kingdom.
Adv Pharmacol. 2017;80:223-247. doi: 10.1016/bs.apha.2017.04.004. Epub 2017 Jun 12.
Of the druggable group of G protein-coupled receptors in the human genome, a number remain which have yet to be paired with an endogenous ligand-orphan GPCRs. Among these 100 or so entities, 3 have been linked to the cannabinoid system. GPR18, GPR55, and GPR119 exhibit limited sequence homology with the established CB and CB cannabinoid receptors. However, the pharmacology of these orphan receptors displays overlap with CB and CB receptors, particularly for GPR18 and GPR55. The linking of GPR119 to the cannabinoid receptors is less convincing and emanates from structural similarities of endogenous ligands active at these GPCRs, but which do not cross-react. This review describes the evidence for describing these orphan GPCRs as cannabinoid receptor-like receptors.
在人类基因组中可成药的G蛋白偶联受体组中，仍有一些尚未与内源性配体配对——孤儿GPCR。在这100个左右的实体中，有3个与大麻素系统有关。GPR18、GPR55和GPR119与已确定的CB1和CB2大麻素受体表现出有限的序列同源性。然而，这些孤儿受体的药理学与CB1和CB2受体存在重叠，特别是对于GPR18和GPR55。GPR119与大麻素受体的联系不太令人信服，源于这些GPCR上活性内源性配体的结构相似性，但它们不会发生交叉反应。本综述描述了将这些孤儿GPCR描述为类大麻素受体的证据。
