Molecular Inflammation Research Center for Aging Intervention (MRCA) and College of Pharmacy, Pusan National University, Busan 609-735, Republic of Korea.
Biomol Ther (Seoul). 2013 Nov;21(6):411-22. doi: 10.4062/biomolther.2013.080.
G-protein-coupled receptors (GPCR) are the largest superfamily of receptors responsible for signaling between cells and tissues, and because they play important physiological roles in homeostasis, they are major drug targets. New technologies have been developed for the identification of new ligands, new GPCR functions, and for drug discovery purposes. In particular, intercellular lipid mediators, such as, lysophosphatidic acid and sphingosine 1-phosphate have attracted much attention for drug discovery and this has resulted in the development of fingolimod (FTY-720) and AM095. The discovery of new intercellular lipid mediators and their GPCRs are discussed from the perspective of drug development. Lipid GPCRs for lysophospholipids, including lysophosphatidylserine, lysophosphatidylinositol, lysophosphatidylcholine, free fatty acids, fatty acid derivatives, and other lipid mediators are reviewed.
G 蛋白偶联受体（GPCR）是细胞间和组织间信号传导的最大受体超家族，由于它们在体内平衡中发挥着重要的生理作用，因此它们是主要的药物靶点。新技术已被开发用于鉴定新的配体、新的 GPCR 功能和药物发现目的。特别是，细胞间脂质介质，如溶血磷脂酸和 1-磷酸鞘氨醇，由于其在药物发现方面的吸引力而受到关注，这导致了 fingolimod（FTY-720）和 AM095 的开发。从药物开发的角度讨论了新的细胞间脂质介质及其 GPCR 的发现。综述了溶血磷脂，包括溶血磷脂酰丝氨酸、溶血磷脂酰肌醇、溶血磷脂酰胆碱、游离脂肪酸、脂肪酸衍生物和其他脂质介质的 GPCR。
