Department of Molecular Biology, The Scripps Research Institute, 10550 N. Torrey Pines Rd., La Jolla, CA 92037, USA.
Pharmacol Rev. 2010 Dec;62(4):579-87. doi: 10.1124/pr.110.003111.
Lysophospholipids are cell membrane-derived lipids that include both glycerophospholipids such as lysophosphatidic acid (LPA) and sphingoid lipids such as sphingosine 1-phosphate (S1P). These and related molecules can function in vertebrates as extracellular signals by binding and activating G protein-coupled receptors. There are currently five LPA receptors, along with a proposed sixth (LPA₁-LPA₆), and five S1P receptors (S1P₁-S1P₅). A remarkably diverse biology and pathophysiology has emerged since the last review, driven by cloned receptors and targeted gene deletion ("knockout") studies in mice, which implicate receptor-mediated lysophospholipid signaling in most organ systems and multiple disease processes. The entry of various lysophospholipid receptor modulatory compounds into humans through clinical trials is ongoing and may lead to new medicines that are based on this signaling system. This review incorporates IUPHAR Nomenclature Committee guidelines in updating the nomenclature for lysophospholipid receptors ( http://www.iuphar-db.org/DATABASE/FamilyMenuForward?familyId=36).
溶血磷脂是细胞膜衍生的脂质，包括甘油磷脂如溶血磷脂酸（LPA）和鞘氨醇脂质如 1-磷酸鞘氨醇（S1P）。这些和相关分子在脊椎动物中可以作为细胞外信号，通过结合和激活 G 蛋白偶联受体发挥作用。目前有五种 LPA 受体，以及一种提议的第六种（LPA₁-LPA₆），和五种 S1P 受体（S1P₁-S1P₅）。自上次综述以来，由于克隆受体和小鼠的靶向基因缺失（“敲除”）研究，出现了令人瞩目的多样性生物学和病理生理学，表明受体介导的溶血磷脂信号转导在大多数器官系统和多种疾病过程中起作用。各种溶血磷脂受体调节化合物通过临床试验进入人体正在进行中，这可能会产生基于该信号系统的新药。本综述结合了 IUPHAR 命名委员会指南，更新了溶血磷脂受体的命名（http://www.iuphar-db.org/DATABASE/FamilyMenuForward?familyId=36）。
