Yokomizo Takehiko
Department of Medical Biochemistry, Graduate School of Medical Sciences, Kyushu University, Higashi-ku, Fukuoka, Japan.
Adv Enzyme Regul. 2011;51(1):59-64. doi: 10.1016/j.advenzreg.2010.08.002. Epub 2010 Oct 28.
Mammals have at least two receptors for LTB4; high-affinity BLT1 and low-affinity BLT2, both of which are GPCRs. 12-HHT serves as a more potent and abundant ligand for BLT2 than LTB4. BLT1 is expressed in a variety of inflammatory and immune cells including granulocytes, eosinophils, macrophages, differentiated Th1, Th2 and Th17 cells, effecter CD8+ T cells, dendritic cells and osteoclasts. BLT1 antagonists will be beneficial for the treatment of various diseases such as bronchial asthma, multiple sclerosis, contact dermatitis, and postmenopausal osteoporosis. BLT2 plays different roles from BLT1, and one important role of BLT2 is the maintenance of mucosal integrity in the colon.
哺乳动物至少有两种白三烯B4受体;高亲和力的BLT1和低亲和力的BLT2,二者均为G蛋白偶联受体。与白三烯B4相比,12-羟基-5,8,10,14-二十碳四烯酸(12-HHT)是一种对BLT2更有效且更丰富的配体。BLT1在多种炎性和免疫细胞中表达,包括粒细胞、嗜酸性粒细胞、巨噬细胞、分化的Th1、Th2和Th17细胞、效应性CD8+T细胞、树突状细胞和破骨细胞。BLT1拮抗剂将有利于治疗各种疾病,如支气管哮喘、多发性硬化症、接触性皮炎和绝经后骨质疏松症。BLT2发挥着与BLT1不同的作用,BLT2的一个重要作用是维持结肠黏膜的完整性。