A potent LPA receptor agonist
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1-Oleoyl lysophosphatidic acid is a species of lysophosphatidic acid (LPA) containing oleic acid at the sn-1 position. Phosphatidic acid is produced either directly through the action of phospholipase D (PLD) or through a two step process involving liberation of diacylglycerol (DAG) by phospholipase C (PLC) followed by phosphorylation of DAG by diglycerol kinase.[1] Hydrolysis of the fatty acid at the sn-2 position by phospholipase A2 (PLA2) yields bioactive LPA. LPA binds to one of five different G protein linked receptors to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility.[2],[1] 1-Oleoyl lysophosphatidic acid is the most potent of the LPA analogs for calcium mobilization in A431 cells and for growth stimulation of a variety of cell lines.[3],[4]
1-油酰溶血磷脂酸是一种溶血磷脂酸 (LPA),在 sn-1 位置含有油酸。磷脂酸是通过磷脂酶 D (PLD) 的作用直接产生的,或者是通过磷脂酶 C (PLC) 释放二酰甘油 (DAG) 然后通过双甘油激酶对 DAG 进行磷酸化的两步过程产生的。 [1]磷脂酶 A2 (PLA2) 水解 sn-2 位的脂肪酸产生具有生物活性的 LPA。 LPA 与五种不同的 G 蛋白连接受体之一结合,介导多种生物反应,包括细胞增殖、平滑肌收缩、血小板聚集、神经突收缩和细胞运动。[2]、[1] 1-油酰溶血磷脂酸是LPA 类似物中最有效的 A431 细胞钙动员和多种细胞系的生长刺激。[3],[4]
Reference:
[1]. Moolenaar, W.H. LPA: A novel lipid mediator with diverse biological actions. Trends in Cell Biology 4, 213-219 (1994).
[2]. Noguchi, K., Ishii, S., and Shimizu, T. Identification of p2y9/GPR23 as a novel G protein-coupled receptor for lysophosphatidic acid, structurally distant from the Edg family. The Journal of Biological Chemisty 278(28), 25600-25606 (2003).
[3]. Jalink, K., Hengeveld, T., Mulder, S., et al. Lysophosphatidic acid-induced Ca2+ mobilization in human A4431 cells: Structure-activity analysis. Biochemistry Journal 307, 609-616 (1995).
[4]. van Corven, E.J., van Rijswijk, A., Jalink, K., et al. Mitogenic action of lysophosphatidic acid and phosphatidic acid on fibroblasts. Dependence on acyl-chain length and inhibition by suramin. Biochemistry Journal 281, 163-169 (1992).
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