1 Department of Ophthalmology, Duke University School of Medicine , Durham, North Carolina.
J Ocul Pharmacol Ther. 2014 Mar-Apr;30(2-3):181-90. doi: 10.1089/jop.2013.0194. Epub 2013 Nov 27.
Homeostasis of aqueous humor (AH) outflow and intraocular pressure (IOP) is essential for normal vision. Impaired AH outflow through the trabecular meshwork (TM) and a resultant elevation in IOP are common changes in primary open-angle glaucoma (POAG), which is the most prevalent form of glaucoma. Although elevated IOP has been recognized as a definitive risk factor for POAG and lowering elevated IOP remains a mainstay for glaucoma treatment, little is known about the molecular mechanisms, especially external cues and intracellular pathways, involved in the regulation of AH outflow in both normal and glaucomatous eyes. In addition, despite the recognition that increased resistance to AH outflow via the conventional pathway consisting of TM and Schlemm's canal is the main cause for elevated IOP, there are no clinically approved drugs that target the conventional pathway to lower IOP in glaucoma patients. The aim of this article is to briefly review published work on the importance of bioactive lysophospholipids (eg, lysophosphatidic acid and sphingosine-1-phosphate), their receptors, metabolism, signaling, and role in the regulation of AH outflow via the TM and IOP, and to discuss pharmacological targeting of key proteins in the lysophospholipid signaling pathways to lower IOP in glaucoma patients.
房水流出和眼内压 (IOP) 的动态平衡对正常视力至关重要。原发性开角型青光眼 (POAG) 中常见的变化是房水通过小梁网 (TM) 的流出受阻,导致 IOP 升高,这是最常见的青光眼形式。虽然升高的 IOP 已被认为是 POAG 的明确危险因素,降低升高的 IOP 仍然是青光眼治疗的主要方法,但对于正常和青光眼眼中调节房水流出的分子机制,特别是外部线索和细胞内途径,知之甚少。此外,尽管人们认识到通过由 TM 和施莱姆氏管组成的传统途径增加房水流出阻力是导致 IOP 升高的主要原因,但目前尚无针对传统途径的临床批准药物可降低青光眼患者的 IOP。本文的目的是简要回顾已发表的关于生物活性溶血磷脂 (例如溶血磷脂酸和鞘氨醇-1-磷酸) 及其受体、代谢、信号转导以及它们在通过 TM 和 IOP 调节房水流出和 IOP 中的作用的重要性的研究工作,并讨论在青光眼患者中降低 IOP 的溶血磷脂信号通路关键蛋白的药理学靶向作用。