Inflammation secondary to tissue injuries serves as a double-edged sword that determines the prognosis of tissue repair. As one of the most important enzymes controlling the inflammation process by producing leukotrienes, 5-lipoxygenase (5-LOX, also called 5-LO) has been one of the therapeutic targets in regulating inflammation for a long time. Although a large number of 5-LOX inhibitors have been explored, only a few of them can be applied clinically. Surprisingly, phosphorylation of 5-LOX reveals great significance in regulating the subcellular localization of 5-LOX, which has proven to be an important mechanism underlying the enzymatic activities of 5-LOX. There are at least three phosphorylation sites in 5-LOX jointly to determine the final inflammatory outcomes, and adjustment of phosphorylation of 5-LOX at different phosphorylation sites brings hope to provide an unrecognized means to regulate inflammation. The present review intends to shed more lights into the set-point-like mechanisms of phosphorylation of 5-LOX and its possible clinical application by summarizing the biological properties of 5-LOX, the relationship of 5-LOX with neurodegenerative diseases and brain injuries, the phosphorylation of 5-LOX at different sites, the regulatory effects and mechanisms of phosphorylated 5-LOX upon inflammation, as well as the potential anti-inflammatory application through balancing the phosphorylation-depended set-point.

继发于组织损伤的炎症是一把双刃剑，它决定了组织修复的预后。作为通过产生白三烯来控制炎症过程的最重要的酶之一，5-脂氧合酶（5-LOX，也称为5-LO）长期以来一直是调节炎症的治疗靶标之一。尽管已经研究了大量的5-LOX抑制剂，但是只有少数几种可以在临床上应用。出人意料的是，5-LOX的磷酸化在调节5-LOX的亚细胞定位中显示出重要意义，已被证明是5-LOX酶促活性的重要机制。5-LOX中至少有三个磷酸化位点共同决定最终的炎症结果，以及在不同磷酸化位点调节5-LOX的磷酸化带来了希望，以提供一种无法识别的调节炎症的手段。本综述旨在通过总结5-LOX的生物学特性，5-LOX与神经退行性疾病和脑损伤的关系，为5-LOX磷酸化的设定点样机制及其可能的临床应用提供更多的启示。 5-LOX在不同位点的磷酸化，磷酸化5-LOX对炎症的调节作用和机制，以及通过平衡依赖于磷酸化的设定点的潜在抗炎应用。