5-脂氧合酶及其抑制剂

5-脂氧合酶（5-lipoxygenase, 5-LOX）是生物体内一种重要的双加氧酶.5-LOX是催化花生四烯酸（arachidonic acid，AA）生成白三烯类（leukotrienes, LTs）的关键酶. LTs是重要的炎症介质，并且在许多疾病中发挥着重要作用.近年来,很多学者致力于5 LOX的研究，从而为5-LOX抑制剂的研发提供理论依据.本文对5-LOX的分子结构、细胞内定位、表达与活性调控及其抑制剂的研究进展进行综述.

5 - Lipoxygenase and its Inhibitors

The 5-lipoxygenase（5-LOX）is an important dioxygenase in organisms, which is the key enzyme catalyzing arachidonic acid into leukotrienes (LTs). LTs is a potent mediator of the inflammatory response and plays important roles in many diseases. 5-LOX has a single polypeptide chain with a molecular mass of 75-80 kD and 673 amino acid residues in animals, which has a N terminalβ barrel domain and a larger catalytic domain containing a single atom of non-heme iron. The cell-type-specific localization of 5-LOX is determined by the balance of nuclear localization signal (NLS)- and nuclear export signal (NES)-dependent mechanisms. In addition, only granulocyte, mast cells, dendritic cells and B lymphocytes can express 5-LOX. Also Ca2+, ATP, FLAP and so on are required for 5-LOX activity. In the recent years, the research of 5-LOX focused on the development of 5-LOX inhibitors.