Group II phospholipase A2 (PLA2G2)

Group II phospholipase A2 (PLA2G2) refers to a family of secreted enzymes that catalyze the hydrolysis of the sn-2 position of membrane phospholipids, preferentially releasing unsaturated fatty acids such as arachidonic acid[1][3][5]. This enzymatic activity initiates production of key lipid mediators (eicosanoids: prostaglandins, leukotrienes) that regulate inflammation, immunity, and vascular function[1][3]. Group II sPLA2s are calcium-dependent, widely expressed in various tissues, and implicated in several pathological conditions, including cardiovascular disease, inflammation, and cancer[1][3][5]. Several isoforms exist (notably IIA and IIE in humans), and they can serve both proinflammatory and host-defense roles. Despite being an attractive therapeutic target, development of selective drugs has been hampered by closely related subtypes and off-target effects, and no sPLA2-targeted treatments are currently clinically approved[5]. Elevated PLA2G2A is considered a biomarker of increased cardiovascular risk and inflammation[1][2].

Other names

Group IIA phospholipase A2Group IIE phospholipase A2Secretory phospholipase A2 (sPLA2)sPLA2-IIAsPLA2-IIEPLA2G2APLA2G2E (gene/protein names)Phosphatidylcholine 2-acylhydrolase

Inhibition of PLA2 catalytic activity, preventing release of arachidonic acid and subsequent eicosanoid production[1][5] Selective enzymatic inhibition at active site or by chelation of essential calcium ions