肝再生磷酸酶2(phosphatase of regenerating liver 2,PRL2)属于肝再生磷酸酶家族,在人体各个组织器官中广泛表达.PRL2异常高表达与肿瘤的发生发展和临床预后密切相关,是多种癌症的潜在治疗靶点.研究表明PRL2通过两种机制发挥促癌作用:一是依赖假磷酸酶活性,主要与镁离子转运体CNNM3结合;二是凭借磷酸酶活性,使底物分子PTEN等去磷酸化.因此,阻断PRL2与CNNM3结合或抑制PRL2磷酸酶活性有望成为新的抗癌策略.现综述了 PRL2与不同癌症的联系、其促癌分子机制和抑制剂的最新研究进展.
The oncogenic mechanism of phosphatase of regenerating liver 2 and the research progress of its inhibitors
The phosphatase of regenerating liver 2(PRL2),a member of the phosphatases of regenerating liver,exhibits widespread expression throughout various tissues and organs in the human body.Elevated expression of PRL2 is closely associated with the initiation,progression,and clinical outcomes of tumors,rendering it a prospective therapeutic target across various malignancies.Studies indicate that PRL2 functions in cancer progression through two mechanisms:firstly,it leverages pseudophosphatase activity,which mainly interacts with the magnesium ion transporter CNNM3;the second is to utilize phosphatase activity to dephosphorylate substrate molecules such as PTEN.Consequently,strategies aimed at disrupting the interaction between PRL2 and CNNM3 or inhibting the phosphatase activity of PRL2 represent novel avenues for anticancer intervention.This review comprehensively outlines the associations between PRL2 with diverse cancers,elucidating the molecular mechanisms underlying its oncogenic properties and the latest advancements of its inhibitors.
phosphatase of regenerating liver 2cancercyclin-M3phosphatase and tensin homologinhibitor