摘要
非受体型蛋白酪氨酸磷酸酶2 (protein tyrosine phosphatase non-receptor type 2, PTPN2)作为蛋白酪氨酸磷酸酶家族成员,通过催化去磷酸化反应,在细胞信号传递中起着重要作用。PTPN2过表达与多种癌症患者预后不良密切相关,而其缺失能有效抑制肿瘤的增长、迁移,并促进细胞凋亡。在免疫系统中,PTPN2在T细胞功能以及肿瘤微环境的调节中起着关键作用。因此,PTPN2在肿瘤发展过程和肿瘤免疫中扮演了重要角色,是一个潜在抗肿瘤新靶点。目前,有多个PTPN2抑制剂或降解剂被发现,其中两个抑制剂已进入临床I期试验阶段。该文综述了PTPN2的结构特性、在抗肿瘤免疫中的功能与应用,以及当前对其抑制剂和降解剂在肿瘤治疗中的研究进展。
Protein tyrosine phosphatase non-receptor type 2(PTPN2),a member of the protein tyrosine phosphatase family,plays an important role in cellular signaling by catalyzing dephosphorylation reactions.Overexpression of PTPN2 is closely associated with poor prognosis of patients with various cancers.And its absence can effectively inhibit tumor growth,migration,and promote apoptosis.In the immune system,PTPN2 plays a key role in the regulation of T cell function and tumor microenvironment.Therefore,PTPN2 plays an important role in tumor development and tumor immunity,and is a potential new anti-tumor target.Currently,several PTPN2 inhibitors or degraders have been identified,and two of them have entered phase I clinical trials.In this paper,we review the structural properties of PTPN2,its functions and applications in anti-tumor immunity,and the current progress of research on its inhibitors and degraders in tumor therapy.
作者
李慧芸
姜凯龙
李佳
LI Hui-Yun;JIANG Kai-Long;LI Jia(School of Pharmacy,Zunyi Medical University,Zunyi 563006,China;Zhongshan Institute for Drug Discovery,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Zhongshan 528400,China)
出处
《生命科学》
CSCD
2024年第5期637-648,共12页
Chinese Bulletin of Life Sciences
基金
广东省高水平新型研发机构(2019B090904008)
广东省高水平创新研究院(2021B0909050003)。
关键词
非受体型蛋白酪氨酸磷酸酶2
功能
抑制剂
降解剂
肿瘤免疫
non-receptor-type protein tyrosine phosphatase 2
function
inhibitor
degrader
tumor immunity