蛋白磷酸酶 2A (PP2A) 是一种丝氨酸/苏氨酸磷酸酶，被认为是参与多种细胞过程的肿瘤抑制因子，对于维持体内细胞活力至关重要。然而，内源性PP2A抑制剂如癌性PP2A抑制剂(CIP2A)和内源性PP2A核蛋白抑制剂2(SET)会抵消PP2A的抗癌功能，促进肿瘤的发生、发展和肿瘤耐药性。但令人惊讶的是，与传统认知相反，用外源小分子化合物抑制抑癌基因PP2A可以增强癌症治疗的功效并实现卓越的肿瘤抑制作用。此外，外源性 PP2A 抑制剂使癌症对治疗重新敏感，并为耐药肿瘤提供新的治疗策略，值得进一步研究。© 2024 Wiley periodicals LLC。

The protein phosphatase 2A (PP2A), a serine/threonine phosphatase, is recognized as a tumor suppressor involved in diverse cellular processes and essential for maintaining cell viability in vivo. However, endogenous inhibitors of PP2A such as cancerous inhibitor of PP2A (CIP2A) and endogenous nuclear protein inhibitor 2 of PP2A (SET) counteract the anticancer function of PP2A, promoting tumorigenesis, development, and drug resistance in tumors. Surprisingly though, contrary to conventional understanding, inhibition of the tumor suppressor gene PP2A with exogenous small molecule compounds can enhance the efficacy of cancer treatment and achieve superior tumor inhibition. Moreover, exogenous PP2A inhibitors resensitize cancers to treatment and provide novel therapeutic strategies for drug-resistant tumors, which warrant further investigation.© 2024 Wiley Periodicals LLC.