1.Recent advances in role of RSK2 in tumorigenesis and its inhibitors
Haixiao LI ; Yuanbao AI ; Sen LIU
Chinese Journal of Pathophysiology 2025;41(4):775-782
Ribosomal S6 kinase 2(RSK2),an important member of the RSK family,is involved in cell prolifera-tion,transformation,apoptosis,and the cell cycle.It plays a pivotal role in the development and progression of various tu-mors,making it a promising target for anticancer drug development.To date,there is a notable paucity of effective inhibi-tors,with only one compound,PMD-026,having advanced to the clinical stage of testing.Earlier studies have suggested that RSK2 was regulated exclusively by MAPK,however recent research has shown that AKT1 also activates RSK2.This article provides an in-depth review of the structural and functional characteristics of the RSK2 protein,its signal transduc-tion pathways,and the relationship between RSK2 and tumor development and progression.We also reviews the status of current research and the challenges associated with developing inhibitors that target different sites of RSK2.The objective was to provide valuable insights for the advancement of RSK2 inhibitors.
2.Recent advances in role of RSK2 in tumorigenesis and its inhibitors
Haixiao LI ; Yuanbao AI ; Sen LIU
Chinese Journal of Pathophysiology 2025;41(4):775-782
Ribosomal S6 kinase 2(RSK2),an important member of the RSK family,is involved in cell prolifera-tion,transformation,apoptosis,and the cell cycle.It plays a pivotal role in the development and progression of various tu-mors,making it a promising target for anticancer drug development.To date,there is a notable paucity of effective inhibi-tors,with only one compound,PMD-026,having advanced to the clinical stage of testing.Earlier studies have suggested that RSK2 was regulated exclusively by MAPK,however recent research has shown that AKT1 also activates RSK2.This article provides an in-depth review of the structural and functional characteristics of the RSK2 protein,its signal transduc-tion pathways,and the relationship between RSK2 and tumor development and progression.We also reviews the status of current research and the challenges associated with developing inhibitors that target different sites of RSK2.The objective was to provide valuable insights for the advancement of RSK2 inhibitors.

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