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Biochem Pharmacol ; 210: 115488, 2023 04.
Article in English | MEDLINE | ID: mdl-36889445

ABSTRACT

The 90 kDa ribosomal S6 kinase (RSK) family of proteins is a group of highly conserved Ser/Thr kinases. They are downstream effectors of the Ras/ERK/MAPK signaling cascade. ERK1/2 activation directly results in the phosphorylation of RSKs, which further, through interaction with a variety of different downstream substrates, activate various signaling events. In this context, they have been shown to mediate diverse cellular processes like cell survival, growth, proliferation, EMT, invasion, and metastasis. Interestingly, increased expression of RSKs has also been demonstrated in various cancers, such as breast, prostate, and lung cancer. This review aims to present the most recent advances in the field of RSK signaling that have occurred, such as biological insights, function, and mechanisms associated with carcinogenesis. We additionally present and discuss the recent advances but also the limitations in the development of pharmacological inhibitors of RSKs, in the context of the use of these kinases as putative, more efficient targets for novel anticancer therapeutic approaches.


Subject(s)
Antineoplastic Agents , Carcinogenesis , Molecular Targeted Therapy , Neoplasms , Ribosomal Protein S6 Kinases, 90-kDa , Animals , Humans , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Carcinogenesis/drug effects , Enzyme Activation , Phosphorylation/drug effects , Ribosomal Protein S6 Kinases, 90-kDa/antagonists & inhibitors , Ribosomal Protein S6 Kinases, 90-kDa/metabolism , Signal Transduction/drug effects , Neoplasms/drug therapy , Neoplasms/metabolism , Neoplasms/pathology
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