ArticleProtein science : a publication of the Protein Society2007
Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors.
Article in Protein science : a publication of the Protein Society, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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23 citing papers in PubMed, 45 citations in OpenAlex.
- Structural insights and biophysical characterization of p90RSK2:ERK2 complex.The Biochemical journal · 2025Article
- RiSKs in Computational Modeling of Isoform-Selective RSK Inhibitors.Journal of chemical information and modeling · 2025Review
- Article
- RSK1 vs. RSK2 Inhibitory Activity of the Marine β-Carboline Alkaloid Manzamine A: A Biochemical, Cervical Cancer Protein Expression, and Computational Study.Marine drugs · 2021Article
- Identification of a New Mutation inBrain sciences · 2021Article
- Article
- A high definition picture of somatic mutations in chronic lymphoproliferative disorder of natural killer cells.Blood cancer journal · 2020Article
- Inhibition of p90RSK activation sensitizes triple-negative breast cancer cells to cisplatin by inhibiting proliferation, migration and EMT.BMB reports · 2019Article
- Structural Basis of Ribosomal S6 Kinase 1 (RSK1) Inhibition by S100B Protein: MODULATION OF THE EXTRACELLULAR SIGNAL-REGULATED KINASE (ERK) SIGNALING CASCADE IN A CALCIUM-DEPENDENT WAY.The Journal of biological chemistry · 2016Article
- RSK3: A regulator of pathological cardiac remodeling.IUBMB life · 2015Review
- Molecular basis for small molecule inhibition of G protein-coupled receptor kinases.ACS chemical biology · 2015Review
- Synthetic lethality screen identifies RPS6KA2 as modifier of epidermal growth factor receptor activity in pancreatic cancer.Neoplasia (New York, N.Y.) · 2013Article
- The unusual mechanism of inhibition of the p90 ribosomal S6 kinase (RSK) by flavonol rhamnosides.Biochimica et biophysica acta · 2013Review
- A Rising Cancer Prevention Target of RSK2 in Human Skin Cancer.Frontiers in oncology · 2013Article
- Article
- Localization and retention of p90 ribosomal S6 kinase 1 in the nucleus: implications for its function.Molecular biology of the cell · 2012Article
- p90 ribosomal S6 kinase 1 (RSK1) and the catalytic subunit of protein kinase A (PKA) compete for binding the pseudosubstrate region of PKAR1alpha: role in the regulation of PKA and RSK1 activities.The Journal of biological chemistry · 2010Article
- Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation.The Journal of biological chemistry · 2010Article
- RSK2 Binding Models Delineate Key Features for Activity.Journal of chemical and pharmaceutical research · 2010Article
- Structural diversity of the active N-terminal kinase domain of p90 ribosomal S6 kinase 2.PloS one · 2009Article
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The p90 ribosomal S6 kinases (RSKs) also known as MAPKAP-Ks are serine/threonine protein kinases that are activated by ERK or PDK1 and act as downstream effectors of mitogen-activated protein kinase (MAPK). RSK1, a member of the RSK family, contains two distinct kinase domains in a single polypeptide chain, the regulatory C-terminal kinase domain (CTKD) and the catalytic N-terminal kinase domain (NTKD). Autophosphorylation of the CTKD leads to activation of the NTKD that subsequently phosphorylates downstream substrates. Here we report the crystal structures of the unactivated RSK1 NTKD bound to different ligands at 2.0 A resolution. The activation loop and helix alphaC, key regulatory elements of kinase function, are disordered. The DFG motif of the inactive RSK1 adopts an "active-like" conformation. The beta-PO(4) group in the AMP-PCP complex adopts a unique conformation that may contribute to inactivity of the enzyme. Structures of RSK1 ligand complexes offer insights into the design of novel anticancer agents and into the regulation of the catalytic activity of RSKs.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.