ArticleBiochemistry2012
Insights into the inhibition of the p90 ribosomal S6 kinase (RSK) by the flavonol glycoside SL0101 from the 1.5 Å crystal structure of the N-terminal domain of RSK2 with bound inhibitor.
Article in Biochemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 44 citations in OpenAlex.
- Carbamate-Bearing Carbohydrates: Natural Occurrence, Pharmacological Relevance, and Chemical Synthesis.ACS omega · 2026Review
- A patent perspective of RSK inhibitors to treat cancer (2020-present).Expert opinion on therapeutic patents · 2026Review
- 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
- Mechanism and cellular actions of the potent AMPK inhibitor BAY-3827.Science advances · 2025Article
- Designing a novel drug-drug conjugate as a prodrug for breast cancer therapy: in silico insights.Molecular diversity · 2025Article
- Classifying protein kinase conformations with machine learning.Protein science : a publication of the Protein Society · 2024Article
- An Assessment of Dispersion-Corrected DFT Methods for Modeling Nonbonded Interactions in Protein Kinase Inhibitor Complexes.Molecules (Basel, Switzerland) · 2024Article
- Comparison of Conformational Analyses of Naturally Occurring Flavonoid-Journal of chemical information and modeling · 2023Article
- Therapeutic targeting of p90 ribosomal S6 kinase.Frontiers in cell and developmental biology · 2023Review
- Identifying requirements for RSK2 specific inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- 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
- Molecular Docking Compounds of Cinnamaldehyde Derivatives as Anticancer Agents.Asian Pacific journal of cancer prevention : APJCP · 2021Article
- Synthesis and Biological Evaluation of 4'-Substituted Kaempfer-3-ols.The Journal of organic chemistry · 2020Article
- The affinity of RSK for cylitol analogues of SL0101 is critically dependent on the B-ring C-4'-hydroxy.Chemical communications (Cambridge, England) · 2020Article
- Regioselective Synthesis of aOrganic letters · 2020Article
- Article
- Development of a RSK Inhibitor as a Novel Therapy for Triple-Negative Breast Cancer.Molecular cancer therapeutics · 2016Article
- Article
- Bacterial Expression, Purification and In Vitro Phosphorylation of Full-Length Ribosomal S6 Kinase 2 (RSK2).PloS one · 2016Article
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
The p90 ribosomal S6 family of kinases (RSK) are potential drug targets, due to their involvement in cancer and other pathologies. There are currently only two known selective inhibitors of RSK, but the basis for selectivity is not known. One of these inhibitors is a naturally occurring kaempferol-α-L-diacetylrhamnoside, SL0101. Here, we report the crystal structure of the complex of the N-terminal kinase domain of the RSK2 isoform with SL0101 at 1.5 Å resolution. The refined atomic model reveals unprecedented structural reorganization of the protein moiety, as compared to the nucleotide-bound form. The entire N-lobe, the hinge region, and the αD-helix undergo dramatic conformational changes resulting in a rearrangement of the nucleotide binding site with concomitant formation of a highly hydrophobic pocket spatially suited to accommodate SL0101. These unexpected results will be invaluable in further optimization of the SL0101 scaffold as a promising lead for a novel class of kinase inhibitors.
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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.