Identifying requirements for RSK2 specific inhibitors

References

• Roskoski R. Jr. Targeting ERK1/2 protein-serine/threonine kinases in human cancers. Pharmacol Res 2019;142:151–68.
   PubMed Web of Science ®Google Scholar
• Theodosakis N, Micevic G, Langdon CG, et al. p90RSK blockade inhibits dual BRAF and MEK inhibitor-resistant melanoma by targeting protein synthesis. J Invest Dermatol 2017;137:2187–96.
   PubMed Web of Science ®Google Scholar
• Kosnopfel C, Sinnberg T, Sauer B, et al. Human melanoma cells resistant to MAPK inhibitors can be effectively targeted by inhibition of the p90 ribosomal S6 kinase. Oncotarget 2017;8:35761–75.
   PubMedGoogle Scholar
• Pambid MR, Berns R, Adomat HH, et al. Overcoming resistance to Sonic Hedgehog inhibition by targeting p90 ribosomal S6 kinase in pediatric medulloblastoma. Pediatr Blood Cancer 2014;61:107–15.
   PubMed Web of Science ®Google Scholar
• Serra V, Eichhorn PJ, Garcia-Garcia C, et al. RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer. J Clin Invest 2013;123(6):2551–2563.
   PubMed Web of Science ®Google Scholar
• Chatterjee S, Huang EH, Christie I, et al. Acquired resistance to the Hsp90 inhibitor, Ganetespib, in KRAS-mutant NSCLC Is mediated via reactivation of the ERK-p90RSK-mTOR signaling network. Mol Cancer Ther 2017;16:793–804.
   PubMed Web of Science ®Google Scholar
• Moyano-Galceran L, Pietila EA, Turunen SP, et al. Adaptive RSK-EphA2-GPRC5A signaling switch triggers chemotherapy resistance in ovarian cancer. EMBO Mol Med, e11177 2020;12(4):e11177.
   PubMed Web of Science ®Google Scholar
• Anjum R, Blenis J. The RSK family of kinases: emerging roles in cellular signalling. Nat Rev Mol Cell Biol 2008;9:747–58.
   PubMed Web of Science ®Google Scholar
• Smith JA, Poteet-Smith CE, Xu Y, et al. Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation. Cancer Res 2005;65:1027–34.
   PubMed Web of Science ®Google Scholar
• Bain J, Plater L, Elliott M, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J 2007;408:297–315.
   PubMed Web of Science ®Google Scholar
• Ludwik KA, Campbell JP, Li M, et al. Development of a RSK inhibitor as a novel therapy for triple-negative breast cancer. Mol Cancer Ther 2016;15:2598–608.
   PubMed Web of Science ®Google Scholar
• Cohen MS, Hadjivassiliou H, Taunton J. A clickable inhibitor reveals context-dependent autoactivation of p90 RSK. Nature Chem Biol 2007;3:156–60.
   PubMed Web of Science ®Google Scholar
• Cohen MS, Zhang C, Shokat KM, Taunton J. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 2005;308:1318–21.
   PubMed Web of Science ®Google Scholar
• Serafimova IM, Pufall MA, Krishnan S, et al. Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles. Nat Chem Biol 2012;8:471–6.
   PubMed Web of Science ®Google Scholar
• Andersen JL, Gesser B, Funder ED, et al. Dimethyl fumarate is an allosteric covalent inhibitor of the p90 ribosomal S6 kinases. Nat Commun 2018;9:4344.
   PubMed Web of Science ®Google Scholar
• Yang ZH, Wu XN, He P, et al. A Non-canonical PDK1-RSK Signal Diminishes Pro-caspase-8-Mediated Necroptosis Blockade. Mol Cell 2020;80:296–310 e296.
   PubMed Web of Science ®Google Scholar
• Sapkota GP, Kieloch A, Lizcano JM, et al. Phosphorylation of the protein kinase mutated in Peutz-Jeghers cancer syndrome, LKB1/STK11, at Ser431 by p90(RSK) and cAMP-dependent protein kinase, but not its farnesylation at Cys(433), is essential for LKB1 to suppress cell vrowth. J Biol Chem 2001;276:19469–82.
   PubMed Web of Science ®Google Scholar
• Edgar AJ, Trost M, Watts C, Zaru R. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep 2014;34:e00091.
   PubMed Web of Science ®Google Scholar
• Neise D, Sohn D, Stefanski A, et al. The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. Cell Death Dis 2013;4:e859.
   PubMed Web of Science ®Google Scholar
• Kirrane TM, Boyer SJ, Burke J, et al. Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. Bioorg Med Chem Lett 2012;22:738–42.
   PubMed Web of Science ®Google Scholar
• Fryer RM, Muthukumarana A, Chen RR, et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. J Pharmacol Exp Ther 2012;340:492–500.
   PubMed Web of Science ®Google Scholar
• Jain R, Mathur M, Lan J, et al. Discovery of potent and selective RSK inhibitors as biological probes. J Med Chem 2015;58(17):6766–6783.
   PubMed Web of Science ®Google Scholar
• Jain R, Mathur M, Lan J, et al. Design and synthesis of potent RSK inhibitors. Bioorg Med Chem Lett 2018;28:3197–201.
   PubMed Web of Science ®Google Scholar
• Ludwik KA, Lannigan DA. Ribosomal S6 kinase (RSK) modulators: a patent review. Expert Opin Ther Pat 2016;26:1061–78.
   PubMed Web of Science ®Google Scholar
• Utepbergenov D, Derewenda U, Olekhnovich N, et al. 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. Biochemistry 2012;51:6499–510.
   PubMed Web of Science ®Google Scholar
• Li M, Li Y, Ludwik KA, et al. Stereoselective synthesis and evaluation of C6″-Substituted 5a-Carbasugar analogues of SL0101 as inhibitors of RSK1/2. Org Lett 2017;19:2410–3.
   PubMed Web of Science ®Google Scholar
• Bernetti M, Cavalli A, Mollica L. Protein-ligand (un)binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling. Med Chem Comm 2017;8:534–50.
   Web of Science ®Google Scholar
• Li Y, Sandusky ZM, Vemula R, et al. Regioselective Synthesis of a C-4'' Carbamate,C-6'' n-Pr Substituted Cyclitol Analogue of SL0101. Org Lett 2020;22:1448–52.
   PubMed Web of Science ®Google Scholar
• Maloney DJ, Hecht SM. Synthesis of a potent and selective inhibitor of p90 Rsk. Org Lett 2005;7:1097–9.
   PubMed Web of Science ®Google Scholar
• Rodrigues CH, Pires DE, Ascher DB. DynaMut: predicting the impact of mutations on protein conformation, flexibility and stability. Nucleic Acids Res 2018;46:W350–W355.
   PubMed Web of Science ®Google Scholar
• Sapkota GP, Cummings L, Newell FS, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J 2007;401:29–38.
   PubMed Web of Science ®Google Scholar
• Joel PB, Smith J, Sturgill TW, et al. pp90rsk1 regulates estrogen receptor-mediated transcription through phosphorylation of Ser-167. Mol Cell Biol 1998;18:1978–84.
   PubMed Web of Science ®Google Scholar
• Smith JA, Maloney DJ, Hecht SM, Lannigan DA. Structural basis for the activity of the RSK-specific inhibitor, SL0101. Bioorg Med Chem 2007;15:5018–34.
   PubMed Web of Science ®Google Scholar
• Li M, Li Y, Mrozowski RM, et al. Synthesis and structure-activity relationship study of 5a-carbasugar analogues of SL0101. ACS Med Chem Lett 2015;6:95–9.
   PubMed Web of Science ®Google Scholar
• Ludwik KA, McDonald OG, Brenin DR, Lannigan DA. ERalpha-mediated nuclear sequestration of RSK2 is required for ER + breast cancer tumorigenesis. Cancer Res 2018;78:2014–25.
   PubMed Web of Science ®Google Scholar
• Copeland RA. Drug-target interaction kinetics: underutilized in drug optimization? Future Med Chem 2016;8:2173–5.
   PubMed Web of Science ®Google Scholar
• Copeland RA, Pompliano DL, Meek TD. Drug-target residence time and its implications for lead optimization. Nature Reviews. Drug Discovery 2006;5:730–9.
   PubMed Web of Science ®Google Scholar
• Eisinger-Mathason TS, Andrade J, Lannigan DA. RSK in tumorigenesis: connections to steroid signaling. Steroids 2010;75:191–202.
   PubMed Web of Science ®Google Scholar