REFERENCES
1. Siegel RL, Wagle NS, Cercek A, Smith RA, Jemal A. Colorectal cancer statistics, 2023. CA Cancer J Clin. 2023;73:233-54.
2. Yu GH, Li SF, Wei R, Jiang Z. Diabetes and colorectal cancer risk: clinical and therapeutic implications. J Diabetes Res. 2022;2022:1747326.
3. Poomakkoth N, Issa A, Abdulrahman N, Abdelaziz SG, Mraiche F. p90 ribosomal S6 kinase: a potential therapeutic target in lung cancer. J Transl Med. 2016;14:14.
4. Carriere A, Ray H, Blenis J, Roux PP. The RSK factors of activating the Ras/MAPK signaling cascade. Front Biosci. 2008;13:4258-75.
5. Jones SW, Erikson E, Blenis J, Maller JL, Erikson RL. A Xenopus ribosomal protein S6 kinase has two apparent kinase domains that are each similar to distinct protein kinases. Proc Natl Acad Sci USA. 1988;85:3377-81.
6. Houles T, Roux PP. Defining the role of the RSK isoforms in cancer. Semin Cancer Biol. 2018;48:53-61.
7. Erikson E, Maller JL. A protein kinase from Xenopus eggs specific for ribosomal protein S6. Proc Natl Acad Sci USA. 1985;82:742-6.
8. Alcorta DA, Crews CM, Sweet LJ, Bankston L, Jones SW, Erikson RL. Sequence and expression of chicken and mouse rsk: homologs of Xenopus laevis ribosomal S6 kinase. Mol Cell Biol. 1989;9:3850-9.
9. Moller DE, Xia CH, Tang W, Zhu AX, Jakubowski M. Human rsk isoforms: cloning and characterization of tissue-specific expression. Am J Physiol. 1994;266:C351-9.
10. Yntema HG, van den Helm B, Kissing J, et al. A novel ribosomal S6-kinase (RSK4; RPS6KA6) is commonly deleted in patients with complex X-linked mental retardation. Genomics. 1999;62:332-43.
11. Deak M, Clifton AD, Lucocq LM, Alessi DR. Mitogen- and stress-activated protein kinase-1 (MSK1) is directly activated by MAPK and SAPK2/p38, and may mediate activation of CREB. EMBO J. 1998;17:4426-41.
12. Smith JA, Poteet-Smith CE, Xu Y, Errington TM, Hecht SM, Lannigan DA. 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.
13. Thakur A, Sun Y, Bollig A, et al. Anti-invasive and antimetastatic activities of ribosomal protein S6 kinase 4 in breast cancer cells. Clin Cancer Res. 2008;14:4427-36.
14. Abdulrahman N, Jaballah M, Poomakkoth N, et al. Inhibition of p90 ribosomal S6 kinase attenuates cell migration and proliferation of the human lung adenocarcinoma through phospho-GSK-3β and osteopontin. Mol Cell Biochem. 2016;418:21-9.
15. Cai J, Ma H, Huang F, et al. Low expression of RSK4 predicts poor prognosis in patients with colorectal cancer. Int J Clin Exp Pathol. 2014;7:4959-70.
16. López-Vicente L, Armengol G, Pons B, et al. Regulation of replicative and stress-induced senescence by RSK4, which is down-regulated in human tumors. Clin Cancer Res. 2009;15:4546-53.
17. Kang S, Elf S, Lythgoe K, et al. p90 ribosomal S6 kinase 2 promotes invasion and metastasis of human head and neck squamous cell carcinoma cells. J Clin Invest. 2010;120:1165-77.
18. Bignone PA, Lee KY, Liu Y, et al. RPS6KA2, a putative tumour suppressor gene at 6q27 in sporadic epithelial ovarian cancer. Oncogene. 2007;26:683-700.
19. Romeo Y, Zhang X, Roux PP. Regulation and function of the RSK family of protein kinases. Biochem J. 2012;441:553-69.
20. Watanabe D, Nogami A, Okada K, Akiyama H, Umezawa Y, Miura O. FLT3-ITD activates RSK1 to enhance proliferation and survival of AML cells by activating mTORC1 and eIF4B cooperatively with PIM or PI3K and by inhibiting bad and BIM. Cancers. 2019;11:1827.
21. Jin G, Yan M, Liu K, et al. Discovery of a novel dual-target inhibitor against RSK1 and MSK2 to suppress growth of human colon cancer. Oncogene. 2020;39:6733-46.
23. Torchiaro E, Lorenzato A, Olivero M, et al. Peritoneal and hematogenous metastases of ovarian cancer cells are both controlled by the p90RSK through a self-reinforcing cell autonomous mechanism. Oncotarget. 2016;7:712-28.
24. M Hajj GN, da Silva FF, de Bellis B, et al. Aberrant expression of RSK1 characterizes high-grade gliomas with immune infiltration. Mol Oncol. 2020;14:159-79.
25. Zhao H, Martin TA, Davies EL, et al. The Clinical implications of RSK1-3 in human breast cancer. Anticancer Res 2016;36:1267-74. Avaliable from: https://ar.iiarjournals.org/content/36/3/1267 [Last accessed on 26 Jan].
26. Li LY, Chen XS, Wang KS, et al. RSK2 protects human breast cancer cells under endoplasmic reticulum stress through activating AMPKα2-mediated autophagy. Oncogene. 2020;39:6704-18.
27. Lee CJ, Lee MH, Yoo SM, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015;15:576.
28. Katsuragawa-Taminishi Y, Mizutani S, Kawaji-Kanayama Y, et al. Triple targeting of RSK, AKT, and S6K as pivotal downstream effectors of PDPK1 by TAS0612 in B-cell lymphomas. Cancer Sci. 2023;114:4691-705.
29. van Jaarsveld MT, Blijdorp IC, Boersma AW, et al. The kinase RSK2 modulates the sensitivity of ovarian cancer cells to cisplatin. Eur J Cancer. 2013;49:345-51.
30. Yao K, Peng C, Zhang Y, et al. RSK2 phosphorylates T-bet to attenuate colon cancer metastasis and growth. Proc Natl Acad Sci USA. 2017;114:12791-6.
31. Kumari A, Gesumaria L, Liu YJ, et al. mTOR inhibition overcomes RSK3-mediated resistance to BET inhibitors in small cell lung cancer. JCI Insight. 2023;8:e156657.
32. Lin H, Morin PJ. A novel homozygous deletion at chromosomal band 6q27 in an ovarian cancer cell line delineates the position of a putative tumor suppressor gene. Cancer Lett. 2001;173:63-70.
33. Fan L, Li P, Yin Z, et al. Ribosomal s6 protein kinase 4: a prognostic factor for renal cell carcinoma. Br J Cancer. 2013;109:1137-46.
34. Chen L, Xu T, Jia Q, Wang X, Li M, Liang G. RSK4: a new prognostic factor in glioma. Pathol Res Pract. 2020;216:153020.
35. Pang F, Zhang L, Li M, et al. Ribosomal S6 protein kinase 4 promotes resistance to EZH2 inhibitors in glioblastoma. Cancer Gene Ther. 2023;30:1636-48.
36. Jiang Y, Ye X, Ji Y, et al. Aberrant expression of RSK4 in breast cancer and its role in the regulation of tumorigenicity. Int J Mol Med. 2017;40:883-90.
37. Li A, Liu D, Liu Y, Zhou Y, Du Z, Song J. A pilot study of RSK4 expression in patients with human non-small cell lung carcinoma. Ann Clin Lab Sci. 2018;48:484-9.
38. Ye Q, Wang X, Jin M, et al. Effect of RSK4 on biological characteristics of colorectal cancer. World J Surg Oncol. 2018;16:240.
39. Rafiee M, Keramati MR, Ayatollahi H, et al. Down-regulation of ribosomal S6 kinase RPS6KA6 in acute myeloid leukemia patients. Cell J. 2016;18:159-64.
40. Li MY, Fan LN, Han DH, et al. Ribosomal S6 protein kinase 4 promotes radioresistance in esophageal squamous cell carcinoma. J Clin Invest. 2020;130:4301-19.
41. Arechavaleta-Velasco F, Zeferino-Toquero M, Estrada-Moscoso I, et al. Ribosomal S6 kinase 4 (RSK4) expression in ovarian tumors and its regulation by antineoplastic drugs in ovarian cancer cell lines. Med Oncol. 2016;33:11.
42. Jiang X, Du W, Yang C, et al. TBX21 attenuates colorectal cancer progression via an ARHGAP29/RSK/GSK3β dependent manner. Cell Oncol. 2023;46:1269-83.
43. Yang Q, Feng M, Ma X, Li H, Xie W. Gene expression profile comparison between colorectal cancer and adjacent normal tissues. Oncol Lett. 2017;14:6071-8.
44. Lara R, Seckl MJ, Pardo OE. The p90 RSK family members: common functions and isoform specificity. Cancer Res. 2013;73:5301-8.
45. Davies AH, Reipas K, Hu K, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015;6:20570-7.
46. Zeniou M, Ding T, Trivier E, Hanauer A. Expression analysis of RSK gene family members: the RSK2 gene, mutated in Coffin-Lowry syndrome, is prominently expressed in brain structures essential for cognitive function and learning. Hum Mol Genet. 2002;11:2929-40.
47. Dümmler BA, Hauge C, Silber J, et al. Functional characterization of human RSK4, a new 90-kDa ribosomal S6 kinase, reveals constitutive activation in most cell types. J Biol Chem. 2005;280:13304-14.
48. Anjum R, Blenis J. The RSK family of kinases: emerging roles in cellular signalling. Nat Rev Mol Cell Biol. 2008;9:747-58.
49. Smith JA, Poteet-Smith CE, Malarkey K, Sturgill TW. Identification of an extracellular signal-regulated kinase (ERK) docking site in ribosomal S6 kinase, a sequence critical for activation by ERK in vivo. J Biol Chem. 1999;274:2893-8.
50. MacKenzie SJ, Baillie GS, McPhee I, Bolger GB, Houslay MD. ERK2 mitogen-activated protein kinase binding, phosphorylation, and regulation of the PDE4D cAMP-specific phosphodiesterases. The involvement of COOH-terminal docking sites and NH2-terminal UCR regions. J Biol Chem. 2000;275:16609-17.
51. Roux PP, Richards SA, Blenis J. Phosphorylation of p90 ribosomal S6 kinase (RSK) regulates extracellular signal-regulated kinase docking and RSK activity. Mol Cell Biol. 2003;23:4796-804.
52. Dimitri CA, Dowdle W, MacKeigan JP, Blenis J, Murphy LO. Spatially separate docking sites on ERK2 regulate distinct signaling events in vivo. Curr Biol. 2005;15:1319-24.
53. Dalby KN, Morrice N, Caudwell FB, Avruch J, Cohen P. Identification of regulatory phosphorylation sites in mitogen-activated protein kinase (MAPK)-activated protein kinase-1a/p90rsk that are inducible by MAPK. J Biol Chem. 1998;273:1496-505.
54. Bjørbaek C, Zhao Y, Moller DE. Divergent functional roles for p90rsk kinase domains. J Biol Chem. 1995;270:18848-52.
55. Vik TA, Ryder JW. Identification of serine 380 as the major site of autophosphorylation of Xenopus pp90rsk. Biochem Biophys Res Commun. 1997;235:398-402.
56. Ghoda L, Lin X, Greene WC. The 90-kDa ribosomal S6 kinase (pp90rsk) phosphorylates the N-terminal regulatory domain of IkappaBalpha and stimulates its degradation in vitro. J Biol Chem. 1997;272:21281-8.
57. Xu S, Bayat H, Hou X, Jiang B. Ribosomal S6 kinase-1 modulates interleukin-1beta-induced persistent activation of NF-kappaB through phosphorylation of IkappaBbeta. Am J Physiol Cell Physiol. 2006;291:C1336-45.
58. David JP, Mehic D, Bakiri L, et al. Essential role of RSK2 in c-Fos-dependent osteosarcoma development. J Clin Invest. 2005;115:664-72.
59. Rolfe M, McLeod LE, Pratt PF, Proud CG. Activation of protein synthesis in cardiomyocytes by the hypertrophic agent phenylephrine requires the activation of ERK and involves phosphorylation of tuberous sclerosis complex 2 (TSC2). Biochem J. 2005;388:973-84.
60. Hsiao KM, Chou SY, Shih SJ, Ferrell JE Jr. Evidence that inactive p42 mitogen-activated protein kinase and inactive rsk exist as a heterodimer in vivo. Proc Natl Acad Sci USA. 1994;91:5480-4.
61. Zhao Y, Bjorbaek C, Moller DE. Regulation and interaction of pp90(rsk) isoforms with mitogen-activated protein kinases. J Biol Chem. 1996;271:29773-9.
62. Calvo N, Carriere P, Martin MJ, Gentili C. RSK activation via ERK modulates human colon cancer cells response to PTHrP. J Mol Endocrinol. 2017;59:13-27.
63. Clark DE, Errington TM, Smith JA, Frierson HF Jr, Weber MJ, Lannigan DA. The serine/threonine protein kinase, p90 ribosomal S6 kinase, is an important regulator of prostate cancer cell proliferation. Cancer Res. 2005;65:3108-16.
64. Méant A, Gao B, Lavoie G, et al. Proteomic analysis reveals a role for RSK in p120-catenin phosphorylation and melanoma cell-cell adhesion. Mol Cell Proteomics. 2020;19:50-64.
65. Zhao Y, Bjørbaek C, Weremowicz S, Morton CC, Moller DE. RSK3 encodes a novel pp90rsk isoform with a unique N-terminal sequence: growth factor-stimulated kinase function and nuclear translocation. Mol Cell Biol. 1995;15:4353-63.
66. Peng C, Zhu F, Wen W, et al. Tumor necrosis factor receptor-associated factor family protein 2 is a key mediator of the epidermal growth factor-induced ribosomal S6 kinase 2/cAMP-responsive element-binding protein/Fos protein signaling pathway. J Biol Chem. 2012;287:25881-92.
67. López-Vicente L, Pons B, Coch L, et al. RSK4 inhibition results in bypass of stress-induced and oncogene-induced senescence. Carcinogenesis. 2011;32:470-6.
68. Boussemart L, Malka-Mahieu H, Girault I, et al. eIF4F is a nexus of resistance to anti-BRAF and anti-MEK cancer therapies. Nature. 2014;513:105-9.
69. Lito P, Rosen N, Solit DB. Tumor adaptation and resistance to RAF inhibitors. Nat Med. 2013;19:1401-9.
70. Roth AD, Tejpar S, Delorenzi M, et al. Prognostic role of KRAS and BRAF in stage II and III resected colon cancer: results of the translational study on the PETACC-3, EORTC 40993, SAKK 60-00 trial. J Clin Oncol. 2010;28:466-74.
71. Barras D, Missiaglia E, Wirapati P, et al. BRAF V600E mutant colorectal cancer subtypes based on gene expression. Clin Cancer Res. 2017;23:104-15.
72. Boussios S, Ozturk MA, Moschetta M, et al. The developing story of predictive biomarkers in colorectal cancer. J Pers Med. 2019;9:12.
73. Sueda T, Sakai D, Kawamoto K, et al. BRAF V600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells. Sci Rep. 2016;6:18949.
74. Morris EJ, Jha S, Restaino CR, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013;3:742-50.
75. Sun Y, Tang L, Wu C, Wang J, Wang C. RSK inhibitors as potential anticancer agents: discovery, optimization, and challenges. Eur J Med Chem. 2023;251:115229.
76. Hilinski MK, Mrozowski RM, Clark DE, Lannigan DA. Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability. Bioorg Med Chem Lett. 2012;22:3244-7.
77. 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.
78. 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.
79. Aronchik I, Appleton BA, Basham SE, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014;12:803-12.
80. Jain R, Mathur M, Lan J, et al. Discovery of potent and selective RSK inhibitors as biological probes. J Med Chem. 2015;58:6766-83.
81. 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.
82. Boyer SJ, Burke J, Guo X, et al. Indole RSK inhibitors. Part 1: discovery and initial SAR. Bioorg Med Chem Lett. 2012;22:733-7.
83. Cohen MS, Zhang C, Shokat KM, Taunton J. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science. 2005;308:1318-21.
84. Cohen MS, Hadjivassiliou H, Taunton J. A clickable inhibitor reveals context-dependent autoactivation of p90 RSK. Nat Chem Biol. 2007;3:156-60.
85. Bain J, Plater L, Elliott M, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007;408:297-315.
86. 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.
87. 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.
88. Li M, Li Y, Ludwik KA, Sandusky ZM, Lannigan DA, O'Doherty GA. Stereoselective synthesis and evaluation of C6″-substituted 5a-carbasugar analogues of SL0101 as inhibitors of RSK1/2. Org Lett. 2017;19:2410-3.
89. 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.
90. Abdulrahman N, Siveen KS, Joseph JM, et al. Inhibition of p90 ribosomal S6 kinase potentiates cisplatin activity in A549 human lung adenocarcinoma cells. J Pharm Pharmacol. 2020;72:1536-45.
91. Zhang S, Liu J, Lu ZY, et al. Combination of RSK inhibitor LJH-685 and FLT3 inhibitor FF-10101 promoted apoptosis and proliferation inhibition of AML cell lines. Cell Oncol. 2022;45:1005-18.
92. Shi X, O'Neill MM, MacDonnell S, Brookes PS, Yan C, Berk BC. The RSK inhibitor BIX02565 limits cardiac ischemia/reperfusion injury. J Cardiovasc Pharmacol Ther. 2016;21:177-86.
93. Chen W, Zheng R, Baade PD, et al. Cancer statistics in China, 2015. CA Cancer J Clin. 2016;66:115-32.
94. Osseis M, Nehmeh WA, Rassy N, et al. Surgery for T4 colorectal cancer in older patients: determinants of outcomes. J Pers Med. 2022;12:1534.
95. Luchini C, Bibeau F, Ligtenberg MJL, et al. ESMO recommendations on microsatellite instability testing for immunotherapy in cancer, and its relationship with PD-1/PD-L1 expression and tumour mutational burden: a systematic review-based approach. Ann Oncol. 2019;30:1232-43.
96. Adeleke S, Haslam A, Choy A, et al. Microsatellite instability testing in colorectal patients with Lynch syndrome: lessons learned from a case report and how to avoid such pitfalls. Per Med. 2022;19:277-86.
97. Grothey A, Sugrue MM, Purdie DM, et al. Bevacizumab beyond first progression is associated with prolonged overall survival in metastatic colorectal cancer: results from a large observational cohort study (BRiTE). J Clin Oncol. 2008;26:5326-34.
98. Cunningham D, Humblet Y, Siena S, et al. Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N Engl J Med. 2004;351:337-45.
99. Tol J, Koopman M, Cats A, et al. Chemotherapy, bevacizumab, and cetuximab in metastatic colorectal cancer. N Engl J Med. 2009;360:563-72.