Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation

Cancer Research

Volumn 65, Issue 3, 2005, Pages 1027-1034

  Smith, Jeffrey A ^a,c   Poteet Smith, Celeste E ^a   Xu, Yaming ^b   Errington, Timothy M ^a   Hecht, Sidney M ^b   Lannigan, Deborah A ^a,b  

^a UNIVERSITY OF VIRGINIA   (United States)

^b UNIVERSITY OF VIRGINIA   (United States)

^c VETERANS AFFAIRS MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ENZYME INHIBITOR; HERBACEOUS AGENT; P90 RIBOSOMAL S6 KINASE; PHOSPHOTRANSFERASE; SL 0101; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ARTICLE; BREAST CANCER; CELL CYCLE G1 PHASE; CELL PROLIFERATION; CELL TRANSFORMATION; CONTROLLED STUDY; GENE OVEREXPRESSION; HUMAN; HUMAN CELL; HUMAN TISSUE; MOLECULAR DYNAMICS; PRIORITY JOURNAL;

AMINO ACID SEQUENCE; BENZOPYRANS; BREAST NEOPLASMS; CELL GROWTH PROCESSES; CELL LINE, TUMOR; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; MOLECULAR SEQUENCE DATA; MONOSACCHARIDES; PHOSPHORYLATION; PLANT EXTRACTS; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RIBOSOMAL PROTEIN S6 KINASES, 90-KDA; SUBSTRATE SPECIFICITY;

EID: 13444270324     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (26)

1. Jones SW, Erikson E, Blenis J, Maller JL, Erikson RL. A Xenopus ribosomal S6 kinase has two apparent kinase domains that are each similar to distinct protein kinases. Proc Natl Acad Sci U S A 1988;85:3377-81.
2. 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.
3. Bjorbaek C, Zhao Y, Moller DE. Divergent functional roles for p90rsk kinase domains. J Biol Chem 1995;270:18848-52.
4. Fisher TL, Blenis J. Evidence for two catalytically active kinase domains in pp90rsk. Mol Cell Biol 1996;16:1212-9.
5. Jensen CJ, Buch MB, Krag TO, Hemmings BA, Gammeltoft S, Frodin M. 90-kDa ribosomal S6 kinase is phosphorylated and activated by 3-phosphoinositide- dependent protein kinase-1. J Biol Chem 1999;274:27168-76.
6. Poteet-Smith CE, Smith JA, Lannigan DA, Freed TA, Sturgill TW. Generation of constitutively active p90 ribosomal S6 kinase in vivo. Implications for the mitogen-activated protein kinase-activated protein kinase family. J Biol Chem 1999;274:22135-8.
7. 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.
8. Gavin AC, Nebreda AR. A MAP kinase docking site is required for phosphorylation and activation of p90(rsk)/MAPKAP kinase-1. Curr Biol 1999;9:281-4.
9. Leighton IA, Dalby KN, Caudwell FB, Cohen PT, Cohen P. Comparison of the specificities of p70 S6 kinase and MAPKAP kinase-1 identifies a relatively specific substrate for p70 S6 kinase the N-terminal kinase domain of MAPKAP kinase-1 is essential for peptide phosphorylation. FEBS Lett 1995;375:289-93.
10. De Cesare D, Jacquot S, Hanauer A, Sassone-Corsi P. Rsk-2 activity is necessary for epidermal growth factor-induced phosphorylation of CREB protein and transcription of c-fos gene. Proc Natl Acad Sci U S A 1998;95:12202-7.
11. Ghoda L, Lin X, Greene WC. The 90-kDa ribosomal S6 kinase (pp90rsk) phosphorylates the N-terminal regulatory domain of IκBα and stimulates its degradation in vitro. J Biol Chem 1997;272:21281-8.
12. Joel PB, Traish AM, Lannigan DA. Estradiol-induced phosphorylation of serine 118 in the estrogen receptor is independent of p42/p44 mitogen-activated protein kinase. J Biol Chem 1998;273:13317-23.
13. Schouten GJ, Vertegaal AC, Whiteside ST, et al. IκBα is a target for the mitogen-activated 90 kDa ribosomal S6 kinase. EMBO J 1997;16:3133-44.
14. Xing J, Ginty DD, Greenberg ME. Coupling of the RAS-MAPK pathway to gene activation by RSK2, a growth factor-regulated CREB kinase. Science 1996;273:959-63.
15. Sutherland C, Leighton IA, Cohen P. Inactivation of glycogen synthase kinase-3β by phosphorylation: new kinase connections in insulin and growth-factor signalling. Biochem J 1993;296:15-9.
16. MSchwab MS, Roberts BT, Gross SD, et al. Bub1 is activated by the protein kinase p90(Rsk) during Xenopus oocyte maturation. Curr Biol 2001;11:141-50.
17. Palmer P, Gavin AC, Nebreda AR. A link between MAP kinase and p34(cdc2)/cyclin B during oocyte maturation: p90(rsk) phosphorylates and inactivates the p34(cdc2) inhibitory kinase Myt1. EMBO J 1998;17:5037-47.
18. Hemmer W, McGlone M, Taylor SS. Recombinant strategies for rapid purification of catalytic subunits of cAMP-dependent protein kinase. Anal Biochem 1997;245:115-22.
19. Zhang J, Chung TDY, Oldenburg KR. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73.
20. Matthes HWD, Luu B, Ourisson G. Cytotoxic components of Zingiber zerumbet, Curcuma zedoaria and C. domestica. Phytochemisty 1980;19:2643-50.
21. Sebolt-Leopold JS. Development of anticancer drugs targeting the MAP kinase pathway. Oncogene 2000;19:6594-5.
22. Lobenhofer EK, Huper G, Iglehart JD, Marks JR. Inhibition of mitogen-activated protein kinase and phosphatidylinositol 3-kinase activity in MCF-7 cells prevents estrogen-induced mitogenesis. Cell Growth 2000;11:99-110.
23. Pages G, Lenormand P, L'Allemain G, Chambard JC, Meloche S, Pouyssegur J. Mitogen-activated protein kinases p42mapk and p44mapk are required for fibroblast proliferation. Proc Natl Acad Sci U S A 1993;90:8319-23.
24. Mills GB, Lu Y, Kohn EC. Linking molecular therapeutics to molecular diagnostics: inhibition of the FRAP/RAFT/TOR component of the P13K pathway preferentially blocks PTEN mutant cells in vitro and in vivo. Proc Natl Acad Sci U S A 2001;98:10031-3.
25. Neshat MS, Mellinghoff IK, Tran C, et al. Enhanced sensitivity of PTEN-deficient tumors to inhibition of FRAP/mTOR. Proc Natl Acad Sci U S A 2001;98:10314-9.
26. Tukey JW. Explanatory data analysis. Reading (MA): Addison-Wesley: 1977.