S9, a novel anticancer agent, exerts its anti-proliferative activity by interfering with both PI3K-Akt-mTOR signaling and microtubule cytoskeleton

PLoS ONE

Volumn 4, Issue 3, 2009, Pages

  Zhang, Chao ^a   Yang, Na ^a   Yang, Chun Hao ^a   Ding, Hua Sheng ^a   Luo, Cheng ^a   Zhang, Yu ^a   Wu, Mao Jiang ^a   Zhang, Xiong Wen ^a   Shen, Xu ^a,b   Jiang, Hua Liang ^a,b   Meng, Ling Hua ^a   Ding, Jian ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

COLCHICINE; MAMMALIAN TARGET OF RAPAMYCIN; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE B; RAPAMYCIN; S 9; VINCRISTINE; WORTMANNIN; ANTINEOPLASTIC AGENT; DRUG DERIVATIVE; GAMMA BUTYROLACTONE; INDOLE DERIVATIVE; MTOR PROTEIN, HUMAN; MTOR PROTEIN, MOUSE; PROTEIN KINASE; TARGET OF RAPAMYCIN KINASE; TUBULIN;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; CELL CYCLE ARREST; CONTROLLED STUDY; CYTOSKELETON; DRUG DOSE COMPARISON; DRUG TARGETING; HUMAN; HUMAN CELL; LIVER CELL CARCINOMA; MICROTUBULE ASSEMBLY; RHABDOMYOSARCOMA; WEIGHT REDUCTION; ANIMAL; BIOCATALYSIS; CELL PROLIFERATION; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECT; METABOLISM; MICROTUBULE; MOUSE; NUDE MOUSE; PHOSPHORYLATION; SIGNAL TRANSDUCTION;

MUS MUSCULUS;

4-BUTYROLACTONE; ANIMALS; ANTINEOPLASTIC AGENTS; BIOCATALYSIS; CELL PROLIFERATION; COLCHICINE; CYTOSKELETON; HUMANS; INDOLES; MICE; MICE, NUDE; MICROTUBULES; MODELS, MOLECULAR; PHOSPHATIDYLINOSITOL 3-KINASES; PHOSPHORYLATION; PROTEIN KINASES; PROTO-ONCOGENE PROTEINS C-AKT; SIGNAL TRANSDUCTION; TOR SERINE-THREONINE KINASES; TUBULIN;

EID: 62849122450     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0004881     Document Type: Article

References (33)

1. Cantley LC (2002) The phosphoinositide 3-kinase pathway. Science 296: 1655-1657.
2. Jefferies HB, Fumagalli S, Dennis PB, Reinhard C, Pearson RB, et al. (1997) Rapamycin suppresses 5'TOP mRNA translation through inhibition of p70s6k. Embo J 16: 3693-3704.
3. Carracedo A, Pandolfi PP (2008) The PTEN-PI3K pathway: of feedbacks and cross-talks. Oncogene 27: 5527-5541.
4. Maira SM, Voliva C, Garcia-Echeverria C (2008) Class IA phosphatidylinositol 3-kinase: from their biologic implication in human cancers to drug discovery. Expert Opin Ther Targets 12: 223-238.
5. Atkins MB, Hidalgo M, Stadler WM, Logan TF, Dutcher JP, et al. (2004) Randomized phase II study of multiple dose levels of CCI-779, a novel mammalian target of rapamycin kinase inhibitor, in patients with advanced refractory renal cell carcinoma. J Clin Oncol 22: 909-918.
6. Boulay A, Zumstein-Mecker S, Stephan C, Beuvink I, Zilbermann F, et al. (2004) Antitumor efficacy of intermittent treatment schedules with the rapamycin derivative RAD001 correlates with prolonged inactivation of ribosomal protein S6 kinase 1 in peripheral blood mononuclear cells. Cancer Res 64: 252-261.
7. O'Reilly KE, Rojo F, She QB, Solit D, Mills GB, et al. (2006) mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res 66: 1500-1508.
8. Ding H, Zhang C, Wu X, Yang C, Zhang X, et al. (2005) Novel indole alphamethylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases. Bioorg Med Chem Lett 15: 4799-4802.
9. Casamayor A, Morrice NA, Alessi DR (1999) Phosphorylation of Ser-241 is essential for the activity of 3-phosphoinositide-dependent protein kinase-1: identification of five sites of phosphorylation in vivo. Biochem J 342(Pt 2): 287-292.
10. Scheid MP, Marignani PA, Woodgett JR (2002) Multiple phosphoinositide 3-kinase-dependent steps in activation of protein kinase B. Mol Cell Biol 22: 6247-6260.
11. Nobes CD, Hawkins P, Stephens L, Hall A (1995) Activation of the small GTP-binding proteins rho and rac by growth factor receptors. J Cell Sci 108(Pt 1): 225-233.
12. Hay N (2005) The Akt-mTOR tango and its relevance to cancer. Cancer Cell 8: 179-183.
13. Sarbassov DD, Guertin DA, Ali SM, Sabatini DM (2005) Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex. Science 307: 1098-1101.
14. Furuta T, Takemura H, Liao ZY, Aune GJ, Redon C, et al. (2003) Phosphorylation of histone H2AX and activation of Mre11, Rad50, and Nbs1 in response to replication-dependent DNA double-strand breaks induced by mammalian DNA topoisomerase I cleavage complexes. J Biol Chem 278: 20303-20312.
15. Walker EH, Pacold ME, Perisic O, Stephens L, Hawkins PT, et al. (2000) Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. Mol Cell 6: 909-919.
16. Chiu MI, Katz H, Berlin V (1994) RAPT1, a mammalian homolog of yeast Tor, interacts with the FKBP12/rapamycin complex. Proc Natl Acad Sci U S A 91: 12574-12578.
17. Yaguchi S, Fukui Y, Koshimizu I, Yoshimi H, Matsuno T, et al. (2006) Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor. J Natl Cancer Inst 98: 545-556.
18. Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, et al. (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9: 341-349.
19. Clute P, Pines J (1999) Temporal and spatial control of cyclin B1 destruction in metaphase. Nat Cell Biol 1: 82-87.
20. Zhang LH, Wu L, Raymon HK, Chen RS, Corral L, et al. (2006) The synthetic compound CC-5079 is a potent inhibitor of tubulin polymerization and tumor necrosis factor-alpha production with antitumor activity. Cancer Res 66: 951-959.
21. Jordan MA (2002) Mechanism of action of antitumor drugs that interact with microtubules and tubulin. Curr Med Chem Anticancer Agents 2: 1-17.
22. Bhattacharyya B, Wolff J (1974) Promotion of flurescence upon binding of colchicine to tubulin. Proc Natl Acad Sci U S A 71: 2627.
23. Wipf P, Halter RJ (2005) Chemistry and biology of wortmannin. Org Biomol Chem 3: 2053-2061.
24. Gastpar R, Goldbrunner M, Marko D, von Angerer E (1998) Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. J Med Chem 41: 4965-4972.
25. Opel D, Westhoff MA, Bender A, Braun V, Debatin KM, et al. (2008) Phosphatidylinositol 3-kinase inhibition broadly sensitizes glioblastoma cells to death receptor- and drug-induced apoptosis. Cancer Res 68: 6271-6280.
26. Zhang C, Yang F, Zhang XW, Wang SC, Li MH, et al. (2006) Grateloupia longifolia polysaccharide inhibits angiogenesis by downregulating tissue factor expression in HMEC-1 endothelial cells. Br J Pharmacol 148: 741-751.
27. Tong YG, Zhang XW, Geng MY, Yue JM, Xin XL, et al. (2006) Pseudolarix acid B, a new tubulin-binding agent, inhibits angiogenesis by interacting with a novel binding site on tubulin. Mol Pharmacol 69: 1226-1233.
28. Dulal Panda HPM, Leslie Wilson (1999) Rapid treadmilling of brain microtubules free of microtubule-associated proteins in vitro and its suppression by tau.
29. Huang CH, Mandelker D, Schmidt-Kittler O, Samuels Y, Velculescu VE, et al. (2007) The structure of a human p110alpha/p85alpha complex elucidates the effects of oncogenic PI3Kalpha mutations. Science 318: 1744-1748.
30. Ravelli RB, Gigant B, Curmi PA, Jourdain I, Lachkar S, et al. (2004) Insight into tubulin regulation from a complex with colchicine and a stathmin-like domain. Nature 428: 198-202.
31. Yang J, Cron P, Good VM, Thompson V, Hemmings BA, et al. (2002) Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP. Nat Struct Biol 9: 940-944.
32. Henikoff S, Henikoff JG (1992) Amino acid substitution matrices from protein blocks. Proc Natl Acad Sci U S A 89: 10915-10919.
33. Morris GM, Goodsell DS, Halliday RS, Huey R, Hart WE, et al. (1998) Automated docking using a Lamarckian genetic algorithm and an empirical binding free energy function. Journal of Computational Chemist 19: 1639-1662.