PF-4708671, a specific inhibitor of p70 ribosomal S6 kinase 1, activates Nrf2 by promoting p62-dependent autophagic degradation of Keap1

Biochemical and Biophysical Research Communications

Volumn 466, Issue 3, 2015, Pages 499-504

  Park, Jeong Su ^a   Kang, Dong Hoon ^b   Lee, Da Hyun ^a   Bae, Soo Han ^a  

^a Yonsei University College of Medicine   (South Korea)

^b Ewha Womans University   (South Korea)

Author keywords

Autophagy; Kelch like ECH associated protein 1 (Keap1); Nuclear factor erythroid 2 related factor 2 (Nrf2); p62; p70 ribosomal S6 kinase 1 (S6K1); PF 4708671

Indexed keywords

CASPASE 3; KELCH LIKE ECH ASSOCIATED PROTEIN 1; PF 4708671; PROTEIN P62; PROTEIN P70; PROTEIN SERINE THREONINE KINASE INHIBITOR; S6 KINASE; TRANSCRIPTION FACTOR NRF2; UNCLASSIFIED DRUG; CYTOSKELETON PROTEIN; HEAT SHOCK PROTEIN; IMIDAZOLE DERIVATIVE; KEAP1 PROTEIN, MOUSE; MESSENGER RNA; NFE2L2 PROTEIN, MOUSE; PF-4708671; PIPERAZINE DERIVATIVE; PROTEIN KINASE INHIBITOR; REACTIVE OXYGEN METABOLITE; RPS6KA1 PROTEIN, MOUSE; SIGNAL TRANSDUCING ADAPTOR PROTEIN; SQSTM1 PROTEIN, MOUSE;

ANIMAL CELL; APOPTOSIS; ARTICLE; AUTOPHAGY; CELL DEATH; CELL PROTECTION; CELL VIABILITY; DRUG MECHANISM; EMBRYO; ENZYME PHOSPHORYLATION; FEMALE; HELA CELL LINE; HUMAN; HUMAN CELL; IMMUNOBLOTTING; MOUSE; NONHUMAN; OXIDATIVE STRESS; PRIORITY JOURNAL; PROTEIN DEGRADATION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; TRANSCRIPTION INITIATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL CULTURE; DEFICIENCY; DRUG EFFECTS; GENETICS; METABOLISM; PHYSIOLOGY; SIGNAL TRANSDUCTION;

ADAPTOR PROTEINS, SIGNAL TRANSDUCING; ANIMALS; APOPTOSIS; AUTOPHAGY; CELLS, CULTURED; CYTOSKELETAL PROTEINS; HEAT-SHOCK PROTEINS; HELA CELLS; HUMANS; IMIDAZOLES; MICE; NF-E2-RELATED FACTOR 2; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTEOLYSIS; REACTIVE OXYGEN SPECIES; RIBOSOMAL PROTEIN S6 KINASES, 90-KDA; RNA, MESSENGER; SIGNAL TRANSDUCTION;

EID: 84943363717     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2015.09.059     Document Type: Article

References (24)

1. L.R. Pearce, D. Komander, and D.R. Alessi The nuts and bolts of AGC protein kinases Nat. Rev. Mol. Cell Biol. 11 2010 9 22
2. L.R. Pearce, G.R. Alton, D.T. Richter, J.C. Kath, L. Lingardo, J. Chapman, C. Hwang, and D.R. Alessi Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1) Biochem. J. 431 2010 245 255
3. S.E. Hong, E.K. Kim, H.O. Jin, H.A. Kim, J.K. Lee, J.S. Koh, H. Seol, J.I. Kim, I.C. Park, and W.C. Noh S6K1 inhibition enhances tamoxifen-induced cell death in MCF-7 cells through translational inhibition of Mcl-1 and survivin Cell Biol. Toxicol. 29 2013 273 282
4. H.N. Choi, H.O. Jin, J.H. Kim, S.E. Hong, H.A. Kim, E.K. Kim, J.K. Lee, I.C. Park, and W.C. Noh Inhibition of S6K1 enhances glucose deprivation-induced cell death via downregulation of anti-apoptotic proteins in MCF-7 breast cancer cells Biochem. Biophys. Res. Commun. 432 2013 123 128
5. S.E. Hong, K.S. Shin, Y.H. Lee, S.K. Seo, S.M. Yun, T.B. Choe, H.A. Kim, E.K. Kim, W.C. Noh, J.I. Kim, C.S. Hwang, J.K. Lee, S.G. Hwang, H.O. Jin, and I.C. Park Inhibition of S6K1 enhances dichloroacetate-induced cell death J. Cancer Res. Clin. Oncol. 141 2015 1171 1179
6. S. Orrenius Reactive oxygen species in mitochondria-mediated cell death Drug Metab. Rev. 39 2007 443 455
7. T.W. Kensler, N. Wakabayashi, and S. Biswal Cell survival responses to environmental stresses via the Keap1-Nrf2-ARE pathway Annu. Rev. Pharmacol. Toxicol. 47 2007 89 116
8. K. Itoh, J. Mimura, and M. Yamamoto Discovery of the negative regulator of Nrf2, Keap1: a historical overview Antioxid. Redox Signal 13 2010 1665 1678
9. K. Taguchi, H. Motohashi, and M. Yamamoto Molecular mechanisms of the Keap1-Nrf2 pathway in stress response and cancer evolution Genes Cells 16 2011 123 140
10. K. Itoh, N. Wakabayashi, Y. Katoh, T. Ishii, K. Igarashi, J.D. Engel, and M. Yamamoto Keap1 represses nuclear activation of antioxidant responsive elements by Nrf2 through binding to the amino-terminal Neh2 domain Genes Dev. 13 1999 76 86
11. M. Komatsu, S. Kageyama, and Y. Ichimura p62/SQSTM1/A170: physiology and pathology Pharmacol. Res. 66 2012 457 462
12. J. Moscat, M.T. Diaz-Meco, and M.W. Wooten Signal integration and diversification through the p62 scaffold protein Trends Biochem. Sci. 32 2007 95 100
13. A. Jain, T. Lamark, E. Sjottem, K.B. Larsen, J.A. Awuh, A. Overvatn, M. McMahon, J.D. Hayes, and T. Johansen p62/SQSTM1 is a target gene for transcription factor NRF2 and creates a positive feedback loop by inducing antioxidant response element-driven gene transcription J. Biol. Chem. 285 2010 22576 22591
14. D.H. Kang, D.J. Lee, K.W. Lee, Y.S. Park, J.Y. Lee, S.H. Lee, Y.J. Koh, G.Y. Koh, C. Choi, D.Y. Yu, J. Kim, and S.W. Kang Peroxiredoxin II is an essential antioxidant enzyme that prevents the oxidative inactivation of VEGF receptor-2 in vascular endothelial cells Mol. Cell 44 2011 545 558
15. L. Wang, M. Chen, J. Yang, and Z. Zhang LC3 fluorescent puncta in autophagosomes or in protein aggregates can be distinguished by FRAP analysis in living cells Autophagy 9 2013 756 769
16. M. Pende, S.H. Um, V. Mieulet, M. Sticker, V.L. Goss, J. Mestan, M. Mueller, S. Fumagalli, S.C. Kozma, and G. Thomas S6K1(-/-)/S6K2(-/-) mice exhibit perinatal lethality and rapamycin-sensitive 5'-terminal oligopyrimidine mRNA translation and reveal a mitogen-activated protein kinase-dependent S6 kinase pathway Mol. Cell Biol. 24 2004 3112 3124
17. M. Komatsu, H. Kurokawa, S. Waguri, K. Taguchi, A. Kobayashi, Y. Ichimura, Y.S. Sou, I. Ueno, A. Sakamoto, K.I. Tong, M. Kim, Y. Nishito, S. Iemura, T. Natsume, T. Ueno, E. Kominami, H. Motohashi, K. Tanaka, and M. Yamamoto The selective autophagy substrate p62 activates the stress responsive transcription factor Nrf2 through inactivation of Keap1 Nat. Cell Biol. 12 2010 213 223
18. S.H. Bae, S.H. Sung, S.Y. Oh, J.M. Lim, S.K. Lee, Y.N. Park, H.E. Lee, D. Kang, and S.G. Rhee Sestrins activate Nrf2 by promoting p62-dependent autophagic degradation of Keap1 and prevent oxidative liver damage Cell Metab. 17 2013 73 84
19. Y. Ichimura, S. Waguri, Y.S. Sou, S. Kageyama, J. Hasegawa, R. Ishimura, T. Saito, Y. Yang, T. Kouno, T. Fukutomi, T. Hoshii, A. Hirao, K. Takagi, T. Mizushima, H. Motohashi, M.S. Lee, T. Yoshimori, K. Tanaka, M. Yamamoto, and M. Komatsu Phosphorylation of p62 activates the Keap1-Nrf2 pathway during selective autophagy Mol. Cell 51 2013 618 631
20. B. Bilanges, and B. Vanhaesebroeck A new tool to dissect the function of p70 S6 kinase Biochem. J. 431 2010 e1 3
21. C. Garrido, L. Galluzzi, M. Brunet, P.E. Puig, C. Didelot, and G. Kroemer Mechanisms of cytochrome c release from mitochondria Cell Death Differ. 13 2006 1423 1433
22. K. Taguchi, N. Fujikawa, M. Komatsu, T. Ishii, M. Unno, T. Akaike, H. Motohashi, and M. Yamamoto Keap1 degradation by autophagy for the maintenance of redox homeostasis Proc. Natl. Acad. Sci. U. S. A. 109 2012 13561 13566
23. A. Lau, X.J. Wang, F. Zhao, N.F. Villeneuve, T. Wu, T. Jiang, Z. Sun, E. White, and D.D. Zhang A noncanonical mechanism of Nrf2 activation by autophagy deficiency: direct interaction between Keap1 and p62 Mol. Cell Biol. 30 2010 3275 3285
24. J. Moscat, and M.T. Diaz-Meco p62 at the crossroads of autophagy, apoptosis, and cancer Cell 137 2009 1001 1004