Expression, purification and functional characterization of IκB kinase-2 (IKK-2) mutants

Protein Expression and Purification

Volumn 72, Issue 2, 2010, Pages 254-261

  Mathialagan, Sumathy ^a   Poda, Gennadiy I ^a   Kurumbail, Ravi G ^a   Selness, Shaun R ^a   Hall, Troii ^a   Reitz, Beverly A ^a   Weinberg, Robin A ^a   Kishore, Nandini ^a   Mbalaviele, Gabriel ^a  

^a PFIZER INC   (United States)

Author keywords

IKK 2; NEMO; NF B; PHA 408

Indexed keywords

I KAPPA B KINASE; INDAZOLE DERIVATIVE; ISONICOTINIC ACID; PHA 408; RECOMBINANT PROTEIN;

ANIMAL; ARMYWORM; ARTICLE; BIOSYNTHESIS; CELL CULTURE; CHEMICAL STRUCTURE; CHEMISTRY; COMPUTER SIMULATION; DRUG DEVELOPMENT; GENETICS; HUMAN; KINETICS; METABOLISM; METHODOLOGY; MUTATION; PHOSPHORYLATION; PROTEIN BINDING; SITE DIRECTED MUTAGENESIS; STRUCTURAL HOMOLOGY;

ANIMALS; CELLS, CULTURED; COMPUTER SIMULATION; DRUG DISCOVERY; HUMANS; I-KAPPA B KINASE; INDAZOLES; ISONICOTINIC ACIDS; KINETICS; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; MUTATION; PHOSPHORYLATION; PROTEIN BINDING; RECOMBINANT PROTEINS; SPODOPTERA; STRUCTURAL HOMOLOGY, PROTEIN;

EID: 77956202931     PISSN: 10465928     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pep.2010.02.009     Document Type: Article

References (31)

1. M. Karin, and F.R. Greten NF-[kappa]B: linking inflammation and immunity to cancer development and progression Nat. Rev. Immunol. 5 2005 749 759
2. Q. Li, and I.M. Verma NF-[kappa]B regulation in the immune system Nat. Rev. Immunol. 2 2002 725 734
3. G. Bonizzi, and M. Karin The two NF-[kappa]B activation pathways and their role in innate and adaptive immunity Trends Immunol. 25 2004 280 288
4. M.S. Hayden, and S. Ghosh Shared Principles in NF-[kappa]B Signaling Cell 132 2008 344 362
5. Z. Chen, J. Hagler, V.J. Palombella, F. Melandri, D. Scherer, D. Ballard, and T. Maniatis Signal-induced site-specific phosphorylation targets I kappa B alpha to the ubiquitin-proteasome pathway Genes Dev. 9 1995 1586 1597
6. J.A. DiDonato, F. Mercurio, and M. Karin Phosphorylation of I kappa B alpha precedes but is not sufficient for its dissociation from NF-kappa B Mol. Cell. Biol. 15 1995 1302 1311
7. K. Brown, S. Gerstberger, L. Carlson, G. Franzoso, and U. Siebenlist Control of I kappa B-alpha proteolysis by site-specific signal-induced phosphorylation Science 267 1995 1485 1488
8. S. Ghosh, and M.S. Hayden New regulators of NF-[kappa]B in inflammation Nat. Rev. Immunol. 8 2008 837 848
9. E. Niederberger, and G. Geisslinger The IKK-NF-{kappa}B pathway: a source for novel molecular drug targets in pain therapy? FASEB J. 22 2008 3432 3442
10. M. Neumann, and M. Naumann Beyond I{kappa}Bs: alternative regulation of NF-{kappa}B activity FASEB J. 21 2007 2642 2654
11. L. Yin, L. Wu, H. Wesche, C.D. Arthur, J.M. White, D.V. Goeddel, and R.D. Schreiber Defective lymphotoxin-beta receptor-induced NF-kappa B transcriptional activity in NIK-deficient mice Science 291 2001 2162 2165
12. S. Fagarasan, R. Shinkura, T. Kamata, F. Nogaki, K. Ikuta, K. Tashiro, and T. Honjo Alymphoplasia (aly)-type nuclear factor {kappa}B-inducing kinase (NIK) causes defects in secondary lymphoid tissue chemokine receptor signaling and homing of peritoneal cells to the Gut-associated lymphatic tissue system J. Exp. Med. 191 2000 1477 1486
13. A. Fütterer, K. Mink, A. Luz, M.H. Kosco-Vilbois, and K. Pfeffer The lymphotoxin [beta] receptor controls organogenesis and affinity maturation in peripheral lymphoid tissues Immunity 9 1998 59 70
14. Z.-W. Li, W. Chu, Y. Hu, M. Delhase, T. Deerinck, M. Ellisman, R. Johnson, and M. Karin The IKKbeta subunit of Ikappa B kinase (IKK) is essential for nuclear factor kappa B activation and prevention of apoptosis J. Exp. Med. 189 1999 1839 1845
15. N. Kishore, Q.K. Huynh, S. Mathialagan, T. Hall, S. Rouw, D. Creely, G. Lange, J. Caroll, B. Reitz, A. Donnelly, H. Boddupalli, R.G. Combs, K. Kretzmer, and C.S. Tripp IKK-i and TBK-1 are enzymatically distinct from the homologous enzyme IKK-2. comparative analysis of recombinant human IKK-i, TBK-1, and IKK-2 J. Biol. Chem. 277 2002 13840 13847
16. J. Strnad, and J.R. Burke I[kappa]B kinase inhibitors for treating autoimmune and inflammatory disorders: potential and challenges Trends Pharmacol. Sci. 28 2007 142 148
17. G. Takaesu, R.M. Surabhi, K.-J. Park, J. Ninomiya-Tsuji, K. Matsumoto, and R.B. Gaynor TAK1 is critical for I[kappa]B kinase-mediated activation of the nF-[kappa]B pathway J. Mol. Biol. 326 2003 105 115
18. S. Ghosh, and M. Karin Missing pieces in the NF-[kappa]B puzzle Cell 109 2002 S81 S96
19. J.R. Burke, M.A. Pattoli, K.R. Gregor, P.J. Brassil, J.F. MacMaster, K.W. McIntyre, X. Yang, V.S. Iotzova, W. Clarke, J. Strnad, Y. Qiu, and F.C. Zusi BMS-345541 is a highly selective inhibitor of Ikappa B Kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice J. Biol. Chem. 278 2003 1450 1456
20. D. Wen, Y. Nong, J.G. Morgan, P. Gangurde, A. Bielecki, J. DaSilva, M. Keaveney, H. Cheng, C. Fraser, L. Schopf, M. Hepperle, G. Harriman, B.D. Jaffee, T.D. Ocain, and Y. Xu A selective small molecule I{kappa}B Kinase beta inhibitor blocks nuclear factor {kappa}B-mediated inflammatory responses in human fibroblast-like synoviocytes, chondrocytes, and mast cells J. Pharmacol. Exp. Ther. 317 2006 989 1001
21. P.L. Podolin, J.F. Callahan, B.J. Bolognese, Y.H. Li, K. Carlson, T.G. Davis, G.W. Mellor, C. Evans, and A.K. Roshak Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of I{kappa}B kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4- fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation J. Pharmacol. Exp. Ther. 312 2005 373 381
22. K. Ziegelbauer, F. Gantner, N.W. Lukacs, A. Berlin, K. Fuchikami, T. Niki, K. Sakai, H. Inbe, K. Takeshita, M. Ishimori, H. Komura, T. Murata, T. Lowinger, and K.B. Bacon A selective novel low-molecular-weight inhibitor of I[kappa]B kinase-[beta] (IKK-[beta]) prevents pulmonary inflammation and shows broad anti-inflammatory activity Br. J. Pharmacol. 145 2005 178 192
23. M. Rushe, L. Silvian, S. Bixler, L.L. Chen, A. Cheung, S. Bowes, H. Cuervo, S. Berkowitz, T. Zheng, K. Guckian, M. Pellegrini, and A. Lugovskoy Structure of a NEMO/IKK-associating domain reveals architecture of the interaction site Structure 16 2008 798 808
24. N. Kishore, C. Sommers, S. Mathialagan, J. Guzova, M. Yao, S. Hauser, K. Huynh, S. Bonar, C. Mielke, L. Albee, R. Weier, M. Graneto, C. Hanau, T. Perry, and C.S. Tripp A selective IKK-2 inhibitor blocks NF-{kappa}B-dependent gene expression in interleukin-1{beta}-stimulated synovial fibroblasts J. Biol. Chem. 278 2003 32861 32871
25. W. Sherman, T. Day, M.P. Jacobson, R.A. Friesner, and R. Farid Novel procedure for modeling ligand/receptor induced fit effects J. Med. Chem. 49 2006 534 553
26. G. Mbalaviele, C.D. Sommers, S.L. Bonar, S. Mathialagan, J.F. Schindler, J.A. Guzova, A.F. Shaffer, M.A. Melton, L.J. Christine, C.S. Tripp, P.-C. Chiang, D.C. Thompson, Y. Hu, and N. Kishore A novel, highly selective, tight binding I{kappa}B kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the NF-{kappa}B pathway in arthritis relevant cells and animal models J. Pharmacol. Exp. Ther. 2009 jpet.108.143800
27. J.J. Buccafusco, J.W. Beach, and A.V. Terry Jr. Desensitization of nicotinic acetylcholine receptors as a strategy for drug development J. Pharmacol. Exp. Ther. 328 2009 364 370
28. E.R. Butelman, T.E. Prisinzano, H. Deng, S. Rus, and M.J. Kreek Unconditioned behavioral effects of the powerful {kappa}-opioid hallucinogen salvinorin A in nonhuman primates: fast onset and entry into cerebrospinal fluid J. Pharmacol. Exp. Ther. 328 2009 588 597
29. C.S. Gibbs, and M.J. Zoller Rational scanning mutagenesis of a protein kinase identifies functional regions involved in catalysis and substrate interactions J. Biol. Chem. 266 1991 8923 8931
30. M. Delhase, M. Hayakawa, Y. Chen, and M. Karin Positive and negative regulation of IB kinase activity through IKK subunit phosphorylation Science 284 1999 309 313
31. F. Mercurio, H. Zhu, B.W. Murray, A. Shevchenko, B.L. Bennett, J.w. Li, D.B. Young, M. Barbosa, M. Mann, A. Manning, and A. Rao IKK-1 and IKK-2: cytokine-activated I{kappa}B kinases essential for NF-B activation Science 278 1997 860 866