Structural basis of RIP1 inhibition by necrostatins

Structure

Volumn 21, Issue 3, 2013, Pages 493-499

  Xie, Tian ^a   Peng, Wei ^a   Liu, Yexing ^a   Yan, Chuangye ^a   Maki, Jenny ^b   Degterev, Alexei ^b   Yuan, Junying ^c   Shi, Yigong ^a  

^a TSINGHUA UNIVERSITY   (China)

^b TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c HARVARD MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACID; B RAF KINASE; NECROSTATIN 1 DERIVATIVE; NECROSTATIN 3 DERIVATIVE; NECROSTATIN 4 DERIVATIVE; NECROSTATIN DERIVATIVE; PROTEIN SERINE THREONINE KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; RECEPTOR INTERACTING SERINE THREONINE PROTEIN KINASE 1; UNCLASSIFIED DRUG; VEMURAFENIB;

AMINO TERMINAL SEQUENCE; ARTICLE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG PROTEIN BINDING; ENZYME CONFORMATION; ENZYME INHIBITION; ENZYME STRUCTURE; NECROPTOSIS; PRIORITY JOURNAL; PROTEIN DOMAIN;

BACULOVIRIDAE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; IMIDAZOLES; INDOLES; ISOENZYMES; KINETICS; MOLECULAR DOCKING SIMULATION; MUTATION; NECROSIS; PROTEIN INTERACTION DOMAINS AND MOTIFS; PROTEIN STRUCTURE, SECONDARY; RECEPTOR-INTERACTING PROTEIN SERINE-THREONINE KINASES; RECOMBINANT FUSION PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THERMODYNAMICS;

EID: 84874860953     PISSN: 09692126     EISSN: 18784186     Source Type: Journal    
DOI: 10.1016/j.str.2013.01.016     Document Type: Article

References (29)

1. P.D. Adams, R.W. Grosse-Kunstleve, L.W. Hung, T.R. Ioerger, A.J. McCoy, N.W. Moriarty, R.J. Read, J.C. Sacchettini, N.K. Sauter, and T.C. Terwilliger PHENIX: building new software for automated crystallographic structure determination Acta Crystallogr. D Biol. Crystallogr. 58 2002 1948 1954
2. G. Bollag, P. Hirth, J. Tsai, J. Zhang, P.N. Ibrahim, H. Cho, W. Spevak, C. Zhang, Y. Zhang, and G. Habets Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma Nature 467 2010 596 599
3. CCP4 (Collaborative Computational Project, Number 4) The CCP4 suite: programs for protein crystallography Acta Crystallogr. D Biol. Crystallogr. 50 1994 760 763
4. D.E. Christofferson, and J. Yuan Necroptosis as an alternative form of programmed cell death Curr. Opin. Cell Biol. 22 2010 263 268
5. A. Degterev, Z. Huang, M. Boyce, Y. Li, P. Jagtap, N. Mizushima, G.D. Cuny, T.J. Mitchison, M.A. Moskowitz, and J. Yuan Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury Nat. Chem. Biol. 1 2005 112 119
6. A. Degterev, J. Hitomi, M. Germscheid, I.L. Ch'en, O. Korkina, X. Teng, D. Abbott, G.D. Cuny, C. Yuan, and G. Wagner Identification of RIP1 kinase as a specific cellular target of necrostatins Nat. Chem. Biol. 4 2008 313 321
7. DeLano, W.L. (2002). The PyMOL Molecular Graphics System. http://www.pymol.org.
8. P. Emsley, and K. Cowtan Coot: model-building tools for molecular graphics Acta Crystallogr. D Biol. Crystallogr. 60 2004 2126 2132
9. M. Feoktistova, P. Geserick, B. Kellert, D.P. Dimitrova, C. Langlais, M. Hupe, K. Cain, M. MacFarlane, G. Häcker, and M. Leverkus cIAPs block Ripoptosome formation, a RIP1/caspase-8 containing intracellular cell death complex differentially regulated by cFLIP isoforms Mol. Cell 43 2011 449 463
10. P.D. Jeffrey, A.A. Russo, K. Polyak, E. Gibbs, J. Hurwitz, J. Massagué, and N.P. Pavletich Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex Nature 376 1995 313 320
11. D.R. Knighton, J.H. Zheng, L.F. Ten Eyck, V.A. Ashford, N.H. Xuong, S.S. Taylor, and J.M. Sowadski Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase Science 253 1991 407 414
12. D.R. Knighton, J.H. Zheng, L.F. Ten Eyck, N.H. Xuong, S.S. Taylor, and J.M. Sowadski Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase Science 253 1991 414 420
13. A.P. Kornev, N.M. Haste, S.S. Taylor, and L.F. Eyck Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism Proc. Natl. Acad. Sci. USA 103 2006 17783 17788
14. S.Y. Lim, S.M. Davidson, M.M. Mocanu, D.M. Yellon, and C.C. Smith The cardioprotective effect of necrostatin requires the cyclophilin-D component of the mitochondrial permeability transition pore Cardiovasc. Drugs Ther. 21 2007 467 469
15. A.J. McCoy, R.W. Grosse-Kunstleve, P.D. Adams, M.D. Winn, L.C. Storoni, and R.J. Read Phaser crystallographic software J. Appl. Cryst. 40 2007 658 674
16. Z. Otwinowski, and W. Minor Processing of X-ray diffraction data collected in oscillation mode Methods Enzymol. 276 1997 307 326
17. E.F. Pettersen, T.D. Goddard, C.C. Huang, G.S. Couch, D.M. Greenblatt, E.C. Meng, and T.E. Ferrin UCSF Chimera - a visualization system for exploratory research and analysis J. Comput. Chem. 25 2004 1605 1612
18. M.J. Robinson, and M.H. Cobb Mitogen-activated protein kinase pathways Curr. Opin. Cell Biol. 9 1997 180 186
19. M. Röring, and T. Brummer Aberrant B-Raf signaling in human cancer - 10 years from bench to bedside Crit. Rev. Oncog. 17 2012 97 121
20. D.M. Rosenbaum, A. Degterev, J. David, P.S. Rosenbaum, S. Roth, J.C. Grotta, G.D. Cuny, J. Yuan, and S.I. Savitz Necroptosis, a novel form of caspase-independent cell death, contributes to neuronal damage in a retinal ischemia-reperfusion injury model J. Neurosci. Res. 88 2010 1569 1576
21. B.Z. Stanger, P. Leder, T.H. Lee, E. Kim, and B. Seed RIP: a novel protein containing a death domain that interacts with Fas/APO-1 (CD95) in yeast and causes cell death Cell 81 1995 513 523
22. N. Stein CHAINSAW: a program for mutating pdb files used as templates in molecular replacement J. Appl. Crystallogr. 41 2008 641 643
23. X. Sun, J. Yin, M.A. Starovasnik, W.J. Fairbrother, and V.M. Dixit Identification of a novel homotypic interaction motif required for the phosphorylation of receptor-interacting protein (RIP) by RIP3 J. Biol. Chem. 277 2002 9505 9511
24. N. Takahashi, L. Duprez, S. Grootjans, A. Cauwels, W. Nerinckx, J.B. DuHadaway, V. Goossens, R. Roelandt, F. Van Hauwermeiren, and C. Libert Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models Cell Death Dis. 3 2012 e437
25. T. Tenev, K. Bianchi, M. Darding, M. Broemer, C. Langlais, F. Wallberg, A. Zachariou, J. Lopez, M. MacFarlane, K. Cain, and P. Meier The Ripoptosome, a signaling platform that assembles in response to genotoxic stress and loss of IAPs Mol. Cell 43 2011 432 448
26. J. Tsai, J.T. Lee, W. Wang, J. Zhang, H. Cho, S. Mamo, R. Bremer, S. Gillette, J. Kong, and N.K. Haass Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity Proc. Natl. Acad. Sci. USA 105 2008 3041 3046
27. P. Vandenabeele, L. Galluzzi, T. Vanden Berghe, and G. Kroemer Molecular mechanisms of necroptosis: an ordered cellular explosion Nat. Rev. Mol. Cell Biol. 11 2010 700 714
28. P.T. Wan, M.J. Garnett, S.M. Roe, S. Lee, D. Niculescu-Duvaz, V.M. Good, C.M. Jones, C.J. Marshall, C.J. Springer, D. Barford, R. Marais Cancer Genome Project Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF Cell 116 2004 855 867
29. Z. You, S.I. Savitz, J. Yang, A. Degterev, J. Yuan, G.D. Cuny, M.A. Moskowitz, and M.J. Whalen Necrostatin-1 reduces histopathology and improves functional outcome after controlled cortical impact in mice J. Cereb. Blood Flow Metab. 28 2008 1564 1573