How chemoproteomics can enable drug discovery and development

Chemistry and Biology

Volumn 19, Issue 1, 2012, Pages 11-22

  Moellering, Raymond E ^a   Cravatt, Benjamin F ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; CRIZOTINIB; CYSTEINE PROTEINASE INHIBITOR; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; ENZYME; ENZYME INHIBITOR; HISTONE DEACETYLASE; HISTONE DEACETYLASE 1; HISTONE DEACETYLASE 3; HISTONE DEACETYLASE 6; HISTONE DEACETYLASE INHIBITOR; HYDROLASE; HYDROLASE INHIBITOR; OXIDOREDUCTASE; PF 04457845; PIPERLONGUMINE; PROTEIN; PROTEIN KINASE; SERINE HYDROLASE INHIBITOR; SERINE PROTEINASE INHIBITOR; UNCLASSIFIED DRUG;

ACTIVITY BASED PROTEIN PROFILING; CHEMISTRY; CHEMOPROTEOMICS; CLINICAL TRIAL (TOPIC); DRUG DESIGN; DRUG DEVELOPMENT; DRUG EFFICACY; DRUG POTENCY; DRUG SCREENING; DRUG TARGETING; GENE SEQUENCE; HUMAN; HUMAN GENOME; IN VITRO STUDY; IN VIVO STUDY; LUNG NON SMALL CELL CANCER; METABOLISM; MOLECULAR LIBRARY; NONHUMAN; OXIDATIVE STRESS; PHARMACODYNAMICS; PHARMACOGENETICS; PHENOTYPE; POLYPHARMACY; PROTEIN ANALYSIS; PROTEIN FUNCTION; PROTEIN PROCESSING; PROTEIN SYNTHESIS; PROTEOMICS; REVIEW;

DRUG DISCOVERY; ENZYMES; GENOME, HUMAN; HUMANS; METABOLIC NETWORKS AND PATHWAYS; PROTEOMICS; SERINE PROTEINASE INHIBITORS; SMALL MOLECULE LIBRARIES;

EID: 84856402803     PISSN: 10745521     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.chembiol.2012.01.001     Document Type: Review

References (95)

1. A. Adibekian, B.R. Martin, C. Wang, K.L. Hsu, D.A. Bachovchin, S. Niessen, H. Hoover, and B.F. Cravatt Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors Nat. Chem. Biol. 7 2011 469 478
2. S. Arastu-Kapur, E.L. Ponder, U.P. Fonović, S. Yeoh, F. Yuan, M. Fonović, M. Grainger, C.I. Phillips, J.C. Powers, and M. Bogyo Identification of proteases that regulate erythrocyte rupture by the malaria parasite Plasmodium falciparum Nat. Chem. Biol. 4 2008 203 213 (Pubitemid 351264129)
3. S. Arastu-Kapur, J.L. Anderl, M. Kraus, F. Parlati, K.D. Shenk, S.J. Lee, T. Muchamuel, M.K. Bennett, C. Driessen, A.J. Ball, and C.J. Kirk Nonproteasomal targets of the proteasome inhibitors bortezomib and carfilzomib: a link to clinical adverse events Clin. Cancer Res. 17 2011 2734 2743
4. D.A. Bachovchin, S.J. Brown, H. Rosen, and B.F. Cravatt Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes Nat. Biotechnol. 27 2009 387 394
5. D.A. Bachovchin, T. Ji, W. Li, G.M. Simon, J.L. Blankman, A. Adibekian, H. Hoover, S. Niessen, and B.F. Cravatt Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening Proc. Natl. Acad. Sci. USA 107 2010 20941 20946
6. D.A. Bachovchin, J.T. Mohr, A.E. Speers, C. Wang, J.M. Berlin, T.P. Spicer, V. Fernandez-Vega, P. Chase, P.S. Hodder, and S.C. Schürer Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors Proc. Natl. Acad. Sci. USA 108 2011 6811 6816
7. M. Bantscheff, D. Eberhard, Y. Abraham, S. Bastuck, M. Boesche, S. Hobson, T. Mathieson, J. Perrin, M. Raida, and C. Rau Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors Nat Biotechnol. 25 2007 1035 1044 (Pubitemid 47517638)
8. M. Bantscheff, C. Hopf, M.M. Savitski, A. Dittmann, P. Grandi, A.M. Michon, J. Schlegl, Y. Abraham, I. Becher, and G. Bergamini Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes Nat. Biotechnol. 29 2011 255 265
9. T. Berg, S.B. Cohen, J. Desharnais, C. Sonderegger, D.J. Maslyar, J. Goldberg, D.L. Boger, and P.K. Vogt Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts Proc. Natl. Acad. Sci. USA 99 2002 3830 3835 (Pubitemid 34252191)
10. F. Bernal, A.F. Tyler, S.J. Korsmeyer, L.D. Walensky, and G.L. Verdine Reactivation of the p53 tumor suppressor pathway by a stapled p53 peptide J. Am. Chem. Soc. 129 2007 2456 2457 (Pubitemid 46364050)
11. A.D. Boran, and R. Iyengar Systems approaches to polypharmacology and drug discovery Curr. Opin. Drug Discov. Devel. 13 2010 297 309
12. J.E. Bradner, N. West, M.L. Grachan, E.F. Greenberg, S.J. Haggarty, T. Warnow, and R. Mazitschek Chemical phylogenetics of histone deacetylases Nat. Chem. Biol. 6 2010 238 243
13. C.R. Braun, J. Mintseris, E. Gavathiotis, G.H. Bird, S.P. Gygi, and L.D. Walensky Photoreactive stapled BH3 peptides to dissect the BCL-2 family interactome Chem. Biol. 17 2010 1325 1333
14. M.E. Bunnage Getting pharmaceutical R&D back on target Nat. Chem. Biol. 7 2011 335 339
15. J.W. Chang, D.K. Nomura, and B.F. Cravatt A potent and selective inhibitor of KIAA1363/AADACL1 that impairs prostate cancer pathogenesis Chem. Biol. 18 2011 476 484
16. S. Chen, J.T. Do, Q. Zhang, S. Yao, F. Yan, E.C. Peters, H.R. Schöler, P.G. Schultz, and S. Ding Self-renewal of embryonic stem cells by a small molecule Proc. Natl. Acad. Sci. USA 103 2006 17266 17271 (Pubitemid 44788958)
17. K.P. Chiang, S. Niessen, A. Saghatelian, and B.F. Cravatt An enzyme that regulates ether lipid signaling pathways in cancer annotated by multidimensional profiling Chem. Biol. 13 2006 1041 1050 (Pubitemid 44557068)
18. H.R. Christofk, M.G. Vander Heiden, M.H. Harris, A. Ramanathan, R.E. Gerszten, R. Wei, M.D. Fleming, S.L. Schreiber, and L.C. Cantley The M2 splice isoform of pyruvate kinase is important for cancer metabolism and tumour growth Nature 452 2008 230 233 (Pubitemid 351380249)
19. B.F. Cravatt, A.T. Wright, and J.W. Kozarich Activity-based protein profiling: from enzyme chemistry to proteomic chemistry Annu Rev Biochem. 77 2008 383 414
20. M.S. Cohen, C. Zhang, K.M. Shokat, and J. Taunton Structural bioinformatics-based design of selective, irreversible kinase inhibitors Science 308 2005 1318 1321 (Pubitemid 40746129)
21. M.S. Cohen, H. Hadjivassiliou, and J. Taunton A clickable inhibitor reveals context-dependent autoactivation of p90 RSK Nat. Chem. Biol. 3 2007 156 160
22. B.F. Cravatt, D.K. Giang, S.P. Mayfield, D.L. Boger, R.A. Lerner, and N.B. Gilula Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides Nature 384 1996 83 87 (Pubitemid 26374593)
23. L. Dang, D.W. White, S. Gross, B.D. Bennett, M.A. Bittinger, E.M. Driggers, V.R. Fantin, H.G. Jang, S. Jin, and M.C. Keenan Cancer-associated IDH1 mutations produce 2-hydroxyglutarate Nature 462 2009 739 744
24. M.I. Davis, J.P. Hunt, S. Herrgard, P. Ciceri, L.M. Wodicka, G. Pallares, M. Hocker, D.K. Treiber, and P.P. Zarrinkar Comprehensive analysis of kinase inhibitor selectivity Nat. Biotechnol. 29 2011 1046 1051
25. M.A. Dawson, R.K. Prinjha, A. Dittmann, G. Giotopoulos, M. Bantscheff, W.I. Chan, S.C. Robson, C.W. Chung, C. Hopf, and M.M. Savitski Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia Nature 478 2011 529 533
26. 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 (Pubitemid 351550892)
27. J.E. Delmore, G.C. Issa, M.E. Lemieux, P.B. Rahl, J. Shi, H.M. Jacobs, E. Kastritis, T. Gilpatrick, R.M. Paranal, and J. Qi BET bromodomain inhibition as a therapeutic strategy to target c-Myc Cell 146 2011 904 917
28. X. Deng, N. Dzamko, A. Prescott, P. Davies, Q. Liu, Q. Yang, J.D. Lee, M.P. Patricelli, T.K. Nomanbhoy, D.R. Alessi, and N.S. Gray Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2 Nat. Chem. Biol. 7 2011 203 205
29. X. Deng, Q. Yang, N. Kwiatkowski, T. Sim, U. McDermott, J.E. Settleman, J.D. Lee, and N.S. Gray Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin- 6(11H)-one as a potent and selective inhibitor of big MAP kinase 1 ACS Med Chem Lett 2 2011 195 200
30. E. Deu, M.J. Leyva, V.E. Albrow, M.J. Rice, J.A. Ellman, and M. Bogyo Functional studies of Plasmodium falciparum dipeptidyl aminopeptidase I using small molecule inhibitors and active site probes Chem. Biol. 17 2010 808 819
31. A.M. Edwards, R. Isserlin, G.D. Bader, S.V. Frye, T.M. Willson, and F.H. Yu Too many roads not taken Nature 470 2011 163 165
32. K.H. Emami, C. Nguyen, H. Ma, D.H. Kim, K.W. Jeong, M. Eguchi, R.T. Moon, J.L. Teo, H.Y. Kim, and S.H. Moon A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected] Proc. Natl. Acad. Sci. USA 101 2004 12682 12687 (Pubitemid 39122083)
33. M. Entzeroth, B. Chapelain, J. Guilbert, and V. Hamon High throughput drug profiling J. Autom. Methods Manag. Chem. 22 2000 171 173 (Pubitemid 32014583)
34. M.J. Evans, A. Saghatelian, E.J. Sorensen, and B.F. Cravatt Target discovery in small-molecule cell-based screens by in situ proteome reactivity profiling Nat. Biotechnol. 23 2005 1303 1307 (Pubitemid 41486859)
35. M.A. Fabian, W.H. Biggs 3rd, D.K. Treiber, C.E. Atteridge, M.D. Azimioara, M.G. Benedetti, T.A. Carter, P. Ciceri, P.T. Edeen, and M. Floyd A small molecule-kinase interaction map for clinical kinase inhibitors Nat. Biotechnol. 23 2005 329 336 (Pubitemid 41094421)
36. M.E. Feldman, B. Apsel, A. Uotila, R. Loewith, Z.A. Knight, D. Ruggero, and K.M. Shokat Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2 PLoS Biol. 7 2009 e38
37. J.J. Fischer, S. Michaelis, A.K. Schrey, A. Diehl, O.Y. Graebner, J. Ungewiss, S. Horzowski, M. Glinski, F. Kroll, M. Dreger, and H. Koester SAHA Capture Compound - a novel tool for the profiling of histone deacetylases and the identification of additional vorinostat binders Proteomics 11 2011 4096 4104
38. S.M. Gadgeel, and G. Bepler Crizotinib: an anaplastic lymphoma kinase inhibitor Future Oncol. 7 2011 947 953
39. D.M. Goldstein, N.S. Gray, and P.P. Zarrinkar High-throughput kinase profiling as a platform for drug discovery Nat. Rev. Drug Discov. 7 2008 391 397 (Pubitemid 351619111)
40. D.C. Greenbaum, A. Baruch, M. Grainger, Z. Bozdech, K.F. Medzihradszky, J. Engel, J. DeRisi, A.A. Holder, and M. Bogyo A role for the protease falcipain 1 in host cell invasion by the human malaria parasite Science 298 2002 2002 2006 (Pubitemid 35425258)
41. C.I. Hall, M.L. Reese, E. Weerapana, M.A. Child, P.W. Bowyer, V.E. Albrow, J.D. Haraldsen, M.R. Phillips, E.D. Sandoval, and G.E. Ward Chemical genetic screen identifies Toxoplasma DJ-1 as a regulator of parasite secretion, attachment, and invasion Proc. Natl. Acad. Sci. USA 108 2011 10568 10573
42. M.W. Harding, A. Galat, D.E. Uehling, and S.L. Schreiber A receptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase Nature 341 1989 758 760 (Pubitemid 19260893)
43. L.K. Henchey, A.L. Jochim, and P.S. Arora Contemporary strategies for the stabilization of peptides in the α-helical conformation Curr. Opin. Chem. Biol. 12 2008 692 697
44. J.C. Henise, and J. Taunton Irreversible Nek2 kinase inhibitors with cellular activity J. Med. Chem. 54 2011 4133 4146
45. S.M. Huang, Y.M. Mishina, S. Liu, A. Cheung, F. Stegmeier, G.A. Michaud, O. Charlat, E. Wiellette, Y. Zhang, and S. Wiessner Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling Nature 461 2009 614 620
46. J.K. Ichida, J. Blanchard, K. Lam, E.Y. Son, J.E. Chung, D. Egli, K.M. Loh, A.C. Carter, F.P. Di Giorgio, and K. Koszka A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog Cell Stem Cell 5 2009 491 503
47. D.S. Johnson, C. Stiff, S.E. Lazerwith, S.R. Kesten, L.K. Fay, M. Morris, D. Beidler, M.B. Liimatta, S.E. Smith, and D.T. Dudley Discovery of PF-04457845: a highly potent, orally bioavailable, and selective urea FAAH inhibitor ACS Med Chem Lett 2 2011 91 96
48. A.C. Kasper, J.B. Baker, H. Kim, and J. Hong The end game of chemical genetics: target identification Future Med Chem 1 2009 727 736
49. A.F. Kluge, and R.C. Petter Acylating drugs: redesigning natural covalent inhibitors Curr. Opin. Chem. Biol. 14 2010 421 427
50. Z.A. Knight, B. Gonzalez, M.E. Feldman, E.R. Zunder, D.D. Goldenberg, O. Williams, R. Loewith, D. Stokoe, A. Balla, and B. Toth A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling Cell 125 2006 733 747
51. Z.A. Knight, H. Lin, and K.M. Shokat Targeting the cancer kinome through polypharmacology Nat. Rev. Cancer 10 2010 130 137
52. N. Kwiatkowski, N. Jelluma, P. Filippakopoulos, M. Soundararajan, M.S. Manak, M. Kwon, H.G. Choi, T. Sim, Q.L. Deveraux, and S. Rottmann Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function Nat. Chem. Biol. 6 2010 359 368
53. D. Leung, C. Hardouin, D.L. Boger, and B.F. Cravatt Discovering potent and selective reversible inhibitors of enzymes in complex proteomes Nat. Biotechnol. 21 2003 687 691 (Pubitemid 36638097)
54. W. Li, J.L. Blankman, and B.F. Cravatt A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases J. Am. Chem. Soc. 129 2007 9594 9595 (Pubitemid 47237463)
55. Y. Liu, M.P. Patricelli, and B.F. Cravatt Activity-based protein profiling: the serine hydrolases Proc. Natl. Acad. Sci. USA 96 1999 14694 14699 (Pubitemid 30019702)
56. J.Z. Long, and B.F. Cravatt The metabolic serine hydrolases and their functions in mammalian physiology and disease Chem. Rev. 111 2011 6022 6063
57. J.Z. Long, W. Li, L. Booker, J.J. Burston, S.G. Kinsey, J.E. Schlosburg, F.J. Pavón, A.M. Serrano, D.E. Selley, and L.H. Parsons Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects Nat. Chem. Biol. 5 2009 37 44
58. C.V. Miduturu, X. Deng, N. Kwiatkowski, W. Yang, L. Brault, P. Filippakopoulos, E. Chung, Q. Yang, J. Schwaller, and S. Knapp High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors Chem. Biol. 18 2011 868 879
59. D.K. Miller, J.W. Gillard, P.J. Vickers, S. Sadowski, C. Léveillé, J.A. Mancini, P. Charleson, R.A. Dixon, A.W. Ford-Hutchinson, and R. Fortin Identification and isolation of a membrane protein necessary for leukotriene production Nature 343 1990 278 281
60. R.E. Moellering, M. Cornejo, T.N. Davis, C. Del Bianco, J.C. Aster, S.C. Blacklow, A.L. Kung, D.G. Gilliland, G.L. Verdine, and J.E. Bradner Direct inhibition of the NOTCH transcription factor complex Nature 462 2009 182 188
61. K. Moulick, J.H. Ahn, H. Zong, A. Rodina, L. Cerchietti, E.M. Gomes DaGama, E. Caldas-Lopes, K. Beebe, F. Perna, and K. Hatzi Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90 Nat. Chem. Biol. 7 2011 818 826
62. B.H. Munos, and W.W. Chin How to revive breakthrough innovation in the pharmaceutical industry Sci. Transl. Med. 3 2011 89cm16
63. A. Nekrutenko, D.M. Hillis, J.C. Patton, R.D. Bradley, and R.J. Baker Cytosolic isocitrate dehydrogenase in humans, mice, and voles and phylogenetic analysis of the enzyme family Mol. Biol. Evol. 15 1998 1674 1684 (Pubitemid 28550991)
64. R.H. Nelson, and J.M. Miles The use of orlistat in the treatment of obesity, dyslipidaemia and type 2 diabetes Expert Opin. Pharmacother. 6 2005 2483 2491 (Pubitemid 41701050)
65. S.E. Ong, M. Schenone, A.A. Margolin, X. Li, K. Do, M.K. Doud, D.R. Mani, L. Kuai, X. Wang, and J.L. Wood Identifying the proteins to which small-molecule probes and drugs bind in cells Proc. Natl. Acad. Sci. USA 106 2009 4617 4622
66. J.P. Overington, B. Al-Lazikani, and A.L. Hopkins How many drug targets are there? Nat. Rev. Drug Discov. 5 2006 993 996 (Pubitemid 44835126)
67. D.W. Parsons, S. Jones, X. Zhang, J.C. Lin, R.J. Leary, P. Angenendt, P. Mankoo, H. Carter, I.M. Siu, and G.L. Gallia An integrated genomic analysis of human glioblastoma multiforme Science 321 2008 1807 1812
68. A. Patgiri, K.K. Yadav, P.S. Arora, and D. Bar-Sagi An orthosteric inhibitor of the Ras-Sos interaction Nat. Chem. Biol. 7 2011 585 587
69. M.P. Patricelli, A.K. Szardenings, M. Liyanage, T.K. Nomanbhoy, M. Wu, H. Weissig, A. Aban, D. Chun, S. Tanner, and J.W. Kozarich Functional interrogation of the kinome using nucleotide acyl phosphates Biochemistry 46 2007 350 358 (Pubitemid 46105428)
70. M.P. Patricelli, T.K. Nomanbhoy, J. Wu, H. Brown, D. Zhou, J. Zhang, S. Jagannathan, A. Aban, E. Okerberg, and C. Herring In situ kinase profiling reveals functionally relevant properties of native kinases Chem. Biol. 18 2011 699 710
71. M. Racchi, M. Mazzucchelli, E. Porrello, C. Lanni, and S. Govoni Acetylcholinesterase inhibitors: novel activities of old molecules Pharmacol. Res. 50 2004 441 451 (Pubitemid 39089089)
72. L. Raj, T. Ide, A.U. Gurkar, M. Foley, M. Schenone, X. Li, N.J. Tolliday, T.R. Golub, S.A. Carr, and A.F. Shamji Selective killing of cancer cells by a small molecule targeting the stress response to ROS Nature 475 2011 231 234
73. A.P. Russ, and S. Lampel The druggable genome: an update Drug Discov. Today 10 2005 1607 1610 (Pubitemid 41817609)
74. C.M. Salisbury, and B.F. Cravatt Activity-based probes for proteomic profiling of histone deacetylase complexes Proc. Natl. Acad. Sci. USA 104 2007 1171 1176 (Pubitemid 46183977)
75. C.M. Salisbury, and B.F. Cravatt Optimization of activity-based probes for proteomic profiling of histone deacetylase complexes J. Am. Chem. Soc. 130 2008 2184 2194 (Pubitemid 351287995)
76. T. Shahian, G.M. Lee, A. Lazic, L.A. Arnold, P. Velusamy, C.M. Roels, R.K. Guy, and C.S. Craik Inhibition of a viral enzyme by a small-molecule dimer disruptor Nat. Chem. Biol. 5 2009 640 646
77. G.M. Simon, and B.F. Cravatt Activity-based proteomics of enzyme superfamilies: serine hydrolases as a case study J. Biol. Chem. 285 2010 11051 11055
78. M. Soda, Y.L. Choi, M. Enomoto, S. Takada, Y. Yamashita, S. Ishikawa, S. Fujiwara, H. Watanabe, K. Kurashina, and H. Hatanaka Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer Nature 448 2007 561 566 (Pubitemid 47206930)
79. D.C. Swinney, and J. Anthony How were new medicines discovered? Nat. Rev. Drug Discov. 10 2011 507 519
80. D.M. Tagore, W.M. Nolte, J.M. Neveu, R. Rangel, L. Guzman-Rojas, R. Pasqualini, W. Arap, W.S. Lane, and A. Saghatelian Peptidase substrates via global peptide profiling Nat. Chem. Biol. 5 2009 23 25
81. J. Taunton, C.A. Hassig, and S.L. Schreiber A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p Science 272 1996 408 411 (Pubitemid 26138177)
82. N.A. Thornberry, and A.E. Weber Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes Curr. Top. Med. Chem. 7 2007 557 568 (Pubitemid 46488280)
83. N.A. Thornberry, H.G. Bull, J.R. Calaycay, K.T. Chapman, A.D. Howard, M.J. Kostura, D.K. Miller, S.M. Molineaux, J.R. Weidner, and J. Aunins A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes Nature 356 1992 768 774
84. J. Trepel, M. Mollapour, G. Giaccone, and L. Neckers Targeting the dynamic HSP90 complex in cancer Nat. Rev. Cancer 10 2010 537 549
85. M.G. Vander Heiden, J.W. Locasale, K.D. Swanson, H. Sharfi, G.J. Heffron, D. Amador-Noguez, H.R. Christofk, G. Wagner, J.D. Rabinowitz, J.M. Asara, and L.C. Cantley Evidence for an alternative glycolytic pathway in rapidly proliferating cells Science 329 2010 1492 1499
86. J. Vermehren, and C. Sarrazin New hepatitis C therapies in clinical development Eur. J. Med. Res. 16 2011 303 314
87. L.D. Walensky, A.L. Kung, I. Escher, T.J. Malia, S. Barbuto, R.D. Wright, G. Wagner, G.L. Verdine, and S.J. Korsmeyer Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix Science 305 2004 1466 1470 (Pubitemid 39167667)
88. M.J. Walsh, K.R. Brimacombe, H. Veith, J.M. Bougie, T. Daniel, W. Leister, L.C. Cantley, W.J. Israelsen, M.G. Vander Heiden, and M. Shen 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase Bioorg. Med. Chem. Lett. 21 2011 6322 6327
89. E. Weerapana, C. Wang, G.M. Simon, F. Richter, S. Khare, M.B. Dillon, D.A. Bachovchin, K. Mowen, D. Baker, and B.F. Cravatt Quantitative reactivity profiling predicts functional cysteines in proteomes Nature 468 2010 790 795
90. A.T. Wright, and B.F. Cravatt Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo Chem. Biol. 14 2007 1043 1051 (Pubitemid 47404904)
91. A.T. Wright, J.D. Song, and B.F. Cravatt A suite of activity-based probes for human cytochrome P450 enzymes J. Am. Chem. Soc. 131 2009 10692 10700
92. N. Yagoda, M. von Rechenberg, E. Zaganjor, A.J. Bauer, W.S. Yang, D.J. Fridman, A.J. Wolpaw, I. Smukste, J.M. Peltier, and J.J. Boniface RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels Nature 447 2007 864 868 (Pubitemid 46920135)
93. Q. Yang, X. Deng, B. Lu, M. Cameron, C. Fearns, M.P. Patricelli, J.R. Yates 3rd, N.S. Gray, and J.D. Lee Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein Cancer Cell 18 2010 258 267
94. J. Zhang, P.L. Yang, and N.S. Gray Targeting cancer with small molecule kinase inhibitors Nat. Rev. Cancer 9 2009 28 39
95. H.Y. Zou, Q. Li, J.H. Lee, M.E. Arango, S.R. McDonnell, S. Yamazaki, T.B. Koudriakova, G. Alton, J.J. Cui, and P.P. Kung An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms Cancer Res. 67 2007 4408 4417 (Pubitemid 46815090)