Identification of Potent Ras Signaling Inhibitors by Pathway-Selective Phenotype-Based Screening

Angewandte Chemie - International Edition

Volumn 43, Issue 4, 2004, Pages 450-454

  Müller, Oliver ^a   Gourzoulidou, Eleni ^a,b   Carpintero, Mercedes ^a,b   Karaguni, Ioanna Maria ^a   Langerak, Anette ^a   Herrmann, Christian ^a,b   Möröy, Tarik ^c   Klein Hitpaß, Ludger ^c   Waldmann, Herbert ^a,b  

^a MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY   (Germany)

^b TU DORTMUND UNIVERSITY   (Germany)

^c UNIVERSITY HOSPITAL ESSEN   (Germany)

Author keywords

Bioorganic chemistry; Combinatorial chemistry; Library screening; Medicinal chemistry; Signal transduction

Indexed keywords

PATHWAY-SELECTIVE PHENOTYPE BASED SCREENING; POTENT RAS SIGNALING INHIBITORS;

ENZYME INHIBITION; MICROSCOPIC EXAMINATION; TUMORS;

BIOLOGICAL MATERIALS;

NONSTEROID ANTIINFLAMMATORY AGENT; RAF PROTEIN; RAS PROTEIN; RAS SIGNALING INHIBITOR; SULINDAC; SULINDAC DERIVATIVE; UNCLASSIFIED DRUG; WNT PROTEIN;

ANIMAL CELL; ARTICLE; CELL LINE; CONCENTRATION RESPONSE; DRUG EFFECT; DRUG SCREENING; DRUG SYNTHESIS; MICROSCOPY; NONHUMAN; PHENOTYPE; PROTEIN PROTEIN INTERACTION; SIGNAL TRANSDUCTION;

ANIMALS; ANNEXIN A5; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; APOPTOSIS; CELL DIVISION; CELL LINE; CELL LINE, TRANSFORMED; CELL SURVIVAL; CELL TRANSFORMATION, NEOPLASTIC; COMBINATORIAL CHEMISTRY TECHNIQUES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SCREENING ASSAYS, ANTITUMOR; EPITHELIAL CELLS; GENES, RAS; INHIBITORY CONCENTRATION 50; MICROSCOPY, FLUORESCENCE; PHENOTYPE; PROTO-ONCOGENE PROTEINS; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; SULINDAC; WNT PROTEINS; ZEBRAFISH PROTEINS;

EID: 0842299428     PISSN: 14337851     EISSN: None     Source Type: Journal    
DOI: 10.1002/anie.200352587     Document Type: Article

References (27)

1. Review: B. R. Stockwell, Neuron 2002, 36, 559-562.
2. See, for example, a) T. U. Mayer, T. M. Kapoor, S. J. Haggarty, R. W. King, S. L. Schreiber, T. J. Mitchison, Science 1999, 286, 971-974;
3. b) S. Hotha, J. C. Yarrow, J. G. Yang, S. Garrett, K. V. Renduchintala, T. U. Mayer, T. M. Kappor, Angew. Chem. 2003, 115, 2481-2484; Angew. Chem. Int. Ed. 2003, 42, 2379-2382.
4. b) S. Hotha, J. C. Yarrow, J. G. Yang, S. Garrett, K. V. Renduchintala, T. U. Mayer, T. M. Kappor, Angew. Chem. 2003, 115, 2481-2484; Angew. Chem. Int. Ed. 2003, 42, 2379-2382.
5. B. E. Evans, K. E. Rittle, M. G. Bock, R. M. DiPardo, R. M. Freidinger, W. L. Whitter, G. F. Lundell, D. E. Veber, P. S. Anderson, R. S. L. Chang, V. J. Lorri, D. J. Cerino, T. B. Chen, P. J. Kling, K. A. Kunkel, J. P. Sprinter, J. Hirshfield, J. Med. Chem. 1988, 31, 2235-2246.
6. R. Breinbauer, I. R. Vetter, H. Waldmann, Angew. Chem. 2002, 114, 3002-3015; Angew. Chem. Int Ed. 2002, 41, 2879-2890.
7. R. Breinbauer, I. R. Vetter, H. Waldmann, Angew. Chem. 2002, 114, 3002-3015; Angew. Chem. Int Ed. 2002, 41, 2879-2890.
8. Reviews: a) H. Waldmann, A. Wittinghofer, Angew. Chem. 2000, 112, 4360-4383; Angew. Chem. Int. Ed. 2000, 39, 4192-4214;
9. Reviews: a) H. Waldmann, A. Wittinghofer, Angew. Chem. 2000, 112, 4360-4383; Angew. Chem. Int. Ed. 2000, 39, 4192-4214;
10. b) J. Downward, Nat. Rev. Cancer 2002, 3, 11-22.
11. a) C. Herrmann, C. Block, C. Geisen, K. Haas, C. Weber, G. Winde, T. Moroy, O. Müller, Oncogene 1998, 17, 1769-1776;
12. b) I. M. Karaguni, P. Herter, P. Debruyne, S. Chtarbova, A. Kasprzynski, U. Herbrand, M. R. Ahmadian, K. H. Glusenkamp, G. Winde, M. Mareel, Cancer Res 2002, 62, 1718-1723.
13. J. Kato-Stankiewicz, I. Hakimi, G. Zhi, J. Zhang, I. Serebriiskii, L. Guo, H. Edamatsu, H. Koide, S. Menon, R. Eckl, S. Sakamuri, Y. Lu, Q.-Z. Chen, S. Agarwal, W. R. Baumbach, E. A. Golemis, F. Tamanoi, V. Khazak, Proc. Natl. Acad. Sci. USA 2002, 99, 14398-14403.
14. a) M. J. Thun, S. J. Henley, C. Patrono, J. Natl. Cancer Inst. 2002, 94, 252-266;
15. b) E. T. Goluboff, Expert Opin. Invest. Drugs 2001, 10, 1875-1882;
16. c) I.-M. Karaguni, M. Carpintero, E. Gourzoulidou, L. Klein-Hitpaβ, T. Möröy, H. Waldmann, O. Müller, unpublished work.
17. a) T-Y. Shen, B. E. Witzel, H. Jones, B. O. Linn, R. B. Greenwald (Merck and Co.), DE 2039426, 1971 [Chem Abstr. 1971, 74, 141379];
18. b) A. Bhattacharya, B. Segmuller, A. Ybarra, Synth. Commun. 1996, 26, 1775-1784.
19. J. Behrens, M. M. Mareel, E. M. Van Roy, W. Birchmeier, J. Cell Biol. 1989, 108, 2435-2447.
20. H. Shimizu, M. A. Julius, M. Giarre, Z. Zheng, A. M. Brown, J. Kitajewski, Cell Growth Differ 1997, 8, 1349-1358.
21. I. M. Karaguni, K. H. Glusenkamp, A. Langerak, C. Geisen, V. Ullrich, G. Winde, T. Möröy, O. Müller, Bioorg. Med. Chem. Lett. 2002, 12, 709-713.
22. F. Denizot, R. Lang, J. Immunol. Methods 1986, 89, 271-277.
23. S. J. Martin, C. P. Reutelingsperger, A. J. McGahon, J. A. Rader, R. C. van Schie, D. M. LaFace, D. R. Green, J. Exp. Med. 1995, 182, 1545-1556.
24. M. van Engeland, L. J. Nieland, F. C. Ramaekers, B. Schutte, C. P. Reutelingsperger, Cytometry 1998, 31, 1-9.
25. H. Waldmann, I. M. Karaguni, M. Carpintero, E. Gourzoulidou, C. Herrmann, C. Brockmann, H. Oschkinat, O. Müller, Angew. Chem. 2004, 116, 460; Angew. Chem. Int. Ed. 2004, 43, 454 (following article in this issue).
26. H. Waldmann, I. M. Karaguni, M. Carpintero, E. Gourzoulidou, C. Herrmann, C. Brockmann, H. Oschkinat, O. Müller, Angew. Chem. 2004, 116, 460; Angew. Chem. Int. Ed. 2004, 43, 454 (following article in this issue).
27. H. Waldmann, O. Müller, unpublished results.