Bypassing a Kinase Activity with an ATP-Competitive Drug

Science

Volumn 302, Issue 5650, 2003, Pages 1533-1537

  Papa, Feroz R ^a   Zhang, Chao ^a   Shokat, Kevan ^a   Waiter, Peter ^a,b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINETRIPHOSPHATE; CELL MEMBRANES; DRUG PRODUCTS; MUTAGENESIS; RNA;

ENDOPLASMIC RETICULUM; PHOSPHORYLATION; UNFOLDED PROTEIN RESPONSE (UPR);

ENZYMES;

1 TERT BUTYL 3 NAPHTHALEN 1 YLMETHYL 1H PYRAZOLO[3,4 D]PYRIMIDIN 4 YLEMINE; ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; DITHIOTHREITOL; ENZYME INHIBITOR; IRE1 KINASE; MESSENGER RNA; NAPHTHYL GROUP; PHOSPHOTRANSFERASE; PHOSPHOTRANSFERASE INHIBITOR; TRANSFER RNA; TUNICAMYCIN; UNCLASSIFIED DRUG;

BIOLOGY; DRUG DEVELOPMENT; PROTEIN;

ARTICLE; AUTOPHOSPHORYLATION; BINDING SITE; CONFORMATIONAL TRANSITION; DRUG SENSITIZATION; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INHIBITION; ESCHERICHIA COLI; PHOSPHORYLATION; PRIORITY JOURNAL; PROTEIN FOLDING; RNA SPLICING; SITE DIRECTED MUTAGENESIS; YEAST;

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; BASIC-LEUCINE ZIPPER TRANSCRIPTION FACTORS; BINDING SITES; BINDING, COMPETITIVE; CYTOSOL; DITHIOTHREITOL; ENDOPLASMIC RETICULUM; ENDORIBONUCLEASES; ENZYME ACTIVATION; LIGANDS; MEMBRANE GLYCOPROTEINS; MODELS, BIOLOGICAL; MUTAGENESIS, SITE-DIRECTED; PHOSPHORYLATION; PROTEIN CONFORMATION; PROTEIN FOLDING; PROTEIN STRUCTURE, TERTIARY; PROTEIN-SERINE-THREONINE KINASES; PYRAZOLES; PYRIMIDINES; REPRESSOR PROTEINS; RNA SPLICING; RNA, MESSENGER; SACCHAROMYCES CEREVISIAE PROTEINS; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TRANSCRIPTION FACTORS; UP-REGULATION;

ESCHERICHIA COLI;

EID: 0344395603     PISSN: 00368075     EISSN: None     Source Type: Journal    
DOI: 10.1126/science.1090031     Document Type: Article

References (33)

1. M. J. Gething, J. Sambrook, Nature 355, 33 (1992).
2. F. J. Stevens, Y. Argon, Semin. Cell Dev. Biol. 10, 443 (1999).
3. C. Patil, P. Walter, Curt. Opin. Cell Biol. 13, 349 (2001).
4. J. S. Cox, C. E. Shamu, P. Walter, Cell 73, 1197 (1993).
5. J. S. Cox, P. Walter, Cell 87, 391 (1996).
6. U. Ruegsegger, J. H. Leber, P. Walter, Cell 107, 103 (2001).
7. C. Sidrauski, P. Walter, Cell 90, 1031 (1997).
8. C. Sidrauski, J. S. Cox, P. Walter, Cell 87, 405 (1996).
9. C. E. Shamu, P. Walter, EMBO J. 15, 3028 (1996).
10. A. Weiss, J. Schlessinger, Cell 94, 277 (1998).
11. K. Mori, W. Ma, M. J. Gething, J. Sambrook, Cell 74, 743 (1993).
12. K. Shah, Y. Liu, C. Deirmengian, K. M. Shokat, Proc. Natl. Acad. Sci. U.S.A. 94, 3565 (1997).
13. A. C. Bishop et al., Curr. Biol. 8, 257 (1998).
14. E. L. Weiss, A. C. Bishop, K. M. Shokat, D. G. Drubin, Nature Cell Biol. 2, 677 (2000).
15. A. C. Bishop et al., Nature 407, 395 (2000).
16. Single-letter abbreviations for the amino acid residues are as follows: A, Ala; D, Asp; G, Gly; L, Leu; and S, Ser.
17. A. S. Carroll, A. C. Bishop, J. L. DeRisi, K. M. Shokat, E. K. O'Shea, Proc. Natl. Acad. Sci. U.S.A. 98, 12578 (2001).
18. F. R. Papa, C. Zhang, K. Shokat, P. Walter, data not shown.
19. M. Huse, J. Kuriyan, Cell 109, 275 (2002).
20. J. L. DeRisi, V. R. Iyer, P. O. Brown, Science 278, 680 (1997).
21. K. J. Travers et al., Cell 101, 249 (2000).
22. Materials and methods are available as supporting material on Science Online.
23. F. Urano, A. Bertolotti, D. Ron, J. Cell Sci. 113, 3697 (2000).
24. S. R. Hubbard, M. Mohammadi, J. Schlessinger, J. Biol. Chem. 273, 11987 (1998).
25. T. Schindler et al., Mol. Cell 3, 639 (1999).
26. M. Porter, T. Schindler, J. Kuriyan, W. T. Miller, J. Biol. Chem. 275, 2721 (2000).
27. F. Schuit, K. Moens, H. Heimberg, D. Pipeleers, J. Biol. Chem. 274, 32803 (1999).
28. R. J. Kaufman et al., Nature Rev. Mol. Cell Biol. 3, 411 (2002).
29. B. Dong, M. Niwa, P. Walter, R. H. Silverman, RNA 7, 361 (2001).
30. S. Naik, J. M. Paranjape, R. H. Silverman, Nucleic Acids Res. 26, 1522 (1998).
31. B. Dong, R. H. Silverman, Nucleic Acids 27, 439 (1999).
32. M. Kroiher, M. A. Miller, R. E. Steele, Bioessays 23, 69 (2001).
33. C allele, S. Ullrich for his initial effort in constructing Ire1 mutants, and J. Kuriyan and members of the Walter and Shokat labs for valuable discussions. Supported by grants from the NIH to P.W. (GM32384) and K.S. (AI44009), and postdoctoral support from the UCSF Molecular Medicine Program (to F.P.). P.W. receives support as an investigator of the Howard Hughes Medical Institute.