Importazole, a small molecule inhibitor of the transport receptor importin-β

ACS Chemical Biology

Volumn 6, Issue 7, 2011, Pages 700-708

  Soderholm, Jonathan F ^a,e   Bird, Stephen L ^a   Kalab, Petr ^a,b   Sampathkumar, Yasaswini ^a   Hasegawa, Keisuke ^b   Uehara Bingen, Michael ^c,d   Weis, Karsten ^a   Heald, Rebecca ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b NATIONAL CANCER INSTITUTE   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d Yonsei University   (South Korea)

^e Yowza Software   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 DIAMINOQUINAZOLINE DERIVATIVE; IMPORTAZOLE; KARYOPHERIN BETA; UNCLASSIFIED DRUG;

ARTICLE; CELL CYCLE; CONTROLLED STUDY; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMAN; HUMAN CELL; MITOSIS; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PURIFICATION; SPINDLE CELL;

ACTIVE TRANSPORT, CELL NUCLEUS; ANIMALS; BETA KARYOPHERINS; CELL EXTRACTS; FEMALE; FLUORESCENCE RESONANCE ENERGY TRANSFER; GTPASE-ACTIVATING PROTEINS; HELA CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; KARYOPHERINS; MITOSIS; MITOTIC SPINDLE APPARATUS; NFATC TRANSCRIPTION FACTORS; OVUM; QUINAZOLINES; RAN GTP-BINDING PROTEIN; RECEPTORS, CYTOPLASMIC AND NUCLEAR; SIGNAL TRANSDUCTION; XENOPUS;

EID: 79959692369     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb2000296     Document Type: Article

References (43)

1. Strom, A. C. and Weis, K. (2001) Importin-beta-like nuclear transport receptors Genome Biol 2, REVIEWS3008
2. Harel, A. and Forbes, D. J. (2004) Importin beta: conducting a much larger cellular symphony Mol. Cell 16, 319-330 (Pubitemid 39504787)
3. Gruss, O. J., Carazo-Salas, R. E., Schatz, C. A., Guarguaglini, G., Kast, J., Wilm, M., Le Bot, N., Vernos, I., Karsenti, E., and Mattaj, I. W. (2001) Ran induces spindle assembly by reversing the inhibitory effect of importin alpha on TPX2 activity Cell 104, 83-93 (Pubitemid 32144974)
4. Nachury, M. V., Maresca, T. J., Salmon, W. C., Waterman-Storer, C. M., Heald, R., and Weis, K. (2001) Importin beta is a mitotic target of the small GTPase Ran in spindle assembly Cell 104, 95-106 (Pubitemid 32144975)
5. Wiese, C., Wilde, A., Moore, M. S., Adam, S. A., Merdes, A., and Zheng, Y. (2001) Role of importin-beta in coupling Ran to downstream targets in microtubule assembly Science 291, 653-656 (Pubitemid 32150424)
6. Kalab, P., Weis, K., and Heald, R. (2002) Visualization of a Ran-GTP gradient in interphase and mitotic Xenopus egg extracts Science 295, 2452-2456 (Pubitemid 34270259)
7. Kalab, P., Pralle, A., Isacoff, E. Y., Heald, R., and Weis, K. (2006) Analysis of a RanGTP-regulated gradient in mitotic somatic cells Nature 440, 697-701
8. Harel, A., Chan, R. C., Lachish-Zalait, A., Zimmerman, E., Elbaum, M., and Forbes, D. J. (2003) Importin beta negatively regulates nuclear membrane fusion and nuclear pore complex assembly Mol. Biol. Cell 14, 4387-4396 (Pubitemid 37444642)
9. Walther, T. C., Askjaer, P., Gentzel, M., Habermann, A., Griffiths, G., Wilm, M., Mattaj, I. W., and Hetzer, M. (2003) RanGTP mediates nuclear pore complex assembly Nature 424, 689-694 (Pubitemid 36987995)
10. Ryan, K. J., Zhou, Y., and Wente, S. R. (2007) The karyopherin Kap95 regulates nuclear pore complex assembly into intact nuclear envelopes in vivo Mol. Biol. Cell 18, 886-898
11. Song, L. and Rape, M. (2010) Regulated degradation of spindle assembly factors by the anaphase-promoting complex Mol. Cell 38, 369-382
12. Dishinger, J. F., Kee, H. L., Jenkins, P. M., Fan, S., Hurd, T. W., Hammond, J. W., Truong, Y. N., Margolis, B., Martens, J. R., and Verhey, K. J. (2010) Ciliary entry of the kinesin-2 motor KIF17 is regulated by importin-beta2 and RanGTP Nat. Cell Biol. 12, 703-710
13. Mayer, T. U., Kapoor, T. M., Haggarty, S. J., King, R. W., Schreiber, S. L., and Mitchison, T. J. (1999) Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen Science 286, 971-974
14. Sawin, K. E., LeGuellec, K., Philippe, M., and Mitchison, T. J. (1992) Mitotic spindle organization by a plus-end-directed microtubule motor Nature 359, 540-543
15. Blangy, A., Lane, H. A., d'Herin, P., Harper, M., Kress, M., and Nigg, E. A. (1995) Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo Cell 83, 1159-1169
16. Kapoor, T. M., Mayer, T. U., Coughlin, M. L., and Mitchison, T. J. (2000) Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5 J. Cell Biol. 150, 975-988
17. Khodjakov, A., Copenagle, L., Gordon, M. B., Compton, D. A., and Kapoor, T. M. (2003) Minus-end capture of preformed kinetochore fibers contributes to spindle morphogenesis J. Cell Biol. 160, 671-683 (Pubitemid 36298263)
18. Canman, J. C., Cameron, L. A., Maddox, P. S., Straight, A., Tirnauer, J. S., Mitchison, T. J., Fang, G., Kapoor, T. M., and Salmon, E. D. (2003) Determining the position of the cell division plane Nature 424, 1074-1078 (Pubitemid 37064310)
19. Ossareh-Nazari, B., Bachelerie, F., and Dargemont, C. (1997) Evidence for a role of CRM1 in signal-mediated nuclear protein export Science 278, 141-144 (Pubitemid 27446296)
20. Kosugi, S., Hasebe, M., Entani, T., Takayama, S., Tomita, M., and Yanagawa, H. (2008) Design of peptide inhibitors for the importin alpha/beta nuclear import pathway by activity-based profiling Chem. Biol. 15, 940-949
21. Ambrus, G., Whitby, L. R., Singer, E. L., Trott, O., Choi, E., Olson, A. J., Boger, D. L., and Gerace, L. (2010) Small molecule peptidomimetic inhibitors of importin alpha/beta mediated nuclear transport Bioorg. Med. Chem. 18, 7611-7620
22. Hintersteiner, M., Ambrus, G., Bednenko, J., Schmied, M., Knox, A. J., Meisner, N. C., Gstach, H., Seifert, J. M., Singer, E. L., Gerace, L., and Auer, M. (2010) Identification of a small molecule inhibitor of importin beta mediated nuclear import by confocal on-bead screening of tagged one-bead one-compound libraries ACS Chem. Biol. 5, 967-979
23. Zhang, J. H., Chung, T. D., and Oldenburg, K. R. (1999) A simple statistical parameter for use in evaluation and validation of high throughput screening assays J. Biomol. Screening 4, 67-73 (Pubitemid 29278954)
24. Feng, B. Y. and Shoichet, B. K. (2006) A detergent-based assay for the detection of promiscuous inhibitors Nat. Protoc. 1, 550-553
25. Floer, M. and Blobel, G. (1996) The nuclear transport factor karyopherin beta binds stoichiometrically to Ran-GTP and inhibits the Ran GTPase activating protein J. Biol. Chem. 271, 5313-5316 (Pubitemid 26083861)
26. Bischoff, F. R. and Gorlich, D. (1997) RanBP1 is crucial for the release of RanGTP from importin beta-related nuclear transport factors FEBS Lett. 419, 249-254 (Pubitemid 28010820)
27. Lee, S. J., Matsuura, Y., Liu, S. M., and Stewart, M. (2005) Structural basis for nuclear import complex dissociation by RanGTP Nature 435, 693-696 (Pubitemid 40825515)
28. Niesen, F. H., Berglund, H., and Vedadi, M. (2007) The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability Nat. Protoc. 2, 2212-2221 (Pubitemid 351565860)
29. Adam, S. A., Marr, R. S., and Gerace, L. (1990) Nuclear protein import in permeabilized mammalian cells requires soluble cytoplasmic factors J. Cell Biol. 111, 807-816
30. Gorlich, D., Pante, N., Kutay, U., Aebi, U., and Bischoff, F. R. (1996) Identification of different roles for RanGDP and RanGTP in nuclear protein import EMBO J. 15, 5584-5594 (Pubitemid 26385618)
31. Lowe, A. R., Siegel, J. J., Kalab, P., Siu, M., Weis, K., and Liphardt, J. T. (2010) Selectivity mechanism of the nuclear pore complex characterized by single cargo tracking Nature 467, 600-603
32. Pollard, V. W., Michael, W. M., Nakielny, S., Siomi, M. C., Wang, F., and Dreyfuss, G. (1996) A novel receptor-mediated nuclear protein import pathway Cell 86, 985-994 (Pubitemid 26336802)
33. Flanagan, W. M., Corthesy, B., Bram, R. J., and Crabtree, G. R. (1991) Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A Nature 352, 803-807 (Pubitemid 21912434)
34. Shibasaki, F., Price, E. R., Milan, D., and McKeon, F. (1996) Role of kinases and the phosphatase calcineurin in the nuclear shuttling of transcription factor NF-AT4 Nature 382, 370-373 (Pubitemid 26260467)
35. Kehlenbach, R. H., Dickmanns, A., and Gerace, L. (1998) Nucleocytoplasmic shuttling factors including Ran and CRM1 mediate nuclear export of NFAT In vitro J. Cell Biol. 141, 863-874 (Pubitemid 28243955)
36. Zhu, J. and McKeon, F. (1999) NF-AT activation requires suppression of Crm1-dependent export by calcineurin Nature 398, 256-260
37. Nishi, K., Yoshida, M., Fujiwara, D., Nishikawa, M., Horinouchi, S., and Beppu, T. (1994) Leptomycin B targets a regulatory cascade of crm1, a fission yeast nuclear protein, involved in control of higher order chromosome structure and gene expression J. Biol. Chem. 269, 6320-6324 (Pubitemid 24191000)
38. Chi, N. C., Adam, E. J., and Adam, S. A. (1997) Different binding domains for Ran-GTP and Ran-GDP/RanBP1 on nuclear import factor p97 J. Biol. Chem. 272, 6818-6822 (Pubitemid 27118172)
39. Xia, F., Lee, C. W., and Altieri, D. C. (2008) Tumor cell dependence on Ran-GTP-directed mitosis Cancer Res. 68, 1826-1833 (Pubitemid 351416568)
40. Azuma, Y., Seino, H., Seki, T., Uzawa, S., Klebe, C., Ohba, T., Wittinghofer, A., Hayashi, N., and Nishimoto, T. (1996) Conserved histidine residues of RCC1 are essential for nucleotide exchange on Ran J. Biochem. 120, 82-91 (Pubitemid 26258252)
41. Uniewicz, K. A., Ori, A., Xu, R., Ahmed, Y., Wilkinson, M. C., Fernig, D. G., and Yates, E. A. (2010) Differential scanning fluorimetry measurement of protein stability changes upon binding to glycosaminoglycans: a screening test for binding specificity Anal. Chem. 82, 3796-3802
42. Hannak, E. and Heald, R. (2006) Investigating mitotic spindle assembly and function in vitro using I egg extracts Nat. Protoc. 1, 2305-2314
43. Murakoshi, H., Lee, S. J., and Yasuda, R. (2008) Highly sensitive and quantitative FRET-FLIM imaging in single dendritic spines using improved non-radiative YFP Brain Cell Biol. 36, 31-42