Identification of TRIO-GEFD1 chemical inhibitors using the yeast exchange assay

Biology of the Cell

Volumn 98, Issue 9, 2006, Pages 511-522

  Blangy, Anne ^a   Bouquier, Nathalie ^a   Gauthier Rouvière, Cécile ^a   Schmidt, Susanne ^a   Debant, Anne ^a   Leonetti, Jean Paul ^a   Fort, Philippe ^a  

^a CNRS   (France)

Author keywords

Guanine nucleotide exchange factor; Mutant; Rho GTPase; RhoG; Screen

Indexed keywords

1 (3 NITROPHENYL) 1H PYRROLE 2,5 DIONE; 1,1' (1,2 PHENYLENE)BIS(1H PYRROLE 2,5 DIONE); 1,1' (2 CHLORO 1,4 PHENYLENE)BIS(1H PYRROLE 2,5 DIONE); ADENOSINE DIPHOSPHATE RIBOSYLATION FACTOR; ADENOSINE DIPHOSPHATE RIBOSYLATION FACTOR 1; ADENOSINE DIPHOSPHATE RIBOSYLATION FACTOR NUCLEOTIDE BINDING SITE OPENER; ANTINEOPLASTIC AGENT; GUANINE NUCLEOTIDE EXCHANGE FACTOR; PEPTIDE LIBRARY; PYRROLE DERIVATIVE; RHO GUANINE NUCLEOTIDE BINDING PROTEIN; RHO GUANOSINE TRIPHOSPHATASE GUANINE NUCLEOTIDE EXCHANGE FACTOR; RHO GUANOSINE TRIPHOSPHATASE GUANINE NUCLEOTIDE EXCHANGE FACTOR INHIBITOR; RHOA GUANINE NUCLEOTIDE BINDING PROTEIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CARCINOGENESIS; CATALYSIS; CONTROLLED STUDY; DRUG BINDING; DRUG POTENCY; DRUG SCREENING; DRUG SPECIFICITY; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVATION; ENZYME REGULATION; HIGH THROUGHPUT SCREENING; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; NUCLEOTIDE BINDING SITE; PRIORITY JOURNAL; PROTO ONCOGENE; RAT; SIGNAL TRANSDUCTION; YEAST EXCHANGE ASSAY;

BIOLOGICAL ASSAY; CELL TRANSFORMATION, NEOPLASTIC; ENZYME INHIBITORS; GTPASE-ACTIVATING PROTEINS; GUANINE NUCLEOTIDE EXCHANGE FACTORS; HUMANS; MODELS, BIOLOGICAL; PHOSPHOPROTEINS; PROTEIN-SERINE-THREONINE KINASES; RHO GTP-BINDING PROTEINS; SACCHAROMYCES CEREVISIAE; SIGNAL TRANSDUCTION;

EID: 33748642768     PISSN: 02484900     EISSN: None     Source Type: Journal    
DOI: 10.1042/BC20060023     Document Type: Article

References (43)

1. Antonny, B., Beraud-Dufour, S., Chardin, P. and Chabre, M. (1997) N-terminal hydrophobic residues of the G-protein ADP-ribosylation factor-1 insert into membrane phospholipids upon GDP to GTP exchange. Biochemistry (Moscow) 36, 4675-4684
2. Aznar, S. and Lacal, J.C. (2001) Searching new targets for anticancer drug design: the families of Ras and Rho GTPases and their effectors. Prog. Nucleic Acid Res. Mol. Biol. 67, 193-234
3. 2+ and the beta-phosphate to destabilize GDP on ARF1. EMBO J. 17, 3651-3659
4. Blangy, A., Vignal, E., Schmidt, S., Debant, A., Gauthier-Rouviere, C. and Fort, P. (2000) TrioGEF1 controls Rac- and Cdc42-dependent cell structures through the direct activation of rhoG. J. Cell Sci. 113, 729-739
5. Chardin, P. and McCormick, F. (1999) Brefeldin A: the advantage of being uncompetitive. Cell 97, 153-155
6. Cherfils, J. (2001) Structural mimicry of DH domains by Arfaptin suggests a model for the recognition of Rac-GDP by its guanine nucleotide exchange factors. FEBS Lett. 507, 280-284
7. Czuchra, A., Wu, X., Meyer, H., van Hengel, J., Schroeder, T., Geffers, R., Rottner, K. and Brakebusch, C. (2005) Cdc42 is not essential for filopodium formation, directed migration, cell polarization, and mitosis in fibroblastoid cells. Mol. Biol. Cell 16, 4473-4484
8. Dadgostar, H., Doyle, S.E., Shahangian, A., Garcia, D.E. and Cheng, G. (2003) T3JAM, a novel protein that specifically interacts with TRAF3 and promotes the activation of JNK(1). FEBS Lett. 553, 403-407
9. De Toledo, M., Colombo, K., Nagase, T., Ohara, O., Fort, P. and Blangy, A. (2000) The yeast exchange assay, a new complementary method to screen for Dbl-like protein specificity: identification of a novel RhoA exchange factor. FEBS Lett. 480, 287-292
10. Erickson, J.W. and Cerione, R.A. (2004) Structural elements, mechanism, and evolutionary convergence of Rho protein-guanine nucleotide exchange factor complexes. Biochemistry (Moscow) 43, 837-842
11. Etienne-Manneville, S. and Hall, A. (2002) Rho GTPases in cell biology. Nature (London) 420, 629-635
12. Farnsworth, C. L. and Feig, L.A. (1991) Dominant inhibitory mutations in the Mg(2+)-binding site of RasH prevent its activation by GTP. Mol. Cell. Biol. 11, 4822-4829
13. Feig, L.A. and Cooper, G.M. (1988a) Inhibition of NIH 3T3 cell proliferation by a mutant ras protein with preferential affinity for GDP. Mol. Cell. Biol. 8, 3235-3243
14. Feig, L.A. and Cooper, G. M. (1988b) Relationship among guanine nucleotide exchange, GTP hydrolysis, and transforming potential of mutated ras proteins. Mol. Cell. Biol. 8, 2472-2478
15. Gao, Y., Xing, J., Streuli, M., Leto, T.L. and Zheng, Y. (2001) Trp(56) of rac1 specifies interaction with a subset of guanine nucleotide exchange factors. J. Biol. Chem. 276, 47530-47541
16. Gao, Y., Dickerson, J.B., Guo, F., Zheng, J. and Zheng, Y. (2004) Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc. Natl. Acad. Sci. U.S.A. 101, 7618-7623
17. Hemsath, L. and Ahmadian, M.R. (2005) Fluorescence approaches for monitoring interactions of Rho GTPases with nucleotides, regulators, and effectors. Methods 37, 173-182
18. Kane, S., Sano, H., Liu, S.C., Asara, J.M., Lane, W.S., Garner, C.C. and Lienhard, G.E. (2002) A method to identify serine kinase substrates. Akt phosphorylates a novel adipocyte protein with a Rab GTPase-activating protein (GAP) domain. J. Biol. Chem. 277, 22115-22118
19. Kanekura, K., Hashimoto, Y., Niikura, T., Aiso, S., Matsuoka, M. and Nishimoto, I. (2004) Alsin, the product of ALS2 gene, suppresses SOD1 mutant neurotoxicity through RhoGEF domain by interacting with SOD1 mutants. J. Biol. Chem. 279, 19247-19256
20. Karnoub, A.E., Symons, M., Campbell, S.L. and Der, C.J. (2004) Molecular basis for Rho GTPase signaling specificity. Breast Cancer Res. Treat. 84, 61-71
21. Larance, M., Ramm, G., Stockli, J., van Dam, E.M., Winata, S., Wasinger, V., Simpson, F., Graham, M., Junutula, J.R., Guilhaus, M. and James, D.E. (2005) Characterization of the role of the Rab GTPase-activating protein AS160 in insulin-regulated GLUT4 trafficking. J. Biol. Chem. 280, 37803-37813
22. Lee, S.H., Eom, M., Lee, S.J., Kim, S., Park, H.J. and Park, D. (2001) BetaPix-enhanced p38 activation by Cdc42/Rac/PAK/MKK3/6-mediated pathway. Implication in the regulation of membrane ruffling. J. Biol. Chem. 276, 25066-25072
23. Li, R. and Zheng, Y. (1997) Residues of the Rho family GTPases Rho and Cdc42 that specify sensitivity to Dbl-like guanine nucleotide exchange factors. J. Biol. Chem. 272, 4671-4679
24. Li, R., Zhang, B. and Zheng, Y. (1997) Structural determinants required for the interaction between Rho GTPase and the GTPase-activating domain of p190. J. Biol. Chem. 272, 32830-32835
25. Meller, N., Merlot, S. and Guda, C. (2005) CZH proteins: a new family of Rho-GEFs. J. Cell Sci. 118, 4937-4946
26. Michiels, F., Habets, G.G., Stam, J.C., van der Kammen, R.A. and Collard, J.G. (1995) A role for Rac in Tiam1-induced membrane ruffling and invasion. Nature (London) 375, 338-340
27. Orrico, A., Galli, L., Cavaliere, M.L., Garavelli, L., Fryns, J.P., Crushell, E., Rinaldi, M.M., Medeira, A. and Sorrentino, V. (2004) Phenotypic and molecular characterisation of the Aarskog-Scott syndrome: a survey of the clinical variability in light of FGD1 mutation analysis in 46 patients. Eur. J. Hum. Genet. 12, 16-23
28. Ramirez De Molina, A., Rodriguez-Gonzalez, A. and Lacal, J.C. (2001) Targeting new anticancer drugs within signalling pathways regulated by the Ras GTPase superfamily [review]. Int. J. Oncol. 19, 5-17
29. Ridley, A.J. (2004) Rho proteins and cancer. Breast Cancer Res. Treat. 84, 13-19
30. Ron, D., Tronick, S.R., Aaronson, S.A. and Eva, A. (1988) Molecular cloning and characterization of the human dbl proto-oncogene: evidence that its overexpression is sufficient to transform NIH/3T3 cells. EMBO J. 7, 2465-2473
31. Rossman, K.L., Cheng, L., Mahon, G.M., Rojas, R.J., Snyder, J.T., Whitehead, I.P. and Sondek, J. (2003) Multifunctional roles for the PH domain of Dbs in regulating Rho GTPase activation. J. Biol. Chem. 278, 18393-18400
32. Rossman, K.L., Der, C.J. and Sondek, J. (2005) GEF means go: turning on Rho GTPases with guanine nucleotide-exchange factors. Nat. Rev. Mol. Cell Biol. 6, 167-180
33. Sahai, E. and Marshall, C.J. (2002) Rho-GTPases and cancer. Nat. Rev. Cancer 2, 133-142
34. Schmidt, S., Diriong, S., Mery, J., Fabbrizio, E. and Debant, A. (2002) Identification of the first Rho-GEF inhibitor, TRIPalpha, which targets the RhoA-specific GEF domain of Trio. FEBS Lett. 523, 35-42
35. Shah, N. and Klausner, R.D. (1993) Brefeldin A reversibly inhibits secretion in Saccharomyces cerevisiae. J. Biol. Chem. 268, 5345-5348
36. Stacey, D.W., Feig, L.A. and Gibbs, J.B. (1991) Dominant inhibitory Ras mutants selectively inhibit the activity of either cellular or oncogenic Ras. Mol. Cell. Biol. 11, 4053-4064
37. Tu, S.S., Wu, W.J., Yang, W., Nolbant, P., Hahn, K. and Cerione, R.A. (2002) Antiapoptotic Cdc42 mutants are potent activators of cellular transformation. Biochemistry 41, 12350-12358
38. Vidal, M. and Endoh, H. (1999) Prospects for drug screening using the reverse two-hybrid system. Trends Biotechnol. 17, 374-381
39. Vignal, E., Blangy, A., Martin, M., Gauthier-Rouviere, C. and Fort, P. (2001) Kinectin is a key effector of RhoG microtubule-dependent cellular activity. Mol. Cell. Biol. 21, 8022-8034
40. Vigorito, E., Bell, S., Hebeis, B.J., Reynolds, H., McAdam, S., Emson, P.C., McKenzie, A. and Turner, M. (2004) Immunological function in mice lacking the Rac-related GTPase RhoG. Mol. Cell. Biol. 24, 719-729
41. Vogel, J.P., Lee, J.N., Kirsch, D.R., Rose, M.D. and Sztul, E.S. (1993) Brefeldin A causes a defect in secretion in Saccharomyces cerevisiae. J. Biol. Chem. 268, 3040-3043
42. Wang, L., Zhu, K. and Zheng, Y. (2004) Oncogenic Dbl, Cdc42, and p21-activated kinase form a ternary signaling intermediate through the minimum interactive domains. Biochemistry (Moscow) 43, 14584-14593
43. Zheng, Y. (2001) Dbl family guanine nucleotide exchange factors. Trends Biochem. Sci. 26, 724-732