Small molecule probes of cellular pathways and networks

ACS Chemical Biology

Volumn 6, Issue 1, 2011, Pages 86-94

  Castoreno, Adam B ^a   Eggert, Ulrike S ^a  

^a HARVARD MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALYCULIN A; CAMPTOTHECIN; CANTHARIDIN; DAUNORUBICIN; DOXORUBICIN; ECHINOMYCIN; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; IMATINIB; METHOTREXATE; MITOXANTRONE; SMALL MOLECULE TRANSPORT AGENT; STEROL; TAMOXIFEN;

BIOSYNTHESIS; CALCIUM HOMEOSTASIS; CANCER CELL; CELL FUNCTION; CELL MEMBRANE PERMEABILITY; ENZYME ACTIVITY; GENE EXPRESSION PROFILING; GENE MUTATION; HUMAN; MOLECULAR LIBRARY; NONHUMAN; PHENOTYPE; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN TARGETING; REGULATORY MECHANISM; REVIEW; SIGNAL TRANSDUCTION; VIRUS REPLICATION;

DRUG DELIVERY SYSTEMS; MOLECULAR PROBES; PROTEOME; RNA INTERFERENCE; SIGNAL TRANSDUCTION; SMALL MOLECULE LIBRARIES;

EID: 79251503920     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb1002976     Document Type: Review

References (39)

1. Peterson, J. R. and Mitchison, T. J. (2002) Small molecules, big impact: a history of chemical inhibitors and the cytoskeleton Chem. Biol. 9, 1275-1285
2. Spudich, J. A. and Lin, S. (1972) Cytochalasin B, its interaction with actin and actomyosin from muscle (cell movement-microfilaments-rabbit striated muscle) Proc. Natl. Acad. Sci. U.S.A. 69, 442-446
3. Eggert, U. S. and Mitchison, T. J. (2006) Small molecule screening by imaging Curr. Opin. Chem. Biol. 10, 232-237
4. Kamijo, K., Ohara, N., Abe, M., Uchimura, T., Hosoya, H., Lee, J. S., and Miki, T. (2006) Dissecting the role of Rho-mediated signaling in contractile ring formation Mol. Biol. Cell 17, 43-55
5. Young, K., Jayasuriya, H., Ondeyka, J. G., Herath, K., Zhang, C., Kodali, S., Galgoci, A., Painter, R., Brown-Driver, V., Yamamoto, R., Silver, L. L., Zheng, Y., Ventura, J. I., Sigmund, J., Ha, S., Basilio, A., Vicente, F., Tormo, J. R., Pelaez, F., Youngman, P., Cully, D., Barrett, J. F., Schmatz, D., Singh, S. B., and Wang, J. (2006) Discovery of FabH/FabF inhibitors from natural products Antimicrob. Agents Chemother. 50, 519-526
6. Wang, J., Soisson, S. M., Young, K., Shoop, W., Kodali, S., Galgoci, A., Painter, R., Parthasarathy, G., Tang, Y. S., Cummings, R., Ha, S., Dorso, K., Motyl, M., Jayasuriya, H., Ondeyka, J., Herath, K., Zhang, C., Hernandez, L., Allocco, J., Basilio, A., Tormo, J. R., Genilloud, O., Vicente, F., Pelaez, F., Colwell, L., Lee, S. H., Michael, B., Felcetto, T., Gill, C., Silver, L. L., Hermes, J. D., Bartizal, K., Barrett, J., Schmatz, D., Becker, J. W., Cully, D., and Singh, S. B. (2006) Platensimycin is a selective FabF inhibitor with potent antibiotic properties Nature 441, 358-361
7. Castoreno, A. B., Smurnyy, Y., Torres, A. D., Vokes, M. S., Jones, T. R., Carpenter, A. E., and Eggert, U. S. (2010) Small molecules discovered in a pathway screen target the Rho pathway in cytokinesis Nat. Chem. Biol. 6, 457-463
8. Sprang, S. R. (1997) G protein mechanisms: insights from structural analysis Annu. Rev. Biochem. 66, 639-678
9. Zhou, Q., Kee, Y. S., Poirier, C. C., Jelinek, C., Osborne, J., Divi, S., Surcel, A., Will, M. E., Eggert, U. S., Muller-Taubenberger, A., Iglesias, P. A., Cotter, R. J., and Robinson, D. N. (2010) 14-3-3 coordinates microtubules, Rac, and myosin II to control cell mechanics and cytokinesis Curr. Biol. 20, 1881-1889
10. Lum, P. Y., Armour, C. D., Stepaniants, S. B., Cavet, G., Wolf, M. K., Butler, J. S., Hinshaw, J. C., Garnier, P., Prestwich, G. D., Leonardson, A., Garrett-Engele, P., Rush, C. M., Bard, M., Schimmack, G., Phillips, J. W., Roberts, C. J., and Shoemaker, D. D. (2004) Discovering modes of action for therapeutic compounds using a genome-wide screen of yeast heterozygotes Cell 116, 121-137
11. Giaever, G., Flaherty, P., Kumm, J., Proctor, M., Nislow, C., Jaramillo, D. F., Chu, A. M., Jordan, M. I., Arkin, A. P., and Davis, R. W. (2004) Chemogenomic profiling: identifying the functional interactions of small molecules in yeast Proc. Natl. Acad. Sci. U.S.A. 101, 793-798
12. Baetz, K., McHardy, L., Gable, K., Tarling, T., Reberioux, D., Bryan, J., Andersen, R. J., Dunn, T., Hieter, P., and Roberge, M. (2004) Yeast genome-wide drug-induced haploinsufficiency screen to determine drug mode of action Proc. Natl. Acad. Sci. U.S.A. 101, 4525-4530
13. Lee, W., St Onge, R. P., Proctor, M., Flaherty, P., Jordan, M. I., Arkin, A. P., Davis, R. W., Nislow, C., and Giaever, G. (2005) Genome-wide requirements for resistance to functionally distinct DNA-damaging agents PLoS Genet 1 e24
14. Parsons, A. B., Lopez, A., Givoni, I. E., Williams, D. E., Gray, C. A., Porter, J., Chua, G., Sopko, R., Brost, R. L., Ho, C. H., Wang, J., Ketela, T., Brenner, C., Brill, J. A., Fernandez, G. E., Lorenz, T. C., Payne, G. S., Ishihara, S., Ohya, Y., Andrews, B., Hughes, T. R., Frey, B. J., Graham, T. R., Andersen, R. J., and Boone, C. (2006) Exploring the mode-of-action of bioactive compounds by chemical-genetic profiling in yeast Cell 126, 611-625
15. Butcher, R. A., Bhullar, B. S., Perlstein, E. O., Marsischky, G., LaBaer, J., and Schreiber, S. L. (2006) Microarray-based method for monitoring yeast overexpression strains reveals small-molecule targets in TOR pathway Nat. Chem. Biol. 2, 103-109
16. Hoon, S., Smith, A. M., Wallace, I. M., Suresh, S., Miranda, M., Fung, E., Proctor, M., Shokat, K. M., Zhang, C., Davis, R. W., Giaever, G., St Onge, R. P., and Nislow, C. (2008) An integrated platform of genomic assays reveals small-molecule bioactivities Nat. Chem. Biol. 4, 498-506
17. Lehar, J., Stockwell, B. R., Giaever, G., and Nislow, C. (2008) Combination chemical genetics Nat. Chem. Biol. 4, 674-681
18. Owens, C. M., Mawhinney, C., Grenier, J. M., Altmeyer, R., Lee, M. S., Borisy, A. A., Lehar, J., and Johansen, L. M. (2010) Chemical combinations elucidate pathway interactions and regulation relevant to Hepatitis C replication Mol. Syst. Biol. 6, 375
19. Huang, S. M., Mishina, Y. M., Liu, S., Cheung, A., Stegmeier, F., Michaud, G. A., Charlat, O., Wiellette, E., Zhang, Y., Wiessner, S., Hild, M., Shi, X., Wilson, C. J., Mickanin, C., Myer, V., Fazal, A., Tomlinson, R., Serluca, F., Shao, W., Cheng, H., Shultz, M., Rau, C., Schirle, M., Schlegl, J., Ghidelli, S., Fawell, S., Lu, C., Curtis, D., Kirschner, M. W., Lengauer, C., Finan, P. M., Tallarico, J. A., Bouwmeester, T., Porter, J. A., Bauer, A., and Cong, F. (2009) Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling Nature 461, 614-620
20. Ewan, K., Pajak, B., Stubbs, M., Todd, H., Barbeau, O., Quevedo, C., Botfield, H., Young, R., Ruddle, R., Samuel, L., Battersby, A., Raynaud, F., Allen, N., Wilson, S., Latinkic, B., Workman, P., McDonald, E., Blagg, J., Aherne, W., and Dale, T. (2010) A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription Cancer Res. 70, 5963-5973
21. Hoffman, G. R., Moerke, N. J., Hsia, M., Shamu, C. E., and Blenis, J. (2010) A high-throughput, cell-based screening method for siRNA and small molecule inhibitors of mTORC1 signaling using the In Cell Western technique Assay Drug Dev. Technol. 8, 186-199
22. Eggert, U. S., Kiger, A. A., Richter, C., Perlman, Z. E., Perrimon, N., Mitchison, T. J., and Field, C. M. (2004) Parallel chemical genetic and genome-wide RNAi screens identify cytokinesis inhibitors and targets PLoS Biol. 2 e379
23. Hughes, T. R., Marton, M. J., Jones, A. R., Roberts, C. J., Stoughton, R., Armour, C. D., Bennett, H. A., Coffey, E., Dai, H., He, Y. D., Kidd, M. J., King, A. M., Meyer, M. R., Slade, D., Lum, P. Y., Stepaniants, S. B., Shoemaker, D. D., Gachotte, D., Chakraburtty, K., Simon, J., Bard, M., and Friend, S. H. (2000) Functional discovery via a compendium of expression profiles Cell 102, 109-126
24. Lamb, J., Crawford, E. D., Peck, D., Modell, J. W., Blat, I. C., Wrobel, M. J., Lerner, J., Brunet, J. P., Subramanian, A., Ross, K. N., Reich, M., Hieronymus, H., Wei, G., Armstrong, S. A., Haggarty, S. J., Clemons, P. A., Wei, R., Carr, S. A., Lander, E. S., and Golub, T. R. (2006) The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease Science 313, 1929-1935
25. Perlman, Z. E., Slack, M. D., Feng, Y., Mitchison, T. J., Wu, L. F., and Altschuler, S. J. (2004) Multidimensional drug profiling by automated microscopy Science 306, 1194-1198
26. Tanaka, M., Bateman, R., Rauh, D., Vaisberg, E., Ramachandani, S., Zhang, C., Hansen, K. C., Burlingame, A. L., Trautman, J. K., Shokat, K. M., and Adams, C. L. (2005) An unbiased cell morphology-based screen for new, biologically active small molecules PLoS Biol. 3 e128
27. MacDonald, M. L., Lamerdin, J., Owens, S., Keon, B. H., Bilter, G. K., Shang, Z., Huang, Z., Yu, H., Dias, J., Minami, T., Michnick, S. W., and Westwick, J. K. (2006) Identifying off-target effects and hidden phenotypes of drugs in human cells Nat. Chem. Biol. 2, 329-337
28. Westwick, J. K. and Michnick, S. W. (2006) Protein-fragment complementation assays (PCA) in small GTPase research and drug discovery Methods Enzymol. 407, 388-401
29. Dolma, S., Lessnick, S. L., Hahn, W. C., and Stockwell, B. R. (2003) Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells Cancer Cell 3, 285-296
30. Gupta, P. B., Onder, T. T., Jiang, G., Tao, K., Kuperwasser, C., Weinberg, R. A., and Lander, E. S. (2009) Identification of selective inhibitors of cancer stem cells by high-throughput screening Cell 138, 645-659
31. Adrian, F. J., Ding, Q., Sim, T., Velentza, A., Sloan, C., Liu, Y., Zhang, G., Hur, W., Ding, S., Manley, P., Mestan, J., Fabbro, D., and Gray, N. S. (2006) Allosteric inhibitors of Bcr-abl-dependent cell proliferation Nat. Chem. Biol. 2, 95-102
32. Zhang, J., Adrian, F. J., Jahnke, W., Cowan-Jacob, S. W., Li, A. G., Iacob, R. E., Sim, T., Powers, J., Dierks, C., Sun, F., Guo, G. R., Ding, Q., Okram, B., Choi, Y., Wojciechowski, A., Deng, X., Liu, G., Fendrich, G., Strauss, A., Vajpai, N., Grzesiek, S., Tuntland, T., Liu, Y., Bursulaya, B., Azam, M., Manley, P. W., Engen, J. R., Daley, G. Q., Warmuth, M., and Gray, N. S. (2010) Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors Nature 463, 501-506
33. Eggert, U. S., Field, C. M., and Mitchison, T. J. (2006) Small molecules in an RNAi world Mol. BioSyst. 2, 93-96
34. Kwok, T. C., Ricker, N., Fraser, R., Chan, A. W., Burns, A., Stanley, E. F., McCourt, P., Cutler, S. R., and Roy, P. J. (2006) A small-molecule screen in C. elegans yields a new calcium channel antagonist Nature 441, 91-95
35. Petrascheck, M., Ye, X., and Buck, L. B. (2007) An antidepressant that extends lifespan in adult Caenorhabditis elegans Nature 450, 553-556
36. Burns, A. R., Wallace, I. M., Wildenhain, J., Tyers, M., Giaever, G., Bader, G. D., Nislow, C., Cutler, S. R., and Roy, P. J. (2010) A predictive model for drug bioaccumulation and bioactivity in Caenorhabditis elegans Nat. Chem. Biol. 6, 549-557
37. Peterson, R. T., Shaw, S. Y., Peterson, T. A., Milan, D. J., Zhong, T. P., Schreiber, S. L., MacRae, C. A., and Fishman, M. C. (2004) Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation Nat. Biotechnol. 22, 595-599
38. Mathew, L. K., Sengupta, S., Kawakami, A., Andreasen, E. A., Lohr, C. V., Loynes, C. A., Renshaw, S. A., Peterson, R. T., and Tanguay, R. L. (2007) Unraveling tissue regeneration pathways using chemical genetics J. Biol. Chem. 282, 35202-35210
39. Rihel, J., Prober, D. A., Arvanites, A., Lam, K., Zimmerman, S., Jang, S., Haggarty, S. J., Kokel, D., Rubin, L. L., Peterson, R. T., and Schier, A. F. (2010) Zebrafish behavioral profiling links drugs to biological targets and rest/wake regulation Science 327, 348-351