Parsimonious discovery of synergistic drug combinations

ACS Chemical Biology

Volumn 6, Issue 12, 2011, Pages 1391-1398

  Severyn, Bryan ^a   Liehr, Robert A ^a   Wolicki, Alex ^a   Nguyen, Kevin H ^a   Hudak, Edward M ^a   Ferrer, Marc ^a   Caldwell, Jeremy S ^a   Hermes, Jeffrey D ^a   Li, Jing ^a   Tudor, Matthew ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA ADRENERGIC RECEPTOR STIMULATING AGENT; CYCLIC AMP; DACTOLISIB; DASATINIB; ERLOTINIB; ETOPOSIDE; INTERFERON; INTERLEUKIN 6; LIPOPOLYSACCHARIDE; N (2,3 DIHYDROXYPROPOXY) 3,4 DIFLUORO 2 (2 FLUORO 4 IODOANILINO)BENZAMIDE; OLAPARIB; PHOSPHODIESTERASE IV INHIBITOR; SORAFENIB; SUNITINIB; TANESPIMYCIN; TEMOZOLOMIDE;

ACUTE PHASE RESPONSE; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CELL VIABILITY ASSAY; DRUG COMBINATION; DRUG EFFICACY; DRUG POTENTIATION; DRUG SCREENING; DRUG TARGETING; HCT 116 CELL LINE; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; MONOCYTE; PRIORITY JOURNAL; THP-1 CELL LINE; CELL STRAIN HCT116; CELL SURVIVAL; COMBINATORIAL CHEMISTRY; DRUG ANTAGONISM; DRUG DEVELOPMENT; DRUG EFFECT; DRUG INTERACTION; GENETIC EPISTASIS; METHODOLOGY; MOLECULAR LIBRARY;

ADRENERGIC BETA-AGONISTS; CELL SURVIVAL; COMBINATORIAL CHEMISTRY TECHNIQUES; DRUG COMBINATIONS; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; DRUG INTERACTIONS; DRUG SYNERGISM; EPISTASIS, GENETIC; HCT116 CELLS; HUMANS; INTERLEUKIN-6; PHOSPHODIESTERASE 4 INHIBITORS; SMALL MOLECULE LIBRARIES;

EID: 84859729831     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb2003225     Document Type: Article

References (48)

1. Keith, C. T., Borisy, A. A., and Stockwell, B. R. (2005) Multicomponent therapeutics for networked systems. Nat. Rev. 4, 71-78.
2. Zimmermann, G. R., Lehar, J., and Keith, C. T. (2007) Multitarget therapeutics: when the whole is greater than the sum of the parts. Drug Discovery Today 12, 34-42.
3. Arav-Boger, R., and Shapiro, T. A. (2005) Molecular mechanisms of resistance in antimalarial chemotherapy: The unmet challenge. Ann. Rev. Pharmacol. Toxicol. 45, 565-585.
4. Vazquez, J. A. (2007) Combination antifungal therapy: The new frontier. Fut. Microbiol. 2, 115-139.
5. Dancey, J. E., and Chen, H. X. (2006) Strategies for optimizing combinations of molecularly targeted anticancer agents. Nat. Rev. 5, 649-659.
6. Dransfield, M. T., and Bailey, W. C. (2004) Fluticasone propionate/salmeterol for the treatment of chronic-obstructive pulmonary disease. Expert Opin. Pharmacother. 5, 1815-1826.
7. Jeschke, M. G., Finnerty, C. C., Kulp, G. A., Przkora, R., Mlcak, R. P., and Herndon, D. N. (2008) Combination of recombinant human growth hormone and propranolol decreases hypermetabolism and inflammation in severely burned children. Pediatr. Crit. Care Med. 9, 209-216.
8. Combates, N. J., Degiannis, D., Raskova, J., and Raska, K. Jr. (1995) Direct inhibition of human CD8+ lymphocyte activation by cyclosporine A and Rapamune-Sirolimus. Clin. Immunol. Immunopathol. 77, 221-228.
9. Pascual, J. (2005) Concentration-controlled everolimus (Certican): combination with reduced dose calcineurin inhibitors. Transplantation 79, 76-79.
10. Chou, T. C. (2006) Theoretical basis, experimental design, and computerized simulation of synergism and antagonism in drug combination studies. Pharmacol. Rev. 58, 621-681.
11. Costa, F., and D'Elios, M. M. (2010) Management of Helicobacter pylori infection. Expert Rev. Anti-Infect. Ther. 8, 887-892.
12. Bush, K., and Macielag, M. J. (2010) New beta-lactam antibiotics and beta-lactamase inhibitors. Expert Opin. Ther. Pat. 20, 1277- 1293.
13. Marcus, R., Paul, M., Elphick, H., and Leibovici, L. (2011) Clinical implications of beta-lactam-Aminoglycoside synergism: systematic review of randomised trials. Int. J. Antimicrob. Agents 37, 491-503.
14. Borisy, A. A., Elliott, P. J., Hurst, N. W., Lee, M. S., Lehar, J., Price, E. R., Serbedzija, G., Zimmermann, G. R., Foley, M. A., Stockwell, B. R., and Keith, C. T. (2003) Systematic discovery of multicomponent therapeutics. Proc. Natl. Acad. Sci. U.S.A. 100, 7977-7982.
15. Chung, T. (1998) Screen compounds singly: Why muck it up. J. Biomol. Screening 3, 171-173.
16. Ferrand, S., Schmid, A., Engeloch, C., and Glickman, J. F. (2005) Statistical evaluation of a self-deconvoluting matrix strategy for high-Throughput screening of the CXCR3 receptor. Assay Drug Dev. Technol. 3, 413-424.
17. Hodder, P., Mull, R., Cassaday, J., Berry, K., and Strulovici, B. (2004) Miniaturization of intracellular calcium functional assays to 1536-well plate format using a fluorometric imaging plate reader. J. Biomol. Screening 9, 417-426.
18. Liu, Y., Lacson, R., Cassaday, J., Ross, D. A., Kreamer, A., Hudak, E., Peltier, R., McLaren, D., Munoz-Sanjuan, I., Santini, F., Strulovici, B., and Ferrer, M. (2009) Identification of small-molecule modulators of mouse SVZ progenitor cell proliferation and differentiation through high-Throughput screening. J. Biomol. Screening 14, 319-329.
19. Greco, W. R., Bravo, G., and Parsons, J. C. (1995) The search for synergy: A critical review from a response surface perspective. Pharmacol. Rev. 47, 331-385.
20. Loewe, S. (1928) Die quantitativen Probleme der Pharmakologie. Ergebn. Physiol. 27, 47-187.
21. Bliss, C. (1939) The toxicity of poisons applied jointly. Ann. Appl. Biol. 26, 585-615.
22. Webb, J. (1963) Effect of more than one inhibitor, in Enzymes and Metabolic Inhibitors, Vol. 1, pp 487-512, Academic Press, New York.
23. Engelman, J. A., Chen, L., Tan, X., Crosby, K., Guimaraes, A. R., Upadhyay, R., Maira, M., McNamara, K., Perera, S. A., Song, Y., Chirieac, L. R., Kaur, R., Lightbown, A., Simendinger, J., Li, T., Padera, R. F., Garcia-Echeverria, C., Weissleder, R., Mahmood, U., Cantley, L. C., and Wong, K. K. (2008) Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers. Nat. Med. 14, 1351-1356.
24. Sunayama, J., Matsuda, K., Sato, A., Tachibana, K., Suzuki, K., Narita, Y., Shibui, S., Sakurada, K., Kayama, T., Tomiyama, A., and Kitanaka, C. (2010) Crosstalk between the PI3K/mTOR and MEK/ERK pathways involved in the maintenance of self-renewal and tumorigenicity of glioblastoma stem-like cells. Stem Cells 28, 1930-1939.
25. Balko, J. M., Jones, B. R., Coakley, V. L., and Black, E. P. (2009) Combined MEK and EGFR inhibition demonstrates synergistic activity in EGFR-dependent NSCLC. Cancer Biol. Ther. 8, 522-530.
26. Ou, D. L., Shen, Y. C., Liang, J. D., Liou, J. Y., Yu, S. L., Fan, H. H., Wang, D. S., Lu, Y. S., Hsu, C., and Cheng, A. L. (2009) Induction of Bim expression contributes to the antitumor synergy between sorafenib and mitogen-Activated protein kinase/extracellular signalregulated kinase kinase inhibitor CI-1040 in hepatocellular carcinoma. Clin. Cancer Res. 15, 5820-5828.
27. McCaig, A. M., Cosimo, E., Leach, M. T., and Michie, A. M. Dasatinib inhibits B cell receptor signalling in chronic lymphocytic leukaemia but novel combination approaches are required to overcome additional pro-survival microenvironmental signals. (2011) Br. J. Haematol. 153, 199-211. DOI:10.1111/j.1365-2141.2010.08507.x.
28. 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.
29. Cobelens, P. M., Kavelaars, A., Vroon, A., Ringeling, M., van der Zee, R., van Eden, W., and Heijnen, C. J. (2002) The beta 2-Adrenergic agonist salbutamol potentiates oral induction of tolerance, suppressing adjuvant arthritis and antigen-specific immunity. J. Immunol. 169, 5028- 5035.
30. Kim, D. H., Muthyala, S., Soliven, B., Wiegmann, K., Wollmann, R., and Chelmicka-Schorr, E. (1994) The beta 2-Adrenergic agonist terbutaline suppresses experimental allergic neuritis in Lewis rats. J. Neuroimmunol. 51, 177-183.
31. Verhoeckx, K. C., Doornbos, R. P., van der Greef, J., Witkamp, R. F., and Rodenburg, R. J. (2005) Inhibitory effects of the betaadrenergic receptor agonist zilpaterol on the LPS-induced production of TNF-Alpha in vitro and in vivo. J. Vet. Pharmacol. Ther. 28, 531-537.
32. Diamant, Z., and Spina, D. (2011) PDE4-inhibitors: A novel, targeted therapy for obstructive airways disease. Pulm. Pharmacol. Ther. 24, 353-360.
33. Nials, A. T., Tralau-Stewart, C. J., Gascoigne, M. H., Ball, D. I., Ranshaw, L. E., and Knowles, R. G. (2011) In vivo characterisation of GSK256066, a high affinity inhaled phosphodiesterase 4 inhibitor. J. Pharmacol. Exp. Ther. 337, 137-144.
34. Juergens, U. R., Stober, M., Libertus, H., Darlath, W., Gillissen, A., and Vetter, H. (2004) Different mechanisms of action of beta2-Adrenergic receptor agonists: A comparison of reproterol, fenoterol and salbutamol on monocyte cyclic-AMP and leukotriene B4 production in vitro. Eur. J. Med. Res. 9, 365-370.
35. Killian, U., Schudt, C. (2006) Altana Pharma AG, Synergistic combination, U.S. Patent 7056936.
36. Teixeira, M. M., Rossi, A. G., Giembycz, M. A., and Hellewell, P. G. (1996) Effects of agents which elevate cyclic AMP on guinea-pig eosinophil homotypic aggregation. Br. J. Pharmacol. 118, 2099-2106.
37. Giaever, G., Chu, A.M., Ni, L., Connelly, C., Riles, L., Veronneau, S., Dow, S., Lucau-Danila, A., Anderson, K., Andre, B., Arkin, A. P., Astromoff, A., El-Bakkoury, M., Bangham, R., Benito, R., Brachat, S., Campanaro, S., Curtiss, M., Davis, K., Deutschbauer, A., Entian, K. D., Flaherty, P., Foury, F., Garfinkel, D. J., Gerstein, M., Gotte, D., Guldener, U., Hegemann, J. H., Hempel, S., Herman, Z., Jaramillo, D. F., Kelly, D. E., Kelly, S. L., Kotter, P., LaBonte, D., Lamb, D. C., Lan, N., Liang, H., Liao, H., Liu, L., Luo, C., Lussier, M., Mao, R., Menard, P., Ooi, S. L., Revuelta, J. L., Roberts, C. J., Rose, M., Ross-Macdonald, P., Scherens, B., Schimmack, G., Shafer, B., Shoemaker, D. D., Sookhai-Mahadeo, S., Storms, R. K., Strathern, J. N., Valle, G., Voet, M., Volckaert, G., Wang, C. Y., Ward, T. R., Wilhelmy, J., Winzeler, E. A., Yang, Y., Yen, G., Youngman, E., Yu, K., Bussey, H., Boeke, J. D., Snyder, M., Philippsen, P., Davis, R. W., and Johnston, M. (2002) Functional profiling of the Saccharomyces cerevisiae genome. Nature 418, 387-391.
38. Costanzo, M., Baryshnikova, A., Bellay, J., Kim, Y., Spear, E. D., Sevier, C. S., Ding, H., Koh, J. L., Toufighi, K., Mostafavi, S., Prinz, J., St Onge, R. P., VanderSluis, B., Makhnevych, T., Vizeacoumar, F. J., Alizadeh, S., Bahr, S., Brost, R. L., Chen, Y., Cokol, M., Deshpande, R., Li, Z., Lin, Z. Y., Liang, W., Marback, M., Paw, J., San Luis, B. J., Shuteriqi, E., Tong, A. H., van Dyk, N., Wallace, I. M., Whitney, J. A., Weirauch, M. T., Zhong, G., Zhu, H., Houry, W. A., Brudno, M., Ragibizadeh, S., Papp, B., Pal, C., Roth, F. P., Giaever, G., Nislow, C., Troyanskaya, O. G., Bussey, H., Bader, G. D., Gingras, A. C., Morris, Q. D., Kim, P. M., Kaiser, C. A., Myers, C. L., Andrews, B. J., and Boone, C. (2010) The genetic landscape of a cell. Science 327, 425-431.
39. Schuldiner, M., Collins, S. R., Thompson, N. J., Denic, V., Bhamidipati, A., Punna, T., Ihmels, J., Andrews, B., Boone, C., Greenblatt, J. F., Weissman, J. S., and Krogan, N. J. (2005) Exploration of the function and organization of the yeast early secretory pathway through an epistatic miniarray profile. Cell 123, 507-519.
40. Tong, A. H., Lesage, G., Bader, G. D., Ding, H., Xu, H., Xin, X., Young, J., Berriz, G. F., Brost, R. L., Chang, M., Chen, Y., Cheng, X., Chua, G., Friesen, H., Goldberg, D. S., Haynes, J., Humphries, C., He, G., Hussein, S., Ke, L., Krogan, N., Li, Z., Levinson, J. N., Lu, H., Menard, P., Munyana, C., Parsons, A. B., Ryan, O., Tonikian, R., Roberts, T., Sdicu, A. M., Shapiro, J., Sheikh, B., Suter, B., Wong, S. L., Zhang, L. V., Zhu, H., Burd, C. G., Munro, S., Sander, C., Rine, J., Greenblatt, J., Peter, M., Bretscher, A., Bell, G., Roth, F. P., Brown, G. W., Andrews, B., Bussey, H., and Boone, C. (2004) Global mapping of the yeast genetic interaction network. Science 303, 808-813.
41. Lehar, J., Krueger, A., Zimmermann, G., and Borisy, A. (2008) High-order combination effects and biological robustness. Mol. Syst. Biol. 4, 215.
42. Lehar, J., Stockwell, B. R., Giaever, G., and Nislow, C. (2008) Combination chemical genetics. Nat. Chem. Biol. 4, 674-681.
43. Lehar, J., Zimmermann, G. R., Krueger, A. S., Molnar, R. A., Ledell, J. T., Heilbut, A. M., Short, G. F., 3rd, Giusti, L. C., Nolan, G. P., Magid, O. A., Lee, M. S., Borisy, A. A., Stockwell, B. R., and Keith, C. T. (2007) Chemical combination effects predict connectivity in biological systems. Mol. Syst. Biol. 3, 80.
44. Yeh, P., Tschumi, A. I., and Kishony, R. (2006) Functional classification of drugs by properties of their pairwise interactions. Nat. Genet. 38, 489-494.
45. Kainkaryam, R. M., and Woolf, P. J. (2008) poolHiTS: A shifted transversal design based pooling strategy for high-Throughput drug screening. BMC bioinformatics 9, 256.
46. Thierry-Mieg, N. (2006) A new pooling strategy for highthroughput screening: The Shifted Transversal Design. BMC Bioinformatics 7, 28.
47. R Development Core Team (2009) R: A Language and Environment for Statistical Computing, R Foundation for Statistical Computing, Vienna, Austria.
48. Hahsler, M., Grun, B., and Hornik, K. (2005) arules-A computational environment for mining association rules and frequent item sets. J. Stat. Software 14, 1-25.