Identification and preliminary characterization of novel small molecules that inhibit growth of human lung adenocarcinoma cells

Journal of Biomolecular Screening

Volumn 14, Issue 10, 2009, Pages 1176-1184

  Somwar, Romel ^a   Shum, David ^a   Djaballah, Hakim ^a   Varmus, Harold ^a  

^a MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

Author keywords

EGFR; High throughput drug screen; KRAS; Lung cancer

Indexed keywords

2 PHENYLPYRIDAZIN 3(2H) ONE DERIVATIVE; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; GEFITINIB; MITOGEN ACTIVATED PROTEIN KINASE; PHOSPHATIDYLINOSITOL 3 KINASE; PYRIDAZINONE DERIVATIVE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; CANCER CELL; CANCER INHIBITION; CELL SURVIVAL; CONTROLLED STUDY; DNA SYNTHESIS; DRUG HALF LIFE; ENZYME ACTIVITY; GENE EXPRESSION; GENE MUTATION; HUMAN; HUMAN CELL; IC 50; LIVER MICROSOME; LUNG ADENOCARCINOMA; ONCOGENE K RAS; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION;

1-PHOSPHATIDYLINOSITOL 3-KINASE; ADENOCARCINOMA; ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL LINE, TUMOR; CELL PROLIFERATION; DNA, NEOPLASM; DRUG SCREENING ASSAYS, ANTITUMOR; HALF-LIFE; HUMANS; HYDRAZINES; LUNG NEOPLASMS; MICROSOMES, LIVER; MITOGEN-ACTIVATED PROTEIN KINASES; PHOSPHORYLATION; RECEPTOR, EPIDERMAL GROWTH FACTOR; SIGNAL TRANSDUCTION; SMALL MOLECULE LIBRARIES;

EID: 71949104673     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057109350919     Document Type: Article

References (26)

1. Jemal A, Siegel R, Ward E, Hao Y, Xu J, Murray T, et al: Cancer statistics, 2008. CA Cancer J Clin 2008;58:71-96.
2. Pao W, Miller VA: Epidermal growth factor receptor mutations, smallmolecule kinase inhibitors, and non-small-cell lung cancer: current knowledge and future directions. J Clin Oncol 2005;23:2556-2568.
3. Lynch TJ, Bell DW, Sordella R, Gurubhagavatula S, Okimoto RA, Brannigan BW, et al: Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-2139.
4. Paez JG, Janne PA, Lee JC, Tracy S, Greulich H, Gabriel S, et al: EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304:1497-1500.
5. Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, et al: EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci USA 2004;101:13306-13311.
6. Kobayashi S, Boggon TJ, Dayaram T, Janne PA, Kocher O, Meyerson M, et al: EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 2005;352:786-792.
7. Pao W, Miller VA, Politi KA, Riely GJ, Somwar R, Zakowski MF, et al: Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med 2005;2:e73.
8. Bean J, Brennan C, Shih JY, Riely G, Viale A, Wang L, et al: MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci USA 2007;104:20932-20937.
9. Engelman JA, Zejnullahu K, Mitsudomi T, Song Y, Hyland C, Park JO, et al: MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007;316:1039-1043.
10. Rodenhuis S, Slebos RJ: The ras oncogenes in human lung cancer. Am Rev Respir Dis 1990;142:S27-S30.
11. Suzuki Y, Orita M, Shiraishi M, Hayashi K, Sekiya T: Detection of ras gene mutations in human lung cancers by single-strand conformation polymorphism analysis of polymerase chain reaction products. Oncogene 1990;5:1037-1043.
12. Ding L, Getz G, Wheeler DA, Mardis ER, McLellan MD, Cibulskis K, et al: Somatic mutations affect key pathways in lung adenocarcinoma. Nature 2008;455:1069-1075.
13. Weir BA, Woo MS, Getz G, Perner S, Ding L, Beroukhim R, et al: Characterizing the cancer genome in lung adenocarcinoma. Nature 2007;450:893-898.
14. Shum D, Radu C, Kim E, Cajuste M, Shao Y, Seshan VE, et al: A high density assay format for the detection of novel cytotoxic agents in large chemical libraries. J Enzyme Inhib Med Chem 2008;23:931-945.
15. Antczak C, Shum D, Radu C, Seshan VE, Djaballah H: Development and validation of a high-density fluorescence polarization-based assay for the trypanosoma RNA triphosphatase TbCet1. Comb Chem High Throughput Screen 2009;12:258-268.
16. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73.
17. Sordella R, Bell DW, Haber DA, Settleman J: Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305:1163-1167.
18. Tracy S, Mukohara T, Hansen M, Meyerson M, Johnson BE, Janne PA: Gefitinib induces apoptosis in the EGFRL858R non-small-cell lung cancer cell line H3255. Cancer Res 2004;64:7241-7244.
19. Ghose AK, Viswanadhan VN, Wendoloski JJ: A knowledge-based approach in designing combinatorial or medicinal chemistry libraries for drug discovery: 1. A qualitative and quantitative characterization of known drug databases. J Comb Chem 1999;1:55-68.
20. Whitehurst AW, Bodemann BO, Cardenas J, Ferguson D, Girard L, Peyton M, et al: Synthetic lethal screen identification of chemosensitizer loci in cancer cells. Nature 2007;446:815-819.
21. Wood LD, Parsons DW, Jones S, Lin J, Sjoblom T, Leary RJ, et al: The genomic landscapes of human breast and colorectal cancers. Science 2007;318:1108-1113.
22. Guha U, Chaerkady R, Marimuthu A, Patterson AS, Kashyap MK, Harsha HC, et al: Comparisons of tyrosine phosphorylated proteins in cells expressing lung cancer-specific alleles of EGFR and KRAS. Proc Natl Acad Sci USA 2008;105:14112-14117.
23. Rikova K, Guo A, Zeng Q, Possemato A, Yu J, Haack H, et al: Global survey of phosphotyrosine signaling identifies oncogenic kinases in lung cancer. Cell 2007;131:1190-1203.
24. Godl K, Wissing J, Kurtenbach A, Habenberger P, Blencke S, Gutbrod H, et al: An efficient proteomics method to identify the cellular targets of protein kinase inhibitors. Proc Natl Acad Sci USA 2003;100: 15434-15439.
25. Lamb J, Crawford ED, Peck D, Modell JW, Blat IC, Wrobel MJ, et al: The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease. Science 2006;313:1929-1935.
26. Yang WS, Stockwell BR: Synthetic lethal screening identifies compounds activating iron-dependent, nonapoptotic cell death in oncogenic- RAS-harboring cancer cells. Chem Biol 2008;15:234-245.