Targeting ROS1 with anaplastic lymphoma kinase inhibitors: A promising therapeutic strategy for a newly defined molecular subset of non-small-cell lung cancer

Journal of Thoracic Oncology

Volumn 7, Issue 11, 2012, Pages 1625-1630

  Chin, Leow Pay ^a   Soo, Ross A ^a,c   Soong, Richie ^a   Ou, Sai Hong I ^b  

^a NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

^b Division of Hematology Oncology   (United States)

^c NATIONAL UNIVERSITY HEALTH SYSTEM   (Singapore)

Author keywords

Anaplastic lymphoma kinase inhibitors; Crizotinib; Non small cell lung cancer; ROS1; Targeted therapy

Indexed keywords

5 CHLORO N2 [1 (5 FLUORO 2 PYRIMIDINYL)ETHYL] N4 (5 METHYL 1H PYRAZOL 3 YL) 2,4 PYRIMIDINEDIAMINE; ANAPLASTIC LYMPHOMA KINASE INHIBITOR; ANTINEOPLASTIC AGENT; AP 26113; ASP 3026; BARRIER TO AUTOINTEGRATION FACTOR; CRIZOTINIB; EPIDERMAL GROWTH FACTOR RECEPTOR; KIST 301072; KIST 301080; MAMMALIAN TARGET OF RAPAMYCIN; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE B; PROTEIN TYROSINE KINASE INHIBITOR; SODIUM PHOSPHATE COTRANSPORTER 2B; SYNDECAN 4; TAE 684; TYROSINE KINASE RECEPTOR; UNCLASSIFIED DRUG; VAV PROTEIN; WZ 5 126;

C ROS ONCOGENE 1; CANCER CHEMOTHERAPY; CANCER PATIENT; CELL PROLIFERATION; CELL SURVIVAL; CHROMOSOME REARRANGEMENT; DOWN REGULATION; DRUG TARGETING; FLUORESCENCE IN SITU HYBRIDIZATION; GENE AMPLIFICATION; GENE EXPRESSION; GENE FUNCTION; GENE FUSION; GENE MUTATION; GENE OVEREXPRESSION; GENE STRUCTURE; GENETIC ASSOCIATION; HUMAN; IMMUNOHISTOCHEMISTRY; LUNG ADENOCARCINOMA; LUNG NON SMALL CELL CANCER; MICROARRAY ANALYSIS; MOLECULARLY TARGETED THERAPY; NONHUMAN; ONCOGENE; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; PROTEIN AGGREGATION; PROTEIN LOCALIZATION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; REVIEW; SIGNAL TRANSDUCTION;

EID: 84867888741     PISSN: 15560864     EISSN: 15561380     Source Type: Journal    
DOI: 10.1097/JTO.0b013e31826baf83     Document Type: Article

References (40)

1. Shibuya M, Hanafusa H, Balduzzi PC. Cellular sequences related to three new onc genes of avian sarcoma virus (fps, yes, and ros) and their expression in normal and transformed cells. J Virol 1982;42:143-152.
2. Nagarajan L, Louie E, Tsujimoto Y, Balduzzi PC, Huebner K, Croce CM. The human c-ros gene (ROS) is located at chromosome region 6q16- -6q22. Proc Natl Acad Sci USA 1986;83:6568-6572.
3. Ou SH, Tan J, Ye n Y, Soo RA. ROS1 as a 'druggable' receptor tyrosine kinase: lessons learned from inhibiting the ALK pathway. Expert Rev Anticancer Ther 2012;12:447-456.
4. Shaw AT, Camidge DR, Engelman JA, et al. Clinical activity of crizotinib in advanced non-small cell lung cancer (NSCLC) harboring ROS1 gene rearrangement. J Clin Oncol 2012;30:(suppl; abstr 7508).
5. Acquaviva J, Wong R, Charest A. The multifaceted roles of the receptor tyrosine kinase ROS in development and cancer. Biochim Biophys Acta 2009;1795:37-52.
6. Charest A, Wilker E W, McLaughlin ME, et al. ROS fusion tyrosine kinase activates a SH2 domain-containing phosphatase-2/phosphatidylinositol 3-kinase/mammalian target of rapamycin signaling axis to form glioblas-toma in mice. Cancer Res 2006;66:7473-7481.
7. Chiarle R, Simmons WJ, Cai H, et al. Stat3 is required for ALK-mediated lymphomagenesis and provides a possible therapeutic target. Nat Med 2005;11:623-629.
8. Chiarle R, Voena C, Ambrogio C, Piva R, Inghirami G. The anaplastic lymphoma kinase in the pathogenesis of cancer. Nat Rev Cancer 2008;8:11-23.
9. Soda M, Takada S, Takeuchi K, et al. A mouse model for EML4-ALK-positive lung cancer. Proc Natl Acad Sci USA 2008;105:19893-19897.
10. Govindan R, Ding L, Griffth M, et al. Genomic landscape of non-small cell lung cancer in smokers and never-smokers. Cell 2012;150:1121-1134.
11. Charest A, Lane K, McMahon K, et al. Fusion of FIG to the receptor tyrosine kinase ROS in a glioblastoma with an interstitial del(6)(q21q21). Genes Chromosomes Cancer 2003;37:58-71.
12. Gu TL, Deng X, Huang F, et al. Survey of tyrosine kinase signaling reveals ROS kinase fusions in human cholangiocarcinoma. PLoS ONE 2011;6:e15640.
13. Rikova K, Guo A, Zeng Q, et al. Global survey of phosphotyrosine signaling identifes oncogenic kinases in lung cancer. Cell 2007;131:1190-1203.
14. Takeuchi K, Soda M, Togashi Y, et al. RET, ROS1 and ALK fusions in lung cancer. Nat Med 2012;18:378-381.
15. Bergethon K, Shaw AT, Ou SH, et al. ROS1 rearrangements defne a unique molecular class of lung cancers. J Clin Oncol 2012;30:863-870.
16. Li C, Fang R, Sun Y, et al. Spectrum of oncogenic driver mutations in lung adenocarcinomas from East Asian never smokers. PLoS ONE 2011;6:e28204.
17. Rimkunas V, Crosby K, Kelly M, et al. Analysis of receptor tyrosine kinase ROS1 positive tumors in non-small cell lung cancer: identifcation of a FIG-ROS1 fusion. Clin Cancer Res 2012;18:4449-4457.
18. Shigematsu H, Gazdar AF. Somatic mutations of epidermal growth factor receptor signaling pathway in lung cancers. Int J Cancer 2006;118:257-262.
19. Solomon B, Varella-Garcia M, Camidge DR. ALK gene rearrangements: a new therapeutic target in a molecularly defned subset of non-small cell lung cancer. J Thorac Oncol 2009;4:1450-1454.
20. Bhattacharjee A, Richards WG, Staunton J, et al. Classifcation of human lung carcinomas by mRNA expression profling reveals distinct adeno-carcinoma subclasses. Proc Natl Acad Sci USA 2001;98:13790-13795.
21. Garber ME, Troyanskaya OG, Schluens K, et al. Diversity of gene expression in adenocarcinoma of the lung. Proc Natl Acad Sci USA 2001;98:13784-13789.
22. Bild AH, Ya o G, Chang JT, et al. Oncogenic pathway signatures in human cancers as a guide to targeted therapies. Nature 2006;439:353-357.
23. Kan Z, Jaiswal BS, Stinson J, et al. Diverse somatic mutation patterns and pathway alterations in human cancers. Nature 2010;466:869-873.
24. Davies H, Hunter C, Smith R, et al. Somatic mutations of the protein kinase gene family in human lung cancer. Cancer Res 2005;65:7591-7595.
25. Ruhe JE, Streit S, Hart S, et al. Genetic alterations in the tyrosine kinase transcriptome of human cancer cell lines. Cancer Res 2007; 67:11368-11376.
26. Cancer Genome Atlas Research Network. Integrated genomic analyses of ovarian cancer. Nature 2011;474:609-615.
27. Durinck S, Ho C, Wang NJ, et al. Temporal dissection of tumorigenesis in primary cancers. Cancer Discov 2011;1:137-143.
28. Mapstone T, McMichael M, Goldthwait D. Expression of platelet-derived growth factors, transforming growth factors, and the ros gene in a variety of primary human brain tumors. Neurosurgery 1991;28:216-222.
29. Watkins D, Dion F, Poisson M, Delattre JY, Rouleau GA. Analysis of oncogene expression in primary human gliomas: evidence for increased expression of the ros oncogene. Cancer Genet Cytogenet 1994; 72:130-136.
30. Zhao JF, Sharma S. Expression of the ROS1 oncogene for tyrosine receptor kinase in adult human meningiomas. Cancer Genet Cytogenet 1995;83:148-154.
31. Girish V, Sachdeva N, Minz RW, Radotra B, Mathuria SN, Arora SK. Bcl2 and ROS1 expression in human meningiomas: an analysis with respect to histological subtype. Indian J Pathol Microbiol 2005;48:325-330.
32. Maher CA, Kumar-Sinha C, Cao X, et al. Transcriptome sequencing to detect gene fusions in cancer. Nature 2009;458:97-101.
33. Levin JZ, Berger MF, Adiconis X, et al. Targeted next-generation sequencing of a cancer transcriptome enhances detection of sequence variants and novel fusion transcripts. Genome Biol 2009;10:R115.
34. Kim H, Yo o SB, Choe JY, et al. Detection of ALK gene rearrangement in non-small cell lung cancer: a comparison of fuorescence in situ hybridization and chromogenic in situ hybridization with correlation of ALK protein expression. J Thorac Oncol 2011;6:1359-1366.
35. Yoshida A, Tsuta K, Nitta H, et al. Bright-feld dual-color chromogenic in situ hybridization for diagnosing echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase-positive lung adenocarcino-mas. J Thorac Oncol 2011;6:1677-1686.
36. McDermott U, Iafrate AJ, Gray NS, et al. Genomic alterations of anaplas-tic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res 2008;68:3389-3395.
37. Lovly CM, Heuckmann JM, de Stanchina E, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors. Cancer Res 2011;71:4920-4931.
38. Katayama R, Khan TM, Benes C, et al. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci USA 2011;108:7535-7540.
39. Park BS, El-Deeb IM, Yo o KH, et al. Design, synthesis and biological evaluation of new potent and highly selective ROS1-tyrosine kinase inhibitor. Bioorg Med Chem Lett 2009;19:4720-4723.
40. El-Deeb IM, Park BS, Jung SJ, et al. Design, synthesis, screening, and molecular modeling study of a new series of ROS1 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett 2009;19:5622-5626.