Advanced search
Publication Cover
Expert Opinion on Therapeutic Patents Volume 19, 2009 - Issue 6
Submit an article Journal homepage
146
Views
6
CrossRef citations to date
0
Altmetric
Reviews

Advances in preclinical small molecules for the treatment of NSCLC

Qiu Zhang Shandong University, Chemistry, 27 Shanda Nanlu, Jinan, 250100 China
,
Wei Feng Shandong University, Chemistry, 27 Shanda Nanlu, Jinan, 250100 China
,
Hongyu Zhou St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, 38105 US
&
Bing Yan Shandong University, Chemistry, 27 Shanda Nanlu, Jinan, 250100 China; St. Jude Children's Research Hospital, Chemical Biology and Therapeutics, 262 Danny Thomas Place, Memphis, 38105 US +901 595 2797; +901 595 5715; [email protected]
Pages 731-751 | Published online: 21 May 2009

Bibliography

  • Cancer: WHO cancer control programme. World Health Organization. 2006. Available from: http://www.who.int/cancer/en. [Last Accessed 2 February 2009]
  • Landis SH, Murray T, Bolden S, Wingo PA. Cancer statistics 1999. CA Cancer J Clin 1999;49:8-31
  • Hirsch FR, Franklin WA, Gazdar AF, Bunn PA Jr. Early detection of lung cancer: clinical perspectives of recent advances in biology and radiology. Clin Cancer Res 2001;7:5-22
  • Hilbe W, Dirnhofer S, Greil R, Wöll E. Biomarkers in nonsmall cell lung cancer prevention. Eur J Cancer Prev 2004;13:425-36
  • Ciardiello F, Tortora G. A novel approach in the treatment of cancer: targeting the epidermal growth factor receptor. Clin Cancer Res 2001;7:2958-70
  • Nicholson RI, Gee JM, Harper ME. EGFR and cancer prognosis. Eur J Cancer 2001;37:s9-15
  • Azim HA Jr, Ganti AK. Targeted therapy in advanced non-small cell lung cancer (NSCLC): Where do we stand? Cancer Treat Rev 2006;32:630-6
  • Sequist LV. Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Oncologist 2007;12:325-30
  • Engelman JA, Jänne PA. Mechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Clin Cancer Res 2008;14:2895-9
  • Riely GJ. Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. J Thorac Oncol 2008;3:146-9
  • Albuschat R, Löwe W, Weber M, et al. 4-Anilinoquinazolines with Lavendustin A subunit as inhibitors of epidermal growth factor receptor tyrosine kinase: syntheses, chemical and pharmacological properties. Eur J Med Chem 2004;39:1001-11
  • Sun HY, Guan S, Bi HC, et al. Determination of CH330331, a novel 4-anilinoquinazoline inhibitor of epidermal growth factor receptor tyrosine kinase, in human Caco-2 monolayers by high performance liquid chromatography with ultraviolet detection: application to a trans-epithelial transport study. J Chromatogr B 2007;854:320-7
  • Fakhoury SA, Lee HT, Reed JE, et al. Pfizer. US2005250761; 2005
  • Ramanadham JP, Nannapaneni VC. Natco Pharma Ltd. WO2006090413; 2006
  • Sakurada A, Tsao MS. Predictive biomarkers for EGFR therapy. IDrugs 2009;12:34-8
  • Aviel-Ronen S, Blackhall FH, Shepherd FA, Tsao MS. K-ras mutations in nonsmall-cell lung carcinoma: a review. Clin Lung Cancer 2006;8:30-8
  • Fontanini G, Lucchi M, Vignati S, et al. Angiogenesis as a prognostic indicator of survival in non-small-cell lung carcinoma: a prospective study. J Natl Cancer Inst 1997;89:881-6
  • Macchiarini P, Fontanini G, Dulmet E, et al. Angiogenesis: an indicator of metastasis in non-small cell lung cancer invading the thoracic inlet. Ann Thorac Surg 1994;57:1534-9
  • Giatromanolaki A, Koukourakis M, O'Byrne K, et al. Prognostic value of angiogenesis in operable non-small cell lung cancer. J Pathol 1996;179:80-8
  • Meert AP, Paesmans M, Martin B, et al. The role of microvessel density on the survival of patients with lung cancer: a systematic review of the literature with meta-analysis. Br J Cancer 2002;87:694-701
  • Bremnes RM, Camps C, Sirera R. Angiogenesis in non-small cell lung cancer: the prognostic impact of neoangiogenesis and the cytokines VEGF and bFGF in tumors and blood. Lung Cancer 2006;51:143-58
  • Ito H, Oshita F, Kameday Y, et al. Expression of vascular endothelial growth factor and basic fibroblast growth factor in small adenocarcinomas. Oncol Rep 2002;9:119-23
  • Volm M, Koomagi R, Mattern J. PD-ECGF, bFGF, and VEGF expression in non-small cell lung carcinomas and their association with lymph node metastasis. Anticancer Res 1999;19:651-5
  • Koukourakis MI, Giatromanolaki A, O'Byrne KJ, et al. Platelet-derived endothelial cell growth factor expression correlates with tumor angiogenesis and prognosis in non-small-cell lung cancer. Br J Cancer 1997;75:477-81
  • Yuan A, Yu CJ, Chen WJ, et al. Correlation of total VEGF mRNA and protein expression with histologic type, tumor angiogenesis, patient survival and timing of relapse in non-small-cell lung cancer. Int J Cancer 2000;89:475-83
  • White ES, Strieter RM, Arenberg DA. Chemokines as therapeutic targets in non-small cell lung cancer. Curr Med Chem Anticancer Agents 2002;2:403-17
  • Petkova DK, Clelland C, Ronan J, et al. Overexpression of cyclooxygenase-2 in non-small cell lung cancer. Respir Med 2004;98:164-72
  • Subbaramaiah K, Dannenberg AJ. Cyclooxygenase 2: a molecular target for cancer prevention and treatment. Trends Pharmacol Sci 2003;24:96-102
  • Hicklin DJ, Ellis LM. Role of the vascular endothelial growth factor pathway in tumor growth and angiogenesis. J Clin Oncol 2005;23:1011-27
  • Shibuya M, Yamaguchi S, Yamane A, et al. Nucleotide sequence and expression of a novel human receptor-type tyrosine kinase (flt) closely related to the fms family. Oncogene 1990;5:519-24
  • Terman B. Identification of a new endothelial cell growth factor receptor tyrosine kinase. Oncogene 1991;6:1677-83
  • Hiratsuka S, Maru Y, Okada A, et al. Involvement of Flt-1 tyrosine kinase (vascular endothelial growth factor receptor-1) in pathological angiogenesis. Cancer Res 2001;61:1207-13
  • Fong GH, Rossant J, Gertsenstein M, Breitman ML. Role of the Flt-1 receptor tyrosine kinase in regulating the assembly of vascular endothelium. Nature 1995;376:66-70
  • Wedge SR, Ogilvie DJ, Dukes M, et al. ZD6474 inhibits vascular endothelial growth factor signalling, angiogenesis, and tumor growth following oral administration. Cancer Res 2002;62:4645-55
  • Amir E, Hughes S, Blackhall F, et al. Targeting Blood Vessels for the Treatment of Non-Small Cell Lung Cancer. Curr Cancer Drug Targets 2008;8:392-403
  • Goss GD, Laurie S, Shepherd F, et al. Phase I study of daily oral AZD2171, a vascular endothelial growth factor receptor inhibitor (VEGFRI), in combination with gemcitabine and cisplatin (G/C) in patients with advanced non-small cell lung cancer (ANSCLC): a study of the NCIC Clinical Trials Group 2007 ASCO Annual Meeting Proceedings [abstract 7649]. J Clin Oncol 2007;25
  • Schiller JH, Larson T, Ou SI, et al. Efficacy and safety of axitinib (AG-013736; AG) in patients with advanced non-small cell lung cancer (NSCLC): a phase II trial 2007 ASCO Annual Meeting Proceedings [abstract 7507]. J Clin Oncol 2007;25
  • Ueda Y, Yamagishi T, Samata K, et al. Antitumor effects of synthetic VEGF-receptor binding antagonist, VGA1155. Anticancer Res 2005;25:3973-7
  • Magnuson NS, Beck T, Vahidi H, et al. The Raf-1 serine/threonine protein kinase. Semin Cancer Biol 1994;5:247-53
  • Auberger J, Loeffler-Ragg J, Wurzer W, Hilbe W. Targeted therapies in non-small cell lung cancer: proven concepts and unfulfilled promises. Curr Cancer Drug Targets 2006;6:271-94
  • Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417:949-54
  • Avruch J, Khokhlatchev A, Kyriakis JM, et al. Ras activation of the Raf kinase: tyrosine kinase recruitment of the MAP kinase cascade. Recent Prog Horm Res 2001;56:127-55
  • Kato K, Cox AD, Hisaka MM, et al. Isoprenoid addition to Ras protein is the critical modification for its membrane association and transforming activity. Proc Natl Acad Sci USA 1992;89:6403-7
  • Reiss Y, Goldstein JL, Seabra MC, et al. Inhibition of purified p21ras farnesyl: protein transferase by Cys-AAX tetrapeptides. Cell 1990;62:81-8
  • Zhu HY, Njoroge FG, Cooper AB, et al. Schering Corp. US2004122018; 2004
  • Cutler DL, Baum C, Zaknoen SL. Schering Corp. WO2003047586; 2004
  • Kohl NE, Omer CA, Conner MW, et al. Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice. Nat Med 1995;1:792-7
  • Nielsen LL, Shi B, Hajian G, et al. Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models. Cancer Res 1999;59:5896-901
  • Yoon S, Seger R. The extracellular signal-regulated kinase: multiple substrates regulate diverse cellular functions. Growth Factors 2006;24:21-44
  • Robinson MJ, Cobb MH. Mitogen-activated protein kinase pathways. Curr Opin Cell Biol 1997;9:180-6
  • Flynn DL, Petillo PA, Kaufman MD, Patt WC; Deciphera Pharmaceuticals LLC: Wo2008033999 2008
  • Flynn DL, Kaufman MD, Patt WC, Petillo PA. Deciphera Pharmaceuticals LLC. WO2008034008; 2008
  • Rinehart J, Adjei AA, Lorusso PM, et al. Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer. J Clin Oncol 2004;22:4456-62
  • Lorusso P, Krishnamurthi S, Rinehart JR, et al. A phase 1–2 clinical study of a second generation oral MEK inhibitor, PD 0325901 in patients with advanced cancer 2005 ASCO Annual Meeting Proceedings [abstract 3011]. J Clin Oncol 2005;23
  • Yeh TC, Marsh V, Bernat BA, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res 2007;13:1576-83
  • Reddy EP, Reddy MVR. Temple university-of the commonwealth system of higher education. US2002022666; 2002
  • Engelman JA, Luo J, Cantley LC. The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet 2006;7:606-19
  • Katso R, Okkenhaug K, Ahmadi K, et al. Cellular function of phosphoinositide 3-kinases: implications for development, homeostasis, and cancer. Annu Rev Cell Dev Biol 2001;17:615-75
  • Engelman JA. The role of phosphoinositide 3-kinase pathway inhibitors in the treatment of lung cancer. Clin Cancer Res 2007;13:s4637-4640
  • Brognard J, Clark AS, Ni Y, Dennis PA. Akt/protein kinase B is constitutively active in non-small cell lung cancer cells and promotes cellular survival and resistance to chemotherapy and radiation. Cancer Res 2001;61:3986-97
  • Gridelli C, Maione P, Rossi A. The potential role of mTOR inhibitors in non-small cell lung cancer. Oncologist 2008;13:139-47
  • Tirado OM, Mateo-Lozano S, Notario V. Rapamycin induces apoptosis of JN-DSRCT-1 cells by increasing the Bax: Bcl-xL ratio through concurrent mechanisms dependent and independent of its mTOR inhibitory activity. Oncogene 2005;24:3348-57
  • Vignot S, Faivre S, Aguirre D, Raymond E. mTOR-targeted therapy of cancer with rapamycin derivatives. Ann Oncol 2005;16:525-37
  • Shimma N, Ebiike H, Ohwada J, et al. Chugai pharmaceutical co Ltd. WO2008018426; 2008
  • Garlich JR, Durden DL, Patterson M, et al. Semafore pharmaceuticals Inc. WO2004089925; 2004
  • Butterworth S, Griffen EJ, Pass M. AstraZeneca AB, AstraZeneca UK Ltd. WO2008032060; 2008
  • Butterworth S, Griffen EJ, Hill GB, Pass M. AstraZeneca AB, AstraZeneca UK Ltd. WO2008032036; 2008
  • Butterworth S, Griffen EJ, Hill GB, Pass M. AstraZeneca AB, AstraZeneca UK Ltd. WO2008032033; 2008
  • Butterworth S, Griffen EJ, Hill GB, Pass M. AstraZeneca AB, AstraZeneca UK Ltd. WO2008032089; 2008
  • Butterworth S, Hill GB, Griffen EJ, Pass M. AstraZeneca AB, AstraZeneca UK Ltd. WO2008032091; 2008
  • Yaguchi S, Fukui Y, Koshimizu I, et al. Antitumor Activity of ZSTK474, a New Phosphatidylinositol 3-Kinase Inhibitor. J Natl Cancer Inst 2006;98:545-56
  • She Q, Solit DB, Ye Q, et al. The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cells. Cancer Cell 2005;8:287-97
  • Engelman JA, Mukohara T, Zejnullahu K, et al. Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer. J Clin Invest 2006;116:2695-706
  • Pandolfi PP. Histone deacetylases and transcriptional therapy with their inhibitors. Cancer Chemother Pharmacol 2001;48:s17-19
  • Bhalla K, List A. Histone deacetylase inhibitors in myelodisplastic syndrome. Best Pract Res Clin Haematol 2004;17:595-611
  • Acharya ML, Sparreboom A, Venitz J, Figg WD. Rational development of histone deacetylase inhibitors as anticancer agents: a review. Mol Pharmacol 2005;68:917-32
  • Richon VM, O'Brien JP. Histone deacetylase inhibitors: a new class of potential therapeutic agents for cancer treatment. Clin Cancer Res 2002;8:662-4
  • Zhu WG, Dai Z, Ding H, et al. Increased expression of unmethylated CDKN2D by 5-aza-2′-deoxycytidine in human lung cancer cells. Oncogene 2001;20:7787-96
  • Rosato RR, Grant S. Histone deacetylase inhibitors in cancer therapy. Cancer Biol Ther 2003;2:30-7
  • Cuneo KC, Fu A, Osusky K, et al. Histone deacetylase inhibitor NVP-LAQ824 sensitizes human nonsmall cell lung cancer to the cytotoxic effects of ionizing radiation. Anticancer Drugs 2007;18:793-800
  • Loprevite M, Tiseo M, Grossi F, et al. In vitro study of CI-994, a histone decatylase inhibitor, in non small cell lung cancer cell lines. Oncol Res 2005;15:39-48
  • Komatsu N, Kawamata N, Takeuchi S, et al. SAHA, a HDAC inhibitor, has profound anti-growth activity against non-small cell lung cancer cells. Oncol Rep 2006;15:187-91
  • Lorusso PM, Demchik L, Foster B, et al. Preclinical antitumor activity of CI-994. Invest New Drugs 1996;14:349-56
  • Graziano MJ, Pilcher GD, Walsh KM, et al. Preclinical toxicity of a new oral anticancer drug, CI-994 (acetyldinaline), in rats and dogs. Invest New Drugs 1997;15:295-310
  • Prakash S, Foster BJ, Meyer M, et al. Chronic oral administration of CI-994: a phase 1 study. Invest New Drugs 2001;19:1-11
  • Wozniak A, O'shaughnessy J, Fiorica J, Grove W. Phase II trial of CI-994 in patients (pts) with advanced nonsmall cell lung cancer (NSCLC) [abstract 1878]. Proc Am Soc Clin Oncol 1999;18:487a
  • Von PAWEL J, Shepherd F, Gatzemeier U, et al. Randomized phase 2 study of the oral histone deacetylase inhibitor CI-994 plus gemcitabine (Gem) vs placebo (PBO) plus Gem in second-line nonsmall cell lung cancer (NSCLC) [abstract 1239]. Proc Am Soc Clin Oncol 2002;21:310a
  • Copley-Merriman K, Von Pawel J, Shepherd F, et al. Randomized phase 2 study of the oral histone deacetylase inhibitor CI-994 plus gemcitabine vs placebo plus gemcitabine in second-line nonsmall cell lung cancer (NSCLC): health-related quality of life results [abstract 1294]. Proc Am Soc Clin Oncol 2002;21:324a
  • Von Pawel J, Koschel G, Crino L, et al. Randomized phase II study of the oral histone deacetylase inhibitor CI-994 plus carboplatin (C) and paclitaxel (T) vs placebo (PBO) plus C/T in the first-line treatment of advanced nonsmall cell lung cancer (NSCLC) [abstract 626]. Proc Am Soc Clin Oncol 2003;22:626
  • Clark M, Copley-Merriman K, Coombs J, et al. Patient reported outcomes (symptoms, functioning, and quality of life) in a randomized phase II study of CI-994 plus carboplatin and paclitaxel (C/T) vs placebo (PBO) plus C/T in the first-line treatment of patients with advanced nonsmall cell lung cancer (NSCLC) [abstract 687]. Proc Am Soc Clin Oncol 2003;22:687
  • Marks PA, Rifkind RA, Richon VM, et al. Histone deacetylases and cancer: causes and therapies. Nat Rev Cancer 2001;1:194-202
  • Hershberger P, Owonikoko TK, Ramalingam S, Belani CP. The effect of p53 gene status on the interaction of vorinostat (suberoylanilide hydroxamic acid-SAHA) with carboplatin in non-small cell lung cancer (NSCLC) cell lines 2007 ASCO Annual Meeting Proceedings [abstract 10567]. J Clin Oncol 2007;25:581s
  • Geng L, Cuneo KC, Fu A, et al. Histone deacetylase (HDAC) inhibitor LBH589 increases duration of γ-H2AX foci and confines HDAC4 to the cytoplasm in irradiated non-small cell lung cancer. Cancer Res 2006;66:11298-304
  • Edwards A, Li J, Atadja P, et al. Effect of the histone deacetylase inhibitor LBH589 against epidermal growth factor receptor-dependent human lung cancer cells. Mol Cancer Ther 2007;6:2515-24
  • Kozikowski AP, Dritschilo A, Jung M, et al. US2005014839; 2005
  • Hassig CA, Symons KT, Guo X, et al. KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther 2008;7:1054-65
  • Wang JC. DNA topoisomerases. Annu Rev Biochem 1985;54:665-97
  • Wang JC, Caron PR, Kim RA. The role of DNA topoisomerase in recombination and genome stability: a double-edged sword? Cell 1990;62:403-6
  • Muller MT. Quantification of eukaryotic topoisomerase reactivity with DNA. Preferential cleavage of supercoiled DNA. Biochim Biophys Acta 1985;824:263-7
  • Wu MJ, Lin CF. Kaohsiung medical university. US2005004211; 2005
  • Bae YS, Noh YH, Lee BW, Park GH. KR784628; 2007
  • Senderowicz AM. Small-molecule cyclin-dependent kinase modulators. Rev Oncogene 2003;22:6609-20
  • Fry DW, Garrett MD. Inhibitors of cyclin-dependent kinases as therapeutic agents for the treatment of cancer. Curr Opin Oncol Endocr Meatabol Invest Drugs 2000;2:40-59
  • Shapiro GI. Cyclin-dependent pathways as targets for cancer treatment. J Clin Oncol 2006;24:1770-83
  • Toogood PL. Progress toward the development of agents to modulate the cell cycle. Curr Opin Chem Biol 2002;6:472-8
  • Knockaert M, Greengard P, Meijer L. Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci 2002;23:417-25
  • Fischer PM, Endicott J, Meijer L. Cyclin-dependent kinase inhibitors. Prog Cell Cycle Res 2003;5:235-48
  • Joshi KS, Rathos MJ, Mahajan P, et al. P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol Cancer Ther 2007;6:926-34
  • Joshi KS, Rathos MJ, Joshi RD, et al. In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol Cancer Ther 2007;6:918-25
  • Dong F, Guo W, Zhang L, et al. Downregulation of XIAP and induction of apoptosis by the synthetic cyclin-dependent kinase inhibitor GW8510 in non-small cell lung cancer cells. Cancer Biol Ther 2006;5:165-70
  • Sennhenn P, Mantoulidis A, Treu M, et al. Boehringer ingelheim Int, Boehringer ingelheim pharma. WO2006131552; 2006
  • Soo ET, Yip GW, Lwin ZM, et al. Heat shock proteins as novel therapeutic targets in cancer. In Vivo 2008;22:311-5
  • Austad BC, Grenier L, Holson EB, et al. Infinity discovery Inc. WO2008073424; 2008
  • Chandarlapaty S, Sawai A, Ye Q, et al. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res 2008;14:240-8
  • Kiang JG, Tsokos GC. Heat shock protein 70 kDa: molecular biology, biochemistry, and physiology. Pharmacol Ther 1998;80:183-201
  • Radons J, Multhoff G. Immunostimulatory functions of membrane-bound and exported heat shock protein 70. Exerc Immunol Rev 2005;11:17-33
  • Koya K, Sun L, Chen S, Jiang J. Synta pharmaceuticals corp. WO2008024304; 2008
  • Hamel E. Antimitotic natural products and their interactions with tubulin. Med Res Rev 1996;16:207-31
  • Pinney K, Wang F, Hadimani M, Del Pilar Mejia M. Univ baylor. WO2004099139; 2004;
  • Tamura K, Nakagawa K, Kurata T, et al. Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative and inhibitor of tubulin polymerization, which was administered to patients with advanced solid tumors on days 1 and 8 in 3-week courses. Cancer Chemother Pharmacol 2007;60:285-93
  • Rajski SR, Williams RM. DNA Cross-linking agents as antitumor drugs. Chem Rev 1998;98:2723-96
  • Hartley JA, O'Hare CC, Baumgart J. DNA alkylation and interstrand cross-linking by treosulfan. Br J Cancer 1999;79:264-6
  • Ward TH, Ranson M. Cancer rec tech Ltd. WO2005107743; 2005
  • Skibo EB, Xing C. US2003139609; 2003
  • Ma PC, Jagadeeswaran R, Jagadeesh S, et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res 2005;65:1479-88
  • Lutterbach B, Zeng Q, Davis LJ, et al. Lung cancer cell lines harboring MET gene amplification are dependent on Met for growth and survival. Cancer Res 2007;67:2081-8
  • Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007;316:1039-43
  • Bean J, Brennan C, Shih JY, 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 2007;104:20932-7
  • Garcia A, Rosen L, Cunninhgam CC, et al. Phase I study of ARQ 197, a selective inhibitor of the c-Met RTK in patients with metastatic solid tumors reaches recommended phase 2 dose 2007 ASCO Annual Meeting Proceedings [abstract 3525]. J Clin Oncol 2007;25
  • Eder JP, Heath E, Appleman L, et al. Phase I experience with c-MET inhibitor XL880 administered orally to patients (pts) with solid tumors. J Clin Oncol 2007;25:3526
  • Ross RW, Stein M, Sarantopoulos J, et al. A phase II study of the c-Met RTK inhibitor XL880 in patients (pts) with papillary renal-cell carcinoma (PRC) 2007 ASCO Annual Meeting Proceedings [abstract 15601]. J Clin Oncol 2007;25
  • Froning KJ, Felce JD, Jessen KA, et al. SGX523: a potent and highly selective small molecule inhibitor of the MET receptor tyrosine kinase. Presented at the AACR centennial annual meeting April 14 – 18, 2007, Los Angeles, CA (2007)
  • SGX initiates phase I trials for SGX523. SGX Pharmaceuticals Inc. 2008. Available from: http://www.medicalnewstoday.com/articles/94211.php. [ Last Accessed 5 February 2008]
  • Sattler M, Pride YB, Ma P, et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res 2003;63:5462-9
  • Puri N, Khramtsov A, Ahmed S, et al. A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res 2007;67:3529-34
  • Ma PC, Schaefer E, Christensen JG, Salgia R. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res 2005;11:2312-9
  • Zou HY, Li Q, Lee JH, et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res 2007;67:4408-17
  • Morotti A, Mila S, Accornero P, et al. K252a inhibits the oncogenic properties of Met, the HGF receptor. Oncogene 2002;21:4885-93
  • Lal M. Sonus pharmaceuticals, Inc. US7129368; 2006;
  • Mijatovic T, Van Quaquebeke E, Deneve N, et al. Unibioscreen S A. WO2008055530; 2008
  • Rodriguez Fernandez RE, Vera Alvarez R, De La Nuez Veulens A, et al. CT Ingenieria genetica biotech. WO2006119713; 2006
  • Kobayashi T, Tachibana K, Ohtake Y. Chugai pharmaceutical co Ltd. JP2000191675; 2000
  • Ozaki T, Morikawa K, Tachibana K. Chugai pharmaceutical co Ltd. JP2000109492; 2000
  • Pfahl M, Al-Shamma HA, Fanjul AN, et al. Maxia pharmaceuticals Inc. WO2003050098; 2003
  • Sohn YS, Baek HG, Lee CO. Korea adv inst sci & technology; IL yang pharm co Ltd; IL yang pharm ind co Ltd. WO2000058321; 2000
  • Lal M. Sonus pharmaceuticals, Inc. US2005209321; 2005
  • Michelakis E, Archer S. Univ alberta. WO2006108276; 2006
  • Vennemann M, Baer T, Braunger J, et al. Altana pharma AG. WO2006075012; 2006
  • Theodorakis E, Batova A. Univ california. WO2008057604; 2008
  • Dziadziuszko R, Camidge DR, Hirsch FR. The insulin-like growth factor pathway in lung cancer. J Thorac Oncol 2008;3:815-8
  • Petasis NA. US2005203184 2005
  • Mun SS, Park JJ, Seo YH, et al. Univ chosun. KR2000074182; 2000
  • Lee HS, Park YJ, Kim MH. Samsung general chemicals co. US5824689; 1998
  • Chen G, Li B, Li J. Welichem biotech Inc. WO2003080624; 2003
  • Li CJ, Zhang J. US2003149069; 2003
  • Ball HA, Cohen PS, Lee L, Ravera CP. Novartis AG, Novartis pharma GMBH. WO2003037897; 2003
  • Pettit GR, Tan R. Univ arizona. US5801222; 1998
  • Zhou HY, Wu SH, Zhai SM, et al. Design, synthesis, cytoselective toxicity, structure–activity relationships, and pharmacophore of thiazolidinone derivatives targeting drug-resistant lung cancer cells. J Med Chem 2008;51:1242-51
  • Teraishi F, Wu S, Sasaki J, et al. P-glycoprotein-independent apoptosis induction by a novel synthetic compound, MMPT [5-[(4-methylphenyl)methylene]-2-(phenylamino)-4 (5H)-thiazolone]. J Pharmacol Exp Ther 2005;314:355-62
  • Wu S, Guo W, Teraishi F, et al. Anticancer activity of 5-benzylidene- 2-phenylimino-1,3-thiazolidin-4-one (BPT) analogs. Med Chem 2006;2:597-605
  • Teraishi F, Wu S, Sasaki J, et al. JNK1-dependent antimitotic activity of thiazolidin compounds in human non-small-cell lung and colon cancer cells. Cell Mol Life Sci 2005;62:2382-9
  • Baselga J. Combining the anti-EGFR agent gefitinib with chemotherapy in non-small-cell lung cancer: how do we go from INTACT to impact? J Clin Oncol 2004;22:759-61
  • Maione P, Gridelli C, Troiani T, Ciardiello F. Combining targeted therapies and drugs with multiple targets in the treatment of NSCLC. Oncologist 2006;11:274-84

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.