NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants

Investigational New Drugs

Volumn 32, Issue 3, 2014, Pages 389-399

  Shin, Jae Sik ^a   Hong, Seung Woo ^a   Moon, Jai Hee ^a   Kim, Jin Sun ^a   Jung, Kyung Ah ^a   Kim, Seung Mi ^a   Lee, Dae Hee ^a   Kim, InKi ^a   Yoon, Seon Joo ^b   Lee, Chang Gyu ^a   Choi, Eun Kyoung ^a   Lee, Joo Young ^a   Kim, Kyu Pyo ^a   Hong, Yong Sang ^a   Lee, Jae Lyun ^a   Kim, Bongcheol ^a   Choi, Eun Kyung ^a   Lee, Jung Shin ^a   Jin, Dong Hoon ^a   Kim, Tae Won ^a  

^a University of Ulsan College of Medicine   (South Korea)

^b NeoPharm Co Ltd   (South Korea)

Author keywords

Constitutively active mutants; Hepatocyte growth factor (HGF); MET; NPS 1034

Indexed keywords

NPS 1034; PHOSPHOTRANSFERASE INHIBITOR; SCATTER FACTOR; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; FUSED HETEROCYCLIC RINGS; NPS-1034; PROTEIN KINASE INHIBITOR; PYRAZOLE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIANGIOGENIC ACTIVITY; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; AUTOPHOSPHORYLATION; BIOLOGICAL ACTIVITY; CELL GROWTH; CELL PROLIFERATION; CELL VIABILITY; CONTROLLED STUDY; DRUG INHIBITION; DRUG POTENCY; ENZYME PHOSPHORYLATION; FEMALE; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; TUMOR REGRESSION; TUMOR XENOGRAFT; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG EFFECTS; DRUG SCREENING; GENETICS; METABOLISM; MUTANT MOUSE STRAIN; MUTATION; NEOPLASMS; PATHOLOGY; TUMOR CELL LINE; TUMOR VOLUME;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; FEMALE; HEPATOCYTE GROWTH FACTOR; HETEROCYCLIC COMPOUNDS, 2-RING; HUMANS; MICE, MUTANT STRAINS; MUTATION; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MET; PYRAZOLES; TUMOR BURDEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84904625181     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-013-0039-4     Document Type: Article

References (32)

1. Sattler M, Salgia R (2009) The MET axis as a therapeutic target. Update Cancer Ther 3(3):109-118. doi:10.1016/j.uct.2009.01.001
2. Otsuka T, Takayama H, Sharp R, Celli G, LaRochelle WJ, Bottaro DP, Ellmore N, Vieira W, Owens JW, Anver M, Merlino G (1998) c-Met autocrine activation induces development of malignant melanoma and acquisition of the metastatic phenotype. Cancer Res 58(22):5157-5167 (Pubitemid 28521177)
3. Sattler M, Salgia R (2007) c-Met and hepatocyte growth factor: potential as novel targets in cancer therapy. Curr Oncol Rep 9(2):102-108 (Pubitemid 46332381)
4. Christensen JG, Burrows J, Salgia R (2005) c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett 225(1):1-26. doi:10.1016/j.canlet.2004.09.044 (Pubitemid 40732764)
5. Toiyama Y, Yasuda H, Saigusa S, Matushita K, Fujikawa H, Tanaka K, Mohri Y, Inoue Y, Goel A, Kusunoki M (2012) Co-expression of hepatocyte growth factor and c-Met predicts peritoneal dissemination established by autocrine hepatocyte growth factor/c-Met signaling in gastric cancer. Int J Cancer 130(12):2912-2921. doi:10.1002/ijc.26330
6. Eder JP, Vande Woude GF, Boerner SA, LoRusso PM (2009) Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin Cancer Res 15(7):2207-2214. doi:10.1158/1078-0432.CCR-08-1306
7. Lorenzato A, Olivero M, Patane S, Rosso E, Oliaro A, Comoglio PM, Di Renzo MF (2002) Novel somatic mutations of the MET oncogene in human carcinoma metastases activating cell motility and invasion. Cancer Res 62(23):7025-7030 (Pubitemid 35424097)
8. Bellon SF, Kaplan-Lefko P, Yang Y, Zhang Y, Moriguchi J, Rex K, Johnson CW, Rose PE, Long AM, O'Connor AB, Gu Y, Coxon A, Kim TS, Tasker A, Burgess TL, Dussault I (2008) c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations. J Biol Chem 283(5):2675-2683. doi:10.1074/jbc.M705774200
9. Park WS, Dong SM, Kim SY, Na EY, Shin MS, Pi JH, Kim BJ, Bae JH, Hong YK, Lee KS, Lee SH, Yoo NJ, Jang JJ, Pack S, Zhuang Z, Schmidt L, Zbar B, Lee JY (1999) Somatic mutations in the kinase domain of the Met/hepatocyte growth factor receptor gene in childhood hepatocellular carcinomas. Cancer Res 59(2):307-310 (Pubitemid 29048858)
10. Di Renzo MF, Olivero M, Martone T, Maffe A, Maggiora P, Stefani AD, Valente G, Giordano S, Cortesina G, Comoglio PM (2000) Somatic mutations of the MET oncogene are selected during metastatic spread of human HNSC carcinomas. Oncogene 19(12):1547-1555. doi:10.1038/sj.onc.1203455 (Pubitemid 30175676)
11. Ma PC, Kijima T, Maulik G, Fox EA, Sattler M, Griffin JD, Johnson BE, Salgia R (2003) c-MET mutational analysis in small cell lung cancer: novel juxtamembrane domain mutations regulating cytoskeletal functions. Cancer Res 63(19):6272-6281 (Pubitemid 37255174)
12. Yuen HF, Abramczyk O, Montgomery G, Chan KK, Huang YH, Sasazuki T, Shirasawa S, Gopesh S, Chan KW, Fennell D, Janne P, El-Tanani M, Murray JT (2012) Impact of oncogenic driver mutations on feedback between the PI3K and MEK pathways in cancer cells. Biosci Rep 32(4):413-422. doi:10.1042/BSR20120050
13. Maritano D, Accornero P, Bonifaci N, Ponzetto C (2000) Two mutations affecting conserved residues in the Met receptor operate via different mechanisms. Oncogene 19(10):1354-1361. doi:10.1038/sj.onc.1203431 (Pubitemid 30160628)
14. Graveel C, Su Y, Koeman J, Wang LM, Tessarollo L, Fiscella M, Birchmeier C, Swiatek P, Bronson R, Vande Woude G (2004) Activating Met mutations produce unique tumor profiles in mice with selective duplication of the mutant allele. Proc Natl Acad Sci U S A 101(49):17198-17203. doi:10.1073/pnas.0407651101 (Pubitemid 39627797)
15. Berthou S, Aebersold DM, Schmidt LS, Stroka D, Heigl C, Streit B, Stalder D, Gruber G, Liang C, Howlett AR, Candinas D, Greiner RH, Lipson KE, Zimmer Y (2004) The Met kinase inhibitor SU11274 exhibits a selective inhibition pattern toward different receptor mutated variants. Oncogene 23(31):5387-5393. doi:10.1038/sj.onc.1207691 (Pubitemid 39005814)
16. Zimmer Y, Vaseva AV, Medova M, Streit B, Blank-Liss W, Greiner RH, Schiering N, Aebersold DM (2010) Differential inhibition sensitivities of MET mutants to the small molecule inhibitor SU11274. Cancer Lett 289(2):228-236. doi:10.1016/j.canlet.2009.08.017
17. Qi J, McTigue MA, Rogers A, Lifshits E, Christensen JG, Janne PA, Engelman JA (2011) Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors. Cancer Res 71(3):1081-1091. doi:10.1158/0008-5472.CAN-10-1623
18. Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F (2011) A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients. Cancer Res 71(15):5255-5264. doi:10.1158/0008-5472.CAN-10-4433
19. Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ (2010) MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res 70(4):1524-1533. doi:10.1158/0008-5472.CAN- 09-2541
20. Hong SW, Kim CJ, Park WS, Shin JS, Lee SD, Ko SG, Jung SI, Park IC, An SK, Lee WK, Lee WJ, Jin DH, Lee MS (2009) p34SEI-1 inhibits apoptosis through the stabilization of the X-linked inhibitor of apoptosis protein: p34SEI-1 as a novel target for anti-breast cancer strategies. Cancer Res 69(3):741-746. doi:10.1158/0008-5472.CAN-08-1189
21. Moonen JR, Krenning G, Brinker MG, Koerts JA, van Luyn MJ, Harmsen MC (2010) Endothelial progenitor cells give rise to proangiogenic smooth muscle-like progeny. Cardiovasc Res 86(3):506-515. doi:10.1093/cvr/cvq012
22. Kong-Beltran M, Seshagiri S, Zha J, Zhu W, Bhawe K, Mendoza N, Holcomb T, Pujara K, Stinson J, Fu L, Severin C, Rangell L, Schwall R, Amler L, Wickramasinghe D, Yauch R (2006) Somatic mutations lead to an oncogenic deletion of met in lung cancer. Cancer Res 66(1):283-289. doi:10.1158/0008-5472.CAN-05- 2749 (Pubitemid 43166034)
23. Zwick E, Bange J, Ullrich A (2001) Receptor tyrosine kinase signalling as a target for cancer intervention strategies. Endocr Relat Cancer 8(3):161-173 (Pubitemid 32947638)
24. Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ, Cherrington JM, Mendel DB (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res 63(21):7345-7355 (Pubitemid 37413476)
25. Crosswell HE, Dasgupta A, Alvarado CS, Watt T, Christensen JG, De P, Durden DL, Findley HW (2009) PHA665752, a small-molecule inhibitor of c-Met, inhibits hepatocyte growth factor-stimulated migration and proliferation of c-Met-positive neuroblastoma cells. BMC Cancer 9:411. doi:10.1186/1471-2407-9- 411
26. Smolen GA, Sordella R, Muir B, Mohapatra G, Barmettler A, Archibald H, Kim WJ, Okimoto RA, Bell DW, Sgroi DC, Christensen JG, Settleman J, Haber DA (2006) Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A 103(7):2316-2321. doi:10.1073/pnas.0508776103
27. Jun HT, Sun J, Rex K, Radinsky R, Kendall R, Coxon A, Burgess TL (2007) AMG 102, a fully human anti-hepatocyte growth factor/scatter factor neutralizing antibody, enhances the efficacy of temozolomide or docetaxel in U-87 MG cells and xenografts. Clin Cancer Res 13(22 Pt 1):6735-6742. doi:10.1158/1078-0432. CCR-06-2969 (Pubitemid 350206811)
28. Guo A, Villen J, Kornhauser J, Lee KA, Stokes MP, Rikova K, Possemato A, Nardone J, Innocenti G, Wetzel R, Wang Y, MacNeill J, Mitchell J, Gygi SP, Rush J, Polakiewicz RD, Comb MJ (2008) Signaling networks assembled by oncogenic EGFR and c-Met. Proc Natl Acad Sci U S A 105(2):692-697. doi:10.1073/pnas.0707270105 (Pubitemid 351171770)
29. Jo M, Stolz DB, Esplen JE, Dorko K, Michalopoulos GK, Strom SC (2000) Cross-talk between epidermal growth factor receptor and c-Met signal pathways in transformed cells. J Biol Chem 275(12):8806-8811 (Pubitemid 30180235)
30. Stommel JM, Kimmelman AC, Ying H, Nabioullin R, Ponugoti AH, Wiedemeyer R, Stegh AH, Bradner JE, Ligon KL, Brennan C, Chin L, DePinho RA (2007) Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies. Science 318(5848):287-290. doi:10.1126/science.1142946 (Pubitemid 47574858)
31. Bean J, Brennan C, Shih JY, Riely G, Viale A, Wang L, Chitale D, Motoi N, Szoke J, Broderick S, Balak M, Chang WC, Yu CJ, Gazdar A, Pass H, Rusch V, Gerald W, Huang SF, Yang PC, Miller V, Ladanyi M, Yang CH, Pao W (2007) MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci U S A 104(52):20932-20937. doi:10.1073/pnas.0710370104
32. Engelman JA, Zejnullahu K, Mitsudomi T, Song Y, Hyland C, Park JO, Lindeman N, Gale CM, Zhao X, Christensen J, Kosaka T, Holmes AJ, Rogers AM, Cappuzzo F, Mok T, Lee C, Johnson BE, Cantley LC, Janne PA (2007) MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316(5827):1039-1043. doi:10.1126/science.1141478 (Pubitemid 46799492)