Targeting c-MET by LY2801653 for treatment of cholangiocarcinoma

Molecular Carcinogenesis

Volumn 55, Issue 12, 2016, Pages 2037-2050

  Barat, Samarpita ^a   Bozko, Przemyslaw ^a   Chen, Xi ^a   Scholta, Tim ^a   Hanert, Franziska ^a   Götze, Julian ^a   Malek, Nisar P ^a   Wilkens, Ludwig ^b   Plentz, Ruben R ^a  

^a UNIVERSITY HOSPITAL TÜBINGEN   (Germany)

^b NORDSTADT HOSPITAL   (Germany)

Author keywords

c MET; cholangiocarcinoma; LY2801653; p MET; small molecule inhibitor

Indexed keywords

BETA GALACTOSIDASE; MERESTINIB; MITOGEN ACTIVATED PROTEIN KINASE; PROTEIN KINASE B; SCATTER FACTOR RECEPTOR; STAT3 PROTEIN; ANTINEOPLASTIC AGENT; INDAZOLE DERIVATIVE; N-(3-FLUORO-4-((1-METHYL-6-(1H-PYRAZOL-4-YL)-1H-INDAZOL-5 YL)OXY)PHENYL)-1-(4-FLUOROPHENYL)-6-METHYL-2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE; NICOTINAMIDE; PROTEIN KINASE INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; BILE DUCT CARCINOMA; CANCER THERAPY; CELL AGING; CELL INVASION; CELL MIGRATION; CELL PROLIFERATION; CLINICAL EFFECTIVENESS; CLINICAL EVALUATION; COHORT ANALYSIS; COLONY FORMATION; CONTROLLED STUDY; DOWN REGULATION; ENZYME INHIBITION; FEMALE; HUMAN; HUMAN CELL; HUMAN TISSUE; HYPOXIA; IN VITRO STUDY; IN VIVO STUDY; MAJOR CLINICAL STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; PROTEIN TARGETING; SENESCENCE; TUMOR GROWTH; TUMOR XENOGRAFT; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; BILE DUCT; BILE DUCT TUMOR; DRUG EFFECTS; METABOLISM; MOLECULARLY TARGETED THERAPY; NUDE MOUSE; PATHOLOGY; PREVENTION AND CONTROL; SIGNAL TRANSDUCTION; TUMOR CELL LINE; TUMOR INVASION;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; BILE DUCT NEOPLASMS; BILE DUCTS; CELL LINE, TUMOR; CELL PROLIFERATION; CHOLANGIOCARCINOMA; FEMALE; HUMANS; INDAZOLES; MICE, NUDE; MOLECULAR TARGETED THERAPY; NEOPLASM INVASIVENESS; NIACINAMIDE; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MET; SIGNAL TRANSDUCTION;

EID: 84954285702     PISSN: 08991987     EISSN: 10982744     Source Type: Journal    
DOI: 10.1002/mc.22449     Document Type: Article

References (47)

1. Gatto M, Alvaro D. New insights on cholangiocarcinoma. World J Gastrointest Oncol 2010; 2:36–145.
2. Welzel TM, McGlynn KA, Hsing AW, O'Brien TR, Pfeiffer RM. Impact of classification of hilar cholangiocarcinomas (Klatskin tumors) on the incidence of intra- and extrahepatic cholangiocarcinoma in the United States. J Natl Cancer Inst 2006; 98:873–875.
3. Von Hahn T, Ciesek S, Wegener G, et al. Epidemiological trends in incidence and mortality of hepatobiliary cancers in Germany. Scand J Gastroenterol 2011; 46:1092–1098.
4. Tyson GL, El-Serag HB. Risk factors for cholangiocarcinoma. Hepatology 2011; 54:173–184.
5. Shaib Y, El-Serag HB. The epidemiology of cholangiocarcinoma. Semin Liver Dis 2004; 24:115–125.
6. El Khatib M, Kalnytska A, Palagani V, et al. Inhibition of hedgehog signaling attenuates carcinogenesis in vitro and increases necrosis of cholangiocellular carcinoma. Hepatology 2013b; 57:1035–1045.
7. El Khatib M, Bozko P, Palagani V, Malek NP, Wilkens L, Plentz RR. Activation of Notch signaling is required for cholangiocarcinoma progression and is enhanced by inactivation of p53 in vivo. PLoS ONE 2013a; 8:e77433.
8. Valle JW, Wasan H, Palmer DH, et al. Cisplatin plus gemcitabine versus gemcitabine for biliary tract cancer. N Engl J Med 2010; 362:1273–1281.
9. Birchmeier C, Birchmeier W, Gherardi E, Vande Woude GF. Met, metastasis, motility and more. Nat Rev Mol Cell Biol 2003; 4:915–925.
10. Gao CF, Woude GF. Vande: HGF/SF-Met signaling in tumor progression. Cell Res 2005; 15:49–51.
11. Danilkovitch-Miagkova A, Zbar B. Dysregulation of Met receptortyrosine kinase activity in invasive tumors. J Clin Invest 2002; 109:863–867.
12. Ma PC, Maulik G, Christensen J, Salgia R. C-Met: Structure, functions and potential for therapeutic inhibition. Cancer Metastasis Rev 2003; 22:309–325.
13. Knowles LM, Stabile LP, Egloff AM, et al. HGF and c-Met participate in paracrine tumorigenic pathways in head and neck squamous cell cancer. Clin Cancer Res 2009; 15:3740–3750.
14. Lengyel E, Prechtel D, Resau JH, et al. C-Met overexpression in node-positive breast cancer identifies patients with poor clinical outcome independent of Her2/neu. Int J Cancer 2005; 113:678–682.
15. Tokunou M, Niki T, Eguchi K, et al. C-MET expression in myofibroblasts: Role in autocrine activation and prognostic significance in lung adenocarcinoma. Am J Pathol 2011; 58:1451–1463.
16. Olivero M, Rizzo M, Madeddu R, et al. Overexpression and activation of hepatocyte growth factor/scatter factor in human non-small-cell lung carcinomas. Br J Cancer 1996; 74:1862–1868.
17. Koochekpour S, Jeffers M, Rulong S, et al. Met and hepatocyte growth factor/scatter factor expression in human gliomas. Cancer Res 1997; 57:5391–5398.
18. Di Renzo MF, Olivero M, Giacomini A, et al. Overexpression and amplification of the met/HGF receptor gene during the progression of colorectal cancer. Clin Cancer Res 1995; 1:147–154.
19. Furukawa T, Duguid WP, Kobari M, Matsuno S, Tsao MS. Hepatocyte growth factor and Met receptor expression in human pancreatic carcinogenesis. Am J Pathol 1995; 147:889–895.
20. Soman NR, Correa P, Ruiz BA, Wogan GN. The TPR-MET oncogenic rearrangement is present and expressed in human gastric carcinoma and precursor lesions. Proc Natl Acad Sci USA 1991; 88:4892–4896.
21. Houldsworth J, Cordon-Cardo C, Ladanyi M, Kelsen DP, Chaganti RS. Gene amplification in gastric and esophageal adenocarcinomas. Cancer Res 1990; 50:6417–6422.
22. Crosswell HE, Dasgupta A, Alvarado CS, et al. PHA665752, a small-molecule inhibitor of c-Met, inhibits hepatocyte growth factor-stimulated migration and proliferation of c-Met-positive neuroblastoma cells. BMC Cancer 2009; 9:411.
23. 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; 67:3529–3534.
24. You H, Ding W, Dang H, Jiang Y, Rountree CB. C-MET represents a potential therapeutic target for personalized treatment in hepatocellular carcinoma. Hepatology 2011; 54:879–889.
25. Sierra JR, Tsao MS. C-MET as a potential therapeutic target and biomarker in cancer. Ther Adv Med Oncol 2011; 3:S21–S35.
26. Hida Y, Morita T, Fujita M, et al. Clinical significance of hepatocyte growth factor and c-Met expression in extrahepatic biliary tract cancers. Oncol Rep 1999; 6:1051–1056.
27. Hammond DE, Carter S, Clague MJ. Met receptor dynamics and signalling. Curr Topics Microbiol Immunol 2004; 286:21–44.
28. Furge KA, Zhang YW, Woude GF. Vande: Met receptor tyrosine kinase: Enhanced signaling through adapter proteins. Oncogene 2000; 19:5582–5589.
29. Goyal L, Muzumdar MD, Zhu AX. Targeting the HGF/c-MET pathway in hepatocellular carcinoma. Clin Cancer Res 2013; 19:2310–2318.
30. Organ SL, Tsao MS. An overview of the c-MET signaling pathway. Ther Adv Med Oncol 2011; 3:7–19.
31. Comoglio PM, Giordano A, Trusolino L. Drug development of MET inhibitors: Targeting oncogene addiction and expedience. Nat Rev Drug Disc 2008; 7:504–516.
32. Terada T, Nakanuma Y, Sirica AE. Immunohistochemical demonstration of MET overexpression in human intrahepatic cholangiocarcinoma and in hepatolithiasis. Hum Pathol 1998; 29:175–180.
33. Farazi PA, Zeisberg M, Glickman J, Zhang Y, Kalluri R, DePinho RA. Chronic bile duct injury associated with fibrotic matrix microenvironment provokes cholangiocarcinoma in p53-deficient mice. Cancer Res 2006; 66:6622–6627.
34. Radaeva S, Ferreira-Gonzalez A, Sirica AE. Overexpression of C-NEU and C-MET during rat liver cholangiocarcinogenesis: A link between biliary intestinal metaplasia and mucin-producing cholangiocarcinoma. Hepatology 1999; 29:1453–1462.
35. Leelawat K, Leelawat S, Tepaksorn P, et al. Involvement of c-Met/hepatocyte growth factor pathway in cholangiocarcinoma cell invasion and its therapeutic inhibition with small interfering RNA specific for c-Met. J Surg Res 2006; 136:78–84.
36. Miyamoto M, Ojima H, Iwasaki M, et al. Prognostic significance of overexpression of c-Met oncoprotein in cholangiocarcinoma. Br J Cancer 2011; 105:131–138.
37. Zender S, Nickeleit I, Wuestefeld T, et al. A critical role for Notch signaling in the formation of cholangiocellular carcinomas. Cancer Cell 2013; 23:784–795.
38. Aishima SI, Taguchi KI, Sugimachi K, Shimada M, Sugimachi K, Tsuneyoshi M. C-erbB-2 and c-Met expression relates to cholangiocarcinogenesis and progression of intrahepatic cholangiocarcinoma. Histopathology 2002; 40:269–278.
39. Kong Y, Cui H, Ramkumar C, Zhang H. Regulation of senescence in cancer and aging. J Aging Res 2011; 2011:963172.
40. Romanov VS, Abramova MV, Svetlikova SB, et al. P21(Waf1) is required for cellular senescence but not for cell cycle arrest induced by the HDAC inhibitor sodium butyrate. Cell Cycle 2010; 9:3945–3955.
41. Yan SB, Peek VL, Ajamie R, et al. LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs 2013; 31:833–844.
42. Wu W, Bi C, Credille KM, Manro JR, et al. Inhibition of tumor growth and metastasis in non-small cell lung cancer by LY 2801 653, an inhibitor of several oncokinases, including MET. Clin Cancer Res 2013; 19:5699–5710.
43. Kawada I, Hasina R, Arif Q, et al. Dramatic antitumor effects of the dual MET/RON small-molecule inhibitor LY2801653 in non-small cell lung cancer. Cancer Res 2014; 74:884–895.
44. Cantwell-Dorris ER, O'Leary JJ, Sheils OM. BRAFV600E: Implications for carcinogenesis and molecular therapy. Mol Cancer Ther 2011; 10:385–394.
45. Xiong A, Yang Z, Shen Y, et al. Transcription factor STAT3 as a novel molecular target for cancer prevention. Cancers (Basel) 2014; 6:926–957.
46. Bid HK, Roberts RD, Manchanda PK, Houghton PJ. RAC1: An emerging therapeutic option for targeting cancer angiogenesis and metastasis. Mol Cancer Ther 2013; 12:1925–1934.
47. Eckerich C, Zapf S, Fillbrandt R, Loges S, Westphal M, Lamszus K. Hypoxia can induce c-Met expression in glioma cells and enhance SF/HGF-induced cell migration. Int J Cancer 2007; 121:276–283.