A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts

Cancer Research

Volumn 67, Issue 8, 2007, Pages 3529-3534

  Puri, Neelu ^a   Khramtsov, Andrey ^a   Ahmed, Salman ^a   Nallasura, Vidya ^a   Hetzel, Jeremy T ^a   Jagadeeswaran, Ramasamy ^a   Karczmar, Greg ^a   Salgia, Ravi ^a  

^a UNIVERSITY OF CHICAGO MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PHA 665752; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG;

ANGIOGENESIS; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CARCINOGENICITY; CATALYSIS; CONTROLLED STUDY; DRUG TARGETING; ENZYME INHIBITION; IMMUNOHISTOCHEMISTRY; LUNG CANCER; LUNG NON SMALL CELL CANCER; MOUSE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SOLID TUMOR; TUMOR VOLUME; XENOGRAFT;

ANIMALS; CARCINOMA, NON-SMALL-CELL LUNG; CARCINOMA, SMALL CELL; CELL GROWTH PROCESSES; CELL LINE, TUMOR; HUMANS; IMMUNOHISTOCHEMISTRY; INDOLES; LUNG NEOPLASMS; MALE; MICE; MICE, NUDE; NEOVASCULARIZATION, PATHOLOGIC; PROTO-ONCOGENE PROTEINS C-MET; SULFONES; THROMBOSPONDIN 1; VASCULAR ENDOTHELIAL GROWTH FACTOR A; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 34248575532     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-06-4416     Document Type: Article

References (20)

1. Jemal A, Siegel R, Ward E, Murray T, Xu J, Thun MJ. Cancer statistics, 2007. CA Cancer J Clin 2007;57:43-66.
2. Baselga J. Targeting tyrosine kinases in cancer: the second wave. Science 2006;312:1175-8.
3. Christensen JG, Burrows J, Salgia R. c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett 2005;225:1-26.
4. 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.
5. Ma PC, Kijima T, Maulik G, et al. c-MET mutational analysis in small cell lung cancer: novel juxtamembrane domain mutations regulating cytoskeletal functions. Cancer Res 2003;63:6272-81.
6. Maulik G, Shrikhande A, Kijima T, Ma PC, Morrison PT, Salgia R. Role of the hepatocyte growth factor receptor, c-Met, in oncogenesis and potential for therapeutic inhibition. Cytokine Growth Factor Rev 2002;13:41-59.
7. Christensen JG, Schreck R, Burrows J, et al. 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 2003;63:7345-55.
8. Bellusci S, Moens G, Gaudino G, et al. Creation of an hepatocyte growth factor/scatter factor autocrine loop in carcinoma cells induces invasive properties associated with increased tumorigenicity. Oncogene 1994;9: 1091-9.
9. Jeffers M, Rong S, Anver M, Vande Woude GF. Autocrine hepatocyte growth factor/scatter factor-Met signaling induces transformation and the invasive/ metastastic phenotype in C127 cells. Oncogene 1996; 13:853-6.
10. Takayama H, LaRochelle WJ, Sharp R, et al. Diverse tumorigenesis associated with aberrant development in mice overexpressing hepatocyte growth factor/scatter factor. Proc Natl Acad Sci U S A 1997;94:701-6.
11. Gallego MI, Bierie B, Hennighausen L. Targeted expression of HGF/SF in mouse mammary epithelium leads to metastatic adenosquamous carcinomas through the activation of multiple signal transduction pathways. Oncogene 2003;22:8498-508.
12. Kong-Beltran M, Stamos J, Wickramasinghe D. The Sema domain of Met is necessary for receptor dimerization and activation. Cancer Cell 2004;6:75-84.
13. Smolen GA, Sordella R, Muir B, et al. 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 2006;103:2316-21.
14. 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.
15. Saucier C, Khoury H, Lai KM, et al. The She adaptor protein is critical for VEGF induction by Met/HGF and ErbB2 receptors and for early onset of tumor angiogenesis. Proc Natl Acad Sci U S A 2004;101:2345-50.
16. 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.
17. Liu LT, Chang HC, Chiang LC, Hung WC. Histone deacetylase inhibitor up-regulates RECK to inhibit MMP-2 activation and cancer cell invasion. Cancer Res 2003;63:3069-72.
18. Wybenga-Groot LE, Baskin B, Ong SH, Tong J, Pawson T, Sicheri F. Structural basis for autoinhibition of the Ephb2 receptor tyrosine kinase by the unphosphorylated juxtamembrane region. Cell 2001;106:745-57.
19. Hellman A, Zlotorynski E, Scherer SW, et al. A role for common fragile site induction in amplification of human oncogenes. Cancer cell 2002;1:89-97.
20. Reiner A, Neumeister B, Spona J, Reiner G, Schemper M, Jakesz R. Immunocytochemical localization of estrogen and progesterone receptor and prognosis in human primary breast cancer. Cancer Res 1990;50:7057-61.