A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer

Cell Cycle

Volumn 8, Issue 15, 2009, Pages 2435-2443

  Hochwald, Steven N ^a   Nyberg, Carl ^a   Zheng, Min ^a   Zheng, Donghang ^a   Wood, Cheng ^a   Massoll, Nicole A ^a   Magis, Andrew ^a   Ostrov, David ^a   Cance, William G ^a   Golubovskaya, Vita M ^a  

^a ROSWELL PARK CANCER INSTITUTE   (United States)

Author keywords

Focal adhesion kinase; Pancreatic cancer; Small molecule inhibitor; Y15; Y397

Indexed keywords

1,2,4,5 BENZENETETRAAMINE TETRAHYDROCHLORIDE; FOCAL ADHESION KINASE; GEMCITABINE; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; AUTOPHOSPHORYLATION; CANCER CHEMOTHERAPY; CANCER GROWTH; CANCER INHIBITION; CELL ADHESION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOSE RESPONSE; DRUG STRUCTURE; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; NONHUMAN; PANCREAS CANCER; TIME; TUMOR REGRESSION;

EID: 68449092818     PISSN: 15384101     EISSN: 15514005     Source Type: Journal    
DOI: 10.4161/cc.8.15.9145     Document Type: Article

References (36)

1. Neito J, Grossbard ML, Kozuch P. Metastatic pancreatic cancer 2008: is the glass less empty? Oncologist 2008; 13:562-76.
2. Schaller MD, Borgman CA, Cobb BS, Vines RR, Reynolds AB, Parsons JT. pp125fak a structurally distinctive protein-tyrosine kinase associated with focal adhesions. Proc Natl Acad Sci USA 1992; 89:5192-6.
3. Kornberg LJ, Earp HS, Turner CE, Prockop C, Juliano RL. Signal transduction by integrins: increased protein tyrosine phosphorylation caused by clustering of beta 1 integrins. Proc Natl Acad Sci USA 1991; 88:8392-6.
4. Burridge K, Turner CE, Romer LH. Tyrosine phosphorylation of paxillin and pp125FAK accompanies cell adhesion to extracellular matrix: a role in cytoskeletal assembly. J Cell Biol 1992; 119:893-903.
5. Cary LA, Guan JL. Focal adhesion kinase in integrin-mediated signaling. Front Biosci 1999; 4:102-13.
6. Guan JL, Shalloway D. Regulation of focal adhesion-associated protein tyrosine kinase by both cellular adhesion and oncogenic transformation. Nature 1992; 358:690-2.
7. Eide BL, Turck CW, Escobedo JA. Identification of Tyr-397 as the primary site of tyrosine phosphorylation and pp60src association in the focal adhesion kinase, pp125FAK. Mol Cell Biol 1995; 15:2819-27.
8. Xing Z, Chen HC, Nowlen JK, Taylor SJ, Shalloway D, Guan JL. Direct interaction of v-Src with the focal adhesion kinase mediated by the Src SH2 domain. Mol Biol Cell 1994; 5:413-21.
9. Cobb BS, Schaller MD, Leu TH, Parsons JT. Stable association of pp60src and pp59fyn with the focal adhesion-associated protein tyrosine kinase, pp125FAK. Mol Cell Bio 1994; 14:147-55.
10. Schaller MD, Hildebrand JD, Shannon JD, Fox JW, Vines RR, Parsons JT. Autophosphorylation of the focal adhesion kinase, pp125FAK, directs SH2-dependent binding of pp60src. Mol Cell Bio 1994; 14:1680-8.
11. Hanks SK, Polte TR. Signaling through focal adhesion kinase. Bioessays 1997; 19:137-45.
12. Golubovskaya VM, Cance WG. Focal adhesion kinase and p53 signaling in cancer cells. Int Rev Cytol 2007; 263:103-53.
13. Xu LH, Owens LV, Sturge GC, Yang X, Liu ET, Craven RJ, et al. Attenuation of the expression of the focal adhesion kinase induces apoptosis in tumor cells. Cell Growth Differ 1996; 7:413-8.
14. Xu LH, Yang X, Craven RJ, Cance WG. The COOH-terminal domain of the focal adhesion kinase induces loss of adhesion and cell death in human tumor cells. Cell Growth Differ 1998; 9:999-1005.
15. Mahlamaki EH, Barlund M, Tanner M, Gorunova L, Hoglund M, Karhu R, et al. Frequent amplification of 8q24, 11q, 17q and 20q-specific genes in pancreatic cancer. Genes Chromosomes Cancer 2002; 35:353-8.
16. Duxbury MS, Ito H, Zinner MJ, Ashley SW, Whang EE. Focal adhesion kinase gene silencing promotes anoikis and suppresses metastasis of human pancreatic adenocarcinoma cells. Surgery 2004; 135:555-62.
17. Liu W, Bloom DA, Cance WG, Golubovskaya V, Kurenova E, Hochwald SN. FAK and IGF-IR interact to provide survival signals in human pancreatic adenocarcinoma cells. Carcinogenesis 2008; 29:1096-107.
18. McLean GW, Carragher NO, Avizienyte E, Evans J, Brunton VG, Frame MC. The role of focal-adhesion kinase in cancer - a new therapeutic opportunity. Nat Rev Cancer 2005; 5:505-15.
19. Shi Q, Hjelmeland AB, Keir ST, Song L, Wickman S, Jackson D, et al. A novel low-molecular weight inhibitor of focal adhesion kinase, TAE226, inhibits glioma growth. Mol Carcinog 2007; 46:488-96.
20. Golubovskaya VM, Virnig C, Cance WG. TAE226-Induced apoptosis in breast cancer cells with overexpressed Src or EGFR. Mol Carcinog 2008; 47:222-34.
21. Liu TJ, LaFortune T, Honda T, Ohmori O, Hatakeyama S, Meyer T, et al. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther 2007; 6:1357-67.
22. Sandberg EM, Ma X, He K, Frank SJ, Ostrov DA, Sayeski PP. Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of jak2 tyrosine kinase autophosphorylation [correction of autophophorylation]. J Med Chem 2005; 48:2526-33.
23. Golubovskaya VM, Nyberg C, Zheng M, Kweh F, Magis A, Ostrov D, et al. A small molecule inhibitor 1,2,4,5-Benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumor growth. J Med Chem 2008; 51:7405-16.
24. Ceccarelli DF, Song HK, Poy F, Schaller MD, Eck MJ. Crystal structure of the FERM domain of focal adhesion kinase. J Biol Chem 2006; 281:252-9.
25. Golubovskaya VM, Finch R, Cance WG. Direct interaction of the N-terminal domain of focal adhesion kinase with the N-terminal transactivation domain of p53. J Biol Chem 2005; 280:25008-21.
26. Goluboskaya VM, Beviglia L, Xu LH, Earp HS, Craven R, Cance WG. Dual inhibition of focal adhesion kinase and epidermal growth factor receptor pathways cooperatively induces death receptor-mediated apoptosis in human breast cancer cells. J Biol Chem 2002; 277:38978-87.
27. Sultana A, Tudur Smith C, Cunningham D, Starling N, Neoptolemos JP, Ghaneh P. Meta-analyses of chemotherapy for locally advanced and metastatic pancreatic cancer: results of secondary end points analyses. Br J Cancer 2008; 99:6-13.
28. Schlaepfer DD, Hunter T. Integrin signaling and tyrosine phosphorylation: just the FAKs? Trends Cell Biol 1998; 8:151-7.
29. Schlaepfer DD, Jones KC, Hunter T. Multiple Grb2-mediated integrin-stimulated signaling pathways to ERK2/mitogen-activated protein kinase: summation of both c-Srcand focal adhesion kinase-initiated tyrosine phosphorylation events. Mol Cell Biol 1998; 18:2571-85.
30. Frisch SM, Vuori K, Ruoslahti E, Chan-Hui PY. Control of adhesion-dependent cell survival by focal adhesion kinase. J Cell Biol 1996; 134:793-9.
31. Ilic D, Almeida EAC, Schlaepfer DD, Dazin P, Aizawa S, Damsky CH. Extracellular matrix survival signals transduced by focal adhesion kinase suppress p53-mediated apoptosis. J Cell Biol 1998; 143:547-60.
32. Cary LA, Chang JF, Guan JL. Stimulation of cell migration by overexpression of focal adhesion kinase and its association with Src and Fyn. J Cell Sci 1996; 109:1787-94.
33. Ilic D, Kanazawa S, Furuta Y, Yamamoto T, Aizawa S. Impairment of mobility in endodermal cells by FAK deficiency. Exp Cell Res 1996; 222:298-303.
34. Halder J, Lin YG, Merritt WM, Spannuth WA, Nick AM, Honda T, et al. Therapeutic efficacy of a novel focal adhesion kinase inhibitor TAE226 in ovarian carcinoma. Cancer Res 2007; 67:10976-83.
35. Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res 2008; 68:1935-44.
36. Golubovskaya VM, Finch R, Kweh F, Massoll NA, Campbell-Thompson M, Wallace MR, et al. p53 regulates FAK expression in human tumor cells. Mol Carcinog 2007; 47:373-82.