Effect of IN-1130, a Small Molecule Inhibitor of Transforming Growth Factor-β Type I Receptor/Activin Receptor-Like Kinase-5, on Prostate Cancer Cells

Journal of Urology

Volumn 180, Issue 6, 2008, Pages 2660-2667

  Lee, Geun Taek ^a   Hong, Jun Hyuk ^a   Mueller, Thomas J ^a   Watson, John A ^a   Kwak, Cheol ^a   Sheen, Youn Young ^a   Kim, Dae Kee ^a   Kim, Seong Jin ^a   Kim, Isaac Yi ^a  

^a ROBERT WOOD JOHNSON MEDICAL SCHOOL   (United States)

Author keywords

3 ((5 (6 methylpyridin 2 yl) 4 (quinoxalin 6 yl) 1H imidazol 2 yl)methy l)benzamide; intercellular signaling peptides and proteins; prostate; prostatic neoplasms; transforming growth factor

Indexed keywords

IN 1130; PROTEIN INHIBITOR; SMAD2 PROTEIN; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL; CELL STRAIN HEPG2; CONTROLLED STUDY; DRUG STRUCTURE; HUMAN; HUMAN CELL; IMMUNOBLOTTING; IN VITRO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROSTATE CANCER;

ANIMALS; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; IMIDAZOLES; MALE; MICE; PROSTATIC NEOPLASMS; QUINOXALINES; TUMOR CELLS, CULTURED;

EID: 55649112720     PISSN: 00225347     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.juro.2008.08.008     Document Type: Article

References (21)

1. Roberts A.B., Frolik C.A., Anzano M.A., and Sporn M.B. Transforming growth factors from neoplastic and nonneoplastic tissues. Fed Proc 42 (1983) 2621
2. Kulkarni A.B., Huh C.G., Becker D., Geiser A., Lyght M., Flanders K.C., et al. Transforming growth factor beta 1 null mutation in mice causes excessive inflammatory response and early death. Proc Natl Acad Sci U S A 90 (1993) 770
3. Brabletz T., Pfeuffer I., Schorr E., Siebelt F., Wirth T., and Serfling E. Transforming growth factor beta and cyclosporin A inhibit the inducible activity of the interleukin-2 gene in T cells through a noncanonical octamer-binding site. Mol Cell Biol 13 (1993) 1155
4. Swain S.L., Huston G., Tonkonogy S., and Weinberg A. Transforming growth factor-beta and IL-4 cause helper T cell precursors to develop into distinct effector helper cells that differ in lymphokine secretion pattern and cell surface phenotype. J Immunol 147 (1991) 2991
5. Ranges G.E., Figari I.S., Espevik T., and Palladino Jr. M.A. Inhibition of cytotoxic T cell development by transforming growth factor beta and reversal by recombinant tumor necrosis factor alpha. J Exp Med 166 (1987) 991
6. Wahl S.M., Hunt D.A., Wakefield L.M., McCartney-Francis N., Wahl L.M., Roberts A.B., et al. Transforming growth factor type beta induces monocyte chemotaxis and growth factor production. Proc Natl Acad Sci U S A 84 (1987) 5788
7. Ding A., Nathan C.F., Graycar J., Derynck R., Stuehr D.J., and Srimal S. Macrophage deactivating factor and transforming growth factors-beta 1 -beta 2 and -beta 3 inhibit induction of macrophage nitrogen oxide synthesis by IFN-gamma. J Immunol 145 (1990) 940
8. Franzen P., ten Dijke P., Ichijo H., Yamashita H., Schulz P., Heldin C.H., et al. Cloning of a TGF beta type I receptor that forms a heteromeric complex with the TGF beta type II receptor. Cell 75 (1993) 681
9. Massague J. TGFbeta signaling: receptors, transducers, and Mad proteins. Cell 85 (1996) 947
10. Derynck R., and Zhang Y.E. Smad-dependent and Smad-independent pathways in TGF-beta family signalling. Nature 425 (2003) 577
11. Kim I.Y., Ahn H.J., Lang S., Oefelein M.G., Oyasu R., Kozlowski J.M., et al. Loss of expression of transforming growth factor-beta receptors is associated with poor prognosis in prostate cancer patients. Clin Cancer Res 4 (1998) 1625
12. Moon J.A., Kim H.T., Cho I.S., Sheen Y.Y., and Kim D.K. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int 70 (2006) 1234
13. Laping N.J., Grygielko E., Mathur A., Butter S., Bomberger J., Tweed C., et al. Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542. Mol Pharmacol 62 (2002) 58
14. Jonk L.J., Itoh S., Heldin C.H., ten Dijke P., and Kruijer W. Identification and functional characterization of a Smad binding element (SBE) in the JunB promoter that acts as a transforming growth factor-beta, activin, and bone morphogenetic protein-inducible enhancer. J Biol Chem 273 (1998) 21145
15. Korchynskyi O., and ten Dijke P. Identification and functional characterization of distinct critically important bone morphogenetic protein-specific response elements in the Id1 promoter. J Biol Chem 277 (2002) 4883
16. Jornvall H., Blokzijl A., ten Dijke P., and Ibanez C.F. The orphan receptor serine/threonine kinase ALK7 signals arrest of proliferation and morphological differentiation in a neuronal cell line. J Biol Chem 276 (2001) 5140
17. DaCosta Byfield S., Major C., Laping N.J., and Roberts A.B. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol 65: (2004) 744
18. Baron V., De Gregorio G., Krones-Herzig A., Virolle T., Calogero A., Urcis R., et al. Inhibition of Egr-1 expression reverses transformation of prostate cancer cells in vitro and in vivo. Oncogene 22 (2003) 4194
19. Shah A.H., Tabayoyong W.B., Kundu S.D., Kim S.J., Van Parijs L., Liu V.C., et al. Suppression of tumor metastasis by blockade of transforming growth factor beta signaling in bone marrow cells through a retroviral-mediated gene therapy in mice. Cancer Res 62 (2002) 7135
20. Sawyer J.S., Anderson B.D., Beight D.W., Campbell R.M., Jones M.L., Herron D.K., et al. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. J Med Chem 46 (2003) 3953
21. Uhl M., Aulwurm S., Wischhusen J., Weiler M., Ma J.Y., Almirez R., et al. SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res 64 (2004) 7954