Progressive transforming growth factor β1-induced lung fibrosis is blocked by an orally active ALK5 kinase inhibitor

American Journal of Respiratory and Critical Care Medicine

Volumn 171, Issue 8, 2005, Pages 889-898

  Bonniaud, Philippe ^b   Margetts, Peter J ^b   Kolb, Martin ^b   Schroeder, Jane Ann ^b   Kapoun, Ann M ^b   Damm, Debby ^b   Murphy, Alison ^b   Chakravarty, Sarvajit ^b   Dugar, Sundeep ^b   Higgins, Linda ^b   Protter, Andrew A ^b   Gauldie, Jack ^a  

^a MCMASTER UNIVERSITY   (Canada)

^b NONE

Author keywords

Fibrogenesis; Interstitial lung fibrosis; Matrix; TGF receptor

Indexed keywords

ACTIVIN RECEPTOR; PHOSPHOTRANSFERASE INHIBITOR; PTERIDINE DERIVATIVE; SD 208; TRANSFORMING GROWTH FACTOR BETA RECEPTOR; TRANSFORMING GROWTH FACTOR BETA1;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; ENZYME ACTIVITY; FEMALE; FIBRIN FORMATION; GENE EXPRESSION; GENE TRANSFER; IC 50; IN VITRO STUDY; LUNG FIBROSIS; LUNG LAVAGE; MOLECULAR WEIGHT; NONHUMAN; PRIORITY JOURNAL; RAT;

ACTIVIN RECEPTORS, TYPE I; ADMINISTRATION, ORAL; ANIMALS; CELLS, CULTURED; DOWN-REGULATION; FEMALE; FIBROBLASTS; LUNG; OLIGONUCLEOTIDE ARRAY SEQUENCE ANALYSIS; PROTEIN KINASE INHIBITORS; PTERIDINES; PULMONARY FIBROSIS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, TRANSFORMING GROWTH FACTOR BETA; TRANSFORMING GROWTH FACTOR BETA; TRANSFORMING GROWTH FACTOR BETA1; UP-REGULATION;

EID: 20244383986     PISSN: 1073449X     EISSN: None     Source Type: Journal    
DOI: 10.1164/rccm.200405-612OC     Document Type: Article

References (44)

1. Crystal RG, Bitterman PB, Mossman B, Schwarz MI, Sheppard D, Almasy L, Chapman HA, Friedman SL, King TE Jr, Leinwand LA, et al. Future research directions in idiopathic pulmonary fibrosis: summary of a National Heart, Lung, and Blood Institute working group. Am J Respir Crit Care Med 2002;166:236-246.
2. American Thoracic Society. Idiopathic pulmonary fibrosis: diagnosis and treatment. International consensus statement: American Thoracic Society (ATS), and the European Respiratory Society (ERS). Am J Respir Crit Care Med 2000;161:646-664.
3. Ziesche R, Hofbauer E, Wittmann K, Petkov V, Block LH. A preliminary study of long-term treatment with interferon gamma-1b and low-dose prednisolone in patients with idiopathic pulmonary fibrosis. N Engl J Med 1999;341:1264-1269.
4. Gauldie J. Pro: inflammatory mechanisms are a minor component of the pathogenesis of idiopathic pulmonary fibrosis. Am J Respir Crit Care Med 2002;165:1205-1206.
5. Keane MP, Strieter RM. The importance of balanced pro-inflammatory and anti-inflammatory mechanisms in diffuse lung disease. Respir Res 2002;3:5.
6. Kelly M, Kolb M, Bonniaud P, Gauldie J. A re-evaluation of fibrogenic cytokines in lung fibrosis. Curr Pharm Des 2003;9:39-49.
7. Sime PJ, Xing Z, Graham FL, Csaky KG, Gauldie J. Adenovector-mediated gene transfer of active transforming growth factor-betal induces prolonged severe fibrosis in rat lung. J Clin Invest 1997;100: 768-776.
8. Wang Q, Wang Y, Hyde DM, Gotwals PJ, Koteliansky VE, Ryan ST, Giri SN. Reduction of bleomycin induced lung fibrosis by transforming growth factor beta soluble receptor in hamsters. Thorax 1999;54:805-812.
9. Dennler S, Goumans MJ, ten Dijke P. Transforming growth factor beta signal transduction. J Leukoc Biol 2002;71:731-740.
10. Derynck R, Feng XH. TGF-beta receptor signaling. Biochim Biophys Acta 1997;1333:F105-F150.
11. Goumans MJ, Valdimarsdottir G, Itoh S, Rosendahl A, Sideras P, ten Dijke P. Balancing the activation state of the endothelium via two distinct TGF-beta type I receptors. EMBO J 2002;21:1743-1753.
12. Roberts AB. The ever-increasing complexity of TGF-beta signaling. Cytokine Growth Factor Rev 2002;13:3-5.
13. Roberts AB, Piek E, Bottinger EP, Ashcroft G, Mitchell JB, Flanders KC. Is Smad3 a major player in signal transduction pathways leading to fibrogenesis? Chest 2001;120:43S-47S.
14. Bonniaud P, Kolb M, Galt T, Robertson J, Robbins C, Stampfli M, Lavery C, Margetts PJ, Roberts AB, Gauldie J. Smad3 null mice develop airspace enlargement and are resistant to TGF-beta-mediated pulmonary fibrosis. J Immunol 2004;173:2099-2108.
15. Bonniaud P, Margetts PJ, Kolb M, Kapoun AM, Protter AA, Gauldie J. TGF-beta1 receptor I inhibitor, SD-208, dramatically inhibits lung fibrosis induced by TGF-beta1 overexpression in rat lungs [abstract]. Am J Respir Crit Care Med 2003;167:A167.
16. Bonniaud P, Margetts PJ, Kolb M, Kapoun AM, Protter AA, Gauldie J. SD-208 an orally active TGF-beta1 receptor antagonist inhibits TGF-beta1 induced progressive lung fibrosis in rat [abstract]. Eur Respir Soc 2003;22:531S.
17. Bett AJ, Haddara W, Prevec L, Graham FL. An efficient and flexible system for construction of adenovirus vectors with insertions or deletions in early regions 1 and 3. Proc Natl Acad Sci USA 1994;91:8802-8806.
18. Kolb M, Bonniaud P, Galt T, Sime PJ, Kelly MM, Margetts PJ, Gauldie J. Differences in the fibrogenic response after transfer of active transforming growth factor-betal gene to lungs of "fibrosis-prone" and "fibrosis-resistant" mouse strains. Am J Respir Cell Mol Biol 2002;27:141-150.
19. Kolb M, Margetts PJ, Anthony DC, Pitossi F, Gauldie J. Transient expression of IL-1beta induces acute lung injury and chronic repair leading to pulmonary fibrosis. J Clin Invest 2001;107:1529-1536.
20. Stegemann H, Stalder K. Determination of hydroxyproline. Clin Chim Acta 1967;18:267-273.
21. Kolb M, Margetts PJ, Galt T, Sime PJ, Xing Z, Schmidt M, Gauldie J. Transient transgene expression of decorin in the lung reduces the fibrotic response to bleomycin. Am J Respir Crit Care Med 2001;163: 770-777.
22. Kapoun AM, Liang F, O'Young G, Damm DL, Quon D, White RT, Munson K, Lam A, Schreiner GF, Protter AA. B-type natriuretic peptide exerts broad functional opposition to transforming growth factor-beta in primary human cardiac fibroblast. Circ Res 2004;94:453-461.
23. King TE Jr, Schwarz MI, Brown K, Tooze JA, Colby TV, Waldron JA Jr, Flint A, Thurlbeck W, Cherniack RM. Idiopathic pulmonary fibrosis: relationship between histopathologic features and mortality. Am J Respir Crit Care Med 2001;164:1025-1032.
24. Gauldie J, Kolb M, Sime PJ. A new direction in the pathogenesis of idiopathic pulmonary fibrosis? Respir Res 2002;3:1.
25. Collard HR, King TE Jr. Treatment of idiopathic pulmonary fibrosis: the rise and fall of corticosteroids. Am J Med 2001;110:326-328.
26. Albanis E, Safadi R, Friedman SL. Treatment of hepatic fibrosis: almost there. Curr Gastroenterol Rep 2003;5:48-56.
27. Yu L, Noble NA, Border WA. Therapeutic strategies to halt renal fibrosis. Curr Opin Pharmacol 2002;2:177-181.
28. Wells RG. Fibrogenesis: V. TGF-beta signaling pathways. Am J Physiol Gastrointest Liver Physiol 2000;279:G845-G850.
29. Lasky JA, Brody AR. Interstitial fibrosis and growth factors. Environ Health Perspect 2000;108:751-762.
30. Santana A, Saxena B, Noble NA, Gold LI, Marshall BC. Increased expression of transforming growth factor beta isoforms (beta 1, beta 2, beta 3) in bleomycin-induced pulmonary fibrosis. Am J Respir Cell Mol Biol 1995;13:34-44.
31. Giri SN, Hyde DM, Hollinger MA. Effect of antibody to transforming growth factor beta on bleomycin induced accumulation of lung collagen in mice. Thorax 1993;48:959-966.
32. Nakao A, Fujii M, Matsumura R, Kumano K, Saito Y, Miyazono K, Iwamoto I. Transient gene transfer and expression of Smad7 prevents bleomycin-induced lung fibrosis in mice. J Clin Invest 1999;104:5-11.
33. Zhao J, Shi W, Wang YL, Chen H, Bringas P Jr, Datto MB, Frederick JP, Wang XF, Warburton D. Smad3 deficiency attenuates bleomycin-induced pulmonary fibrosis in mice. Am J Physiol Lung Cell Mol Physiol 2002;282:L585-L593.
34. Tran TT, Ma JY, Li Z, Chakravarty S, McEnroe G, Murphy A, Dugar S, Lam A, Liu DY, Scheiner G, et al. A small molecule orally active TGF-b-R1 kinase inhibitor, SD-208, reduces profibrotic gene expression and biochemical and morphological markers of fibrosis in the rat bleomycin model of pulmonary fibrosis [abstract]. Am J Respir Crit Care Med 2003;167:A666.
35. Pardo A, Ruiz V, Arreola JL, Ramirez R, Cisneros-Lira J, Gaxiola M, Barrios R, Kala SV, Lieberman MW, Selman M. Bleomycin-induced pulmonary fibrosis is attenuated in gamma-glutamyl transpeptidase-deficient mice. Am J Respir Crit Care Med 2003;167:925-932.
36. Cailes JB, O'Connor CM, Pantelidis P, Southcott AM, Fitzgerald M, Black CM, Du Bois RM. Neutrophil activation in fibrosing alveolitis: a comparison of lone cryptogenic fibrosing alveolitis and systemic sclerosis. Eur Respir J 1996;9:992-999.
37. Branton MH, Kopp JB. TGF-beta and fibrosis. Microbes Infect 1999;1:1349-1365.
38. Martin M, Lefaix J, Delanian S. TGF-beta1 and radiation fibrosis: a master switch and a specific therapeutic target? Int J Radiat Oncol Biol Phys 2000;47:277-290.
39. McAnulty RJ, Laurent GJ. Pathogenesis of lung fibrosis and potential new therapeutic strategies. Exp Nephrol 1995;3:96-107.
40. Nagase H, Woessner JF Jr. Matrix metalloproteinases. J Biol Chem 1999; 274:21491-21494.
41. Selman M, King TE, Pardo A. Idiopathic pulmonary fibrosis: prevailing and evolving hypotheses about its pathogenesis and implications for therapy. Ann Intern Med 2001;134:1.36-151.
42. Selman M, Ruiz V, Cabrera S, Segura L, Ramirez R, Barrios R, Pardo A. TIMP-1, -2, -3, and -4 in idiopathic pulmonary fibrosis: a prevailing nondegradative lung microenvironment? Am J Physiol Lung Cell Mol Physiol 2000;279:L562-L574.
43. Bonniaud P, Martin G, Margetts PJ, Ask K, Robertson J, Gauldie J, Kolb M. Connective tissue growth factor is crucial to inducing a profibrotic environment in fibrosis-resistant BALB/c mouse lungs. Am J Respir Cell Mol Biol 2004;31:510-516.
44. Rice AB, Moomaw CR, Morgan DL, Bonner JC. Specific inhibitors of platelet-derived growth factor or epidermal growth factor receptor tyrosine kinase reduce pulmonary fibrosis in rats. Am J Pathol 1999;155:213-221.