Oral administration of gw788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in chagas disease

PLoS Neglected Tropical Diseases

Volumn 6, Issue 6, 2012, Pages

  de Oliveira, Fabiane L ^a   Araújo Jorge, Tania C ^a   de Souza, Elen M ^a   de Oliveira, Gabriel M ^a   Degrave, Wim M ^a   Feige, Jean Jacques ^b,c,d   Bailly, Sabine ^b,c,d   Waghabi, Mariana C ^a  

^a INSTITUTO OSWALDO CRUZ   (Brazil)

^b INSERM   (France)

^c UNIV GRENOBLE ALPES   (France)

^d CEA GRENOBLE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 [3 (PYRIDIN 2 YL) 1H PYRAZOL 4 YL] PYRIDIN 2 YL) N (TETRAHYDRO 2HPYRAN 4 YL) BENZAMIDE; ALANINE AMINOTRANSFERASE; ASPARTATE AMINOTRANSFERASE; COLLAGEN TYPE 1; CONNEXIN 43; FIBRONECTIN; GW788388; TRANSFORMING GROWTH FACTOR BETA; TRANSFORMING GROWTH FACTOR BETA INHIBITOR; UNCLASSIFIED DRUG; UREA; 4 (4 (3 (PYRIDIN 2 YL) 1H PYRAZOL 4 YL)PYRIDIN 2 YL) N (TETRAHYDRO 2H PYRAN 4 YL)BENZAMIDE; 4-(4-(3-(PYRIDIN-2-YL)-1H-PYRAZOL-4-YL)PYRIDIN-2-YL)-N-(TETRAHYDRO-2H-PYRAN-4-YL)BENZAMIDE; BENZAMIDE DERIVATIVE; PYRAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CHAGAS DISEASE; CONTROLLED STUDY; ELECTROCARDIOGRAPHY; HEART CONDUCTION; HEART INJURY; HEART MUSCLE FIBROSIS; HEART RATE; HISTOPATHOLOGY; IMMUNOBLOTTING; IMMUNOHISTOCHEMISTRY; MALE; MOUSE; NONHUMAN; PARASITEMIA; PR INTERVAL; PROTEIN EXPRESSION; QRS COMPLEX; QT INTERVAL; SIGNAL TRANSDUCTION; SURVIVAL; SURVIVAL RATE; TRYPANOSOMA CRUZI; WESTERN BLOTTING; ANIMAL; DISEASE MODEL; DRUG ANTAGONISM; FIBROSIS; HEART MUSCLE; ORAL DRUG ADMINISTRATION; PATHOGENICITY; PATHOLOGY; TREATMENT OUTCOME;

ADMINISTRATION, ORAL; ANIMALS; BENZAMIDES; CHAGAS CARDIOMYOPATHY; DISEASE MODELS, ANIMAL; FIBROSIS; MALE; MICE; MYOCARDIUM; PYRAZOLES; TRANSFORMING GROWTH FACTOR BETA; TREATMENT OUTCOME; TRYPANOSOMA CRUZI;

EID: 84863669381     PISSN: 19352727     EISSN: 19352735     Source Type: Journal    
DOI: 10.1371/journal.pntd.0001696     Document Type: Article

References (42)

1. Jannin J, Villa L, (2007) An overview of Chagas disease treatment. Mem Inst Oswaldo Cruz 102: 95-97.
2. Rassi A Jr, Rassi A, Little WC, (2000) Chagas' heart disease. Clin Cardiol 23: 883-889.
3. Coura J, de Castro S, (2002) A critical review on Chagas disease chemotherapy. Mem Inst Oswaldo Cruz 97: 3-24.
4. Marin-Neto JA, Rassi A Jr, Avezum A Jr, Mattos AC, Rassi A, et al. (2009) The BENEFIT trial: testing the hypothesis that trypanocidal therapy is beneficial for patients with chronic Chagas heart disease. Mem Inst Oswaldo Cruz 104: 319-324.
5. Roberts AB, Flanders KC, Heine UI, Jakowlew S, Kondaiah P, et al. (1990) Transforming growth factor-beta: multifunctional regulator of differentiation and development. Philos Trans R Soc Lond B Biol Sci 327: 145-154.
6. Massague J, Gomis RR, (2006) The logic of TGFbeta signaling. FEBS Lett 580: 2811-2820.
7. Reed SG, (1999) TGF-beta in infections and infectious diseases. Microbes Infect 1: 1313-1325.
8. Araujo-Jorge TC, Waghabi MC, Soeiro Mde N, Keramidas M, Bailly S, et al. (2008) Pivotal role for TGF-beta in infectious heart disease: The case of Trypanosoma cruzi infection and consequent Chagasic myocardiopathy. Cytokine Growth Factor Rev 19: 405-413.
9. Araujo-Jorge TC, Waghabi MC, Hasslocher-Moreno AM, Xavier SS, Higuchi Md Mde L, et al. (2002) Implication Of Transforming Growth Factor-beta1 In Chagas Disease Myocardiopathy. J Infect Dis 186: 1823-1828.
10. Waghabi MC, Coutinho-Silva R, Feige JJ, Higuchi Mde L, Becker D, et al. (2009) Gap junction reduction in cardiomyocytes following transforming growth factor-beta treatment and Trypanosoma cruzi infection. Mem Inst Oswaldo Cruz 104: 1083-1090.
11. Waghabi MC, Keramidas M, Calvet CM, Meuser M, de Nazare CSM, et al. (2007) SB-431542, a transforming growth factor beta inhibitor, impairs Trypanosoma cruzi infection in cardiomyocytes and parasite cycle completion. Antimicrob Agents Chemother 51: 2905-2910.
12. Waghabi MC, de Souza EM, de Oliveira GM, Keramidas M, Feige JJ, et al. (2009) Pharmacological inhibition of transforming growth factor beta signaling decreases infection and prevents heart damage in acute Chagas' disease. Antimicrob Agents Chemother 53: 4694-4701.
13. Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, et al. (2006) Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem 49: 2210-2221.
14. Petersen M, Thorikay M, Deckers M, van Dinther M, Grygielko ET, et al. (2008) Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int 73: 705-715.
15. Olivieri BP, de Souza AP, Cotta-de-Almeida V, de Castro SL, Araujo-Jorge T, (2006) Trypanosoma cruzi: alteration in the lymphoid compartments following interruption of infection by early acute benznidazole therapy in mice. Exp Parasitol 114: 228-234.
16. Waghabi MC, Coutinho CM, Soeiro MN, Pereira MC, Feige JJ, et al. (2002) Increased Trypanosoma cruzi invasion and heart fibrosis associated with high transforming growth factor beta levels in mice deficient in alpha(2)-macroglobulin. Infect Immun 70: 5115-5123.
17. Ronco MT, Frances DE, Ingaramo PI, Quiroga AD, Alvarez ML, et al. (2010) Tumor necrosis factor alpha induced by Trypanosoma cruzi infection mediates inflammation and cell death in the liver of infected mice. Cytokine 49: 64-72.
18. Souza AP, Jelicks LA, Tanowitz HB, Olivieri BP, Medeiros MM, et al. (2010) The benefits of using selenium in the treatment of Chagas disease: prevention of right ventricle chamber dilatation and reversion of Trypanosoma cruzi-induced acute and chronic cardiomyopathy in mice. Mem Inst Oswaldo Cruz 105: 746-751.
19. Ming M, Ewen ME, Pereira ME, (1995) Trypanosome invasion of mammalian cells requires activation of the TGF beta signaling pathway. Cell 82: 287-296.
20. Hall BS, Pereira MA, (2000) Dual role for transforming growth factor beta-dependent signaling in Trypanosoma cruzi infection of mammalian cells. Infect Immun 68: 2077-2081.
21. Waghabi MC, Keramidas M, Feige JJ, Araujo-Jorge TC, Bailly S, (2005) Activation of transforming growth factor beta by Trypanosoma cruzi. Cell Microbiol 7: 511-517.
22. Waghabi MC, Keramidas M, Bailly S, Degrave W, Mendonca-Lima L, et al. (2005) Uptake of host cell transforming growth factor-beta by Trypanosoma cruzi amastigotes in cardiomyocytes: potential role in parasite cycle completion. Am J Pathol 167: 993-1003.
23. Teixeira AR, Gomes C, Nitz N, Sousa AO, Alves RM, et al. (2011) Trypanosoma cruzi in the chicken model: Chagas-like heart disease in the absence of parasitism. PLoS Negl Trop Dis 5: e1000.
24. Teixeira AR, Hecht MM, Guimaro MC, Sousa AO, Nitz N, (2011) Pathogenesis of chagas' disease: parasite persistence and autoimmunity. Clin Microbiol Rev 24: 592-630.
25. Zhang M, Fennell C, Ranford-Cartwright L, Sakthivel R, Gueirard P, et al. (2010) The Plasmodium eukaryotic initiation factor-2alpha kinase IK2 controls the latency of sporozoites in the mosquito salivary glands. J Exp Med 207: 1465-1474.
26. van Baarlen P, van Belkum A, Summerbell RC, Crous PW, Thomma BP, (2007) Molecular mechanisms of pathogenicity: how do pathogenic microorganisms develop cross-kingdom host jumps? FEMS Microbiol Rev 31: 239-277.
27. Ziyadeh FN, Hoffman BB, Han DC, Iglesias-De La Cruz MC, Hong SW, et al. (2000) Long-term prevention of renal insufficiency, excess matrix gene expression, and glomerular mesangial matrix expansion by treatment with monoclonal antitransforming growth factor-beta antibody in db/db diabetic mice. Proc Natl Acad Sci U S A 97: 8015-8020.
28. Han DC, Hoffman BB, Hong SW, Guo J, Ziyadeh FN, (2000) Therapy with antisense TGF-beta1 oligodeoxynucleotides reduces kidney weight and matrix mRNAs in diabetic mice. Am J Physiol Renal Physiol 278: F628-634.
29. Russo LM, del Re E, Brown D, Lin HY, (2007) Evidence for a role of transforming growth factor (TGF)-beta1 in the induction of postglomerular albuminuria in diabetic nephropathy: amelioration by soluble TGF-beta type II receptor. Diabetes 56: 380-388.
30. Callahan JF, Burgess JL, Fornwald JA, Gaster LM, Harling JD, et al. (2002) Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). J Med Chem 45: 999-1001.
31. Laping NJ, Grygielko E, Mathur A, Butter S, Bomberger J, et al. (2002) 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: 58-64.
32. Tanaka H, Shinto O, Yashiro M, Yamazoe S, Iwauchi T, et al. (2010) Transforming growth factor beta signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Oncol Rep 24: 1637-1643.
33. Lagares D, Garcia-Fernandez RA, Jimenez CL, Magan-Marchal N, Busnadiego O, et al. (2010) Endothelin 1 contributes to the effect of transforming growth factor beta1 on wound repair and skin fibrosis. Arthritis Rheum 62: 878-889.
34. Tan SM, Zhang Y, Connelly KA, Gilbert RE, Kelly DJ, (2010) Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol 298: H1415-1425.
35. Eickhoff CS, Lawrence CT, Sagartz JE, Bryant LA, Labovitz AJ, et al. (2010) ECG detection of murine chagasic cardiomyopathy. J Parasitol 96: 758-764.
36. Gaita F, Giustetto C, Bianchi F, Wolpert C, Schimpf R, et al. (2003) Short QT Syndrome: a familial cause of sudden death. Circulation 108: 965-970.
37. Manzullo EC, Chuit R, (1999) Risk of death due to chronic chagasic cardiopathy. Mem Inst Oswaldo Cruz 94: 317-320.
38. Strauss DG, Cardoso S, Lima JA, Rochitte CE, Wu KC, (2011) ECG scar quantification correlates with cardiac magnetic resonance scar size and prognostic factors in Chagas' disease. Heart 97: 357-361.
39. Severs NJ, (2001) Gap junction remodeling and cardiac arrhythmogenesis: cause or coincidence? J Cell Mol Med 5: 355-366.
40. Chanson M, Derouette JP, Roth I, Foglia B, Scerri I, et al. (2005) Gap junctional communication in tissue inflammation and repair. Biochim Biophys Acta 1711: 197-207.
41. Tabibzadeh S, (2002) Homeostasis of extracellular matrix by TGF-beta and lefty. Front Biosci 7: d1231-1246.
42. Peng SB, Yan L, Xia X, Watkins SA, Brooks HB, et al. (2005) Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry 44: 2293-2304.