Macitentan slows down the dermal fibrotic process in systemic sclerosis: In vitro findings

Journal of Biological Regulators and Homeostatic Agents

Volumn 27, Issue 2, 2013, Pages 455-462

  Corallo, C ^a   Pecetti, G ^b   Iglarz, M ^c   Volpi, N ^a   Franci, D ^a   Montella, A ^a   D'Onofrio, F ^a   Nuti, R ^a   Giordano, Nicola ^a  

^a UNIVERSITY OF SIENA   (Italy)

^b Medical and Scientific Direction   (Italy)

^c ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

Endothelin 1; ET receptors; Macitentan; Systemic sclerosis

Indexed keywords

ACT 132577; ALPHA SMOOTH MUSCLE ACTIN; DRUG METABOLITE; MACITENTAN; UNCLASSIFIED DRUG; ACTA2 PROTEIN, HUMAN; ACTIN; ENDOTHELIN A RECEPTOR; ENDOTHELIN B RECEPTOR; N (5 (4 BROMOPHENYL) 6 (2 (5 BROMOPYRIMIDIN 2 YLOXY)ETHOXY)PYRIMIDIN 4 YL) N' PROPYLAMINOSULFONAMIDE; N-(5-(4-BROMOPHENYL)-6-(2-(5-BROMOPYRIMIDIN-2-YLOXY)ETHOXY)PYRIMIDIN-4-YL)-N'-PROPYLAMINOSULFONAMIDE; PYRIMIDINE DERIVATIVE; SULFONAMIDE;

ADULT; ARTICLE; CLINICAL ARTICLE; CONTROLLED STUDY; DERMIS; DRUG EFFECT; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; PROTEIN EXPRESSION; SKIN FIBROBLAST; SKIN FIBROSIS; SYSTEMIC SCLEROSIS; AGED; DRUG ANTAGONISM; FIBROSIS; MIDDLE AGED; PATHOLOGY; SKIN;

ACTINS; AGED; FEMALE; FIBROSIS; HUMANS; MIDDLE AGED; PYRIMIDINES; RECEPTOR, ENDOTHELIN A; RECEPTOR, ENDOTHELIN B; SCLERODERMA, SYSTEMIC; SKIN; SULFONAMIDES;

EID: 84883471768     PISSN: 0393974X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (29)

1. Korn JH. Pathogenesis of systemic sclerosis. Arthritis and allied conditions, Koopman WJ editor 2001; 1643-54.
2. Zamora MR, O'Brien RF, Rutherford RB, Weil JV. Serum endothelin-1 concentrations and cold provocation in primary Raynaud's phenomenon. Lancet 1990; 336(8724):1144-7. (Pubitemid 20362904)
3. Soldano S, Montagna P, Brizzolara R. Endothelin receptor antagonists: effects on extracellular matrix synthesis in primary cultures of skin fibroblasts from systemic sclerosis patients. Reumatismo 2012; 64(5):326-34.
4. Korn JH, Mayes M, Matucci-Cerinic M, et al. Digital ulcers in systemic sclerosis: prevention by treatment with bosentan, an oral endothelin receptor antagonist. Arthritis Rheumatism 2004; 50:3985-93. (Pubitemid 39643947)
5. Finsnes F, Lyberg T, Christensen G, Skjønsberg OH. Effect of Endothelin antagonism on the production of cytokines in eosinophilic airway inflammation. Am J Physiol Lung Cell Mol Physiol 2001; 280:659-65.
6. Shi-Wen X, Rodríguez-Pascual F, Lamas S. Constitutive ALK5-independent c-Jun N-terminal kinase activation contributes to endothelin-1 overexpression in pulmonary fibrosis: evidence of an autocrine endothelin loop operating through the endothelin A and B receptors. Mol Cell Biol 2006; 26:5518-27. (Pubitemid 44036217)
7. st Systemic Sclerosis World Congress 2010.
8. Dooley A, Shi-Wen X, Aden N, Tranah T, Desai N, Denton CP, Abraham DJ, Bruckdorfer R. Modulation of collagen type I, fibronectin and dermal fibroblast function and activity, in systemic sclerosis by the antioxidant epigallocatechin-3-gallate. Rheumatology (Oxford) 2010; 49(11):2024-36.
9. Andrawis NS, Wang E, Abernethy DR. Endothelin-1 induces an increase in total protein synthesis and expression of the smooth muscle alpha-actin gene in vascular smooth muscle cells. Life Sci 1996; 59(7):523-8. (Pubitemid 26274413)
10. Hinz B, Phan SH, Thannickal VJ, Galli A, Bochaton-Piallat ML, Gabbiani G. The myofibroblast: one function, multiple origins. Am J Pathol 2007; 170(6): 1807-16Frommer KW, Müller-Ladner U. Expression and function of ETA and ETB receptors in SSc. Rheumatology (Oxford) 2008; 47(5):27-8.
11. Kakoki M, Hirata Y, Hayakawa H, et al. Effect of hypertension, diabetes mellitus, and hypercholesterolemia on endhotelin type B receptor-mediated nitric oxide release from rat kidney. Circulation 1999; 99:1242-8. (Pubitemid 29120098)
12. Abraham DJ, Vancheeswaran R, Dashwood MR, Rajkumar VS, Pantelides P, Xu SW, du Bois RM, Black CM. Increased levels of endothelin-1 and differential endothelin type A and type B receptor expression in scleroderma-associated fibrotic lung disease. Am J Pathol 1997; 151:831-41. (Pubitemid 27385615)
13. Gregan B, Jürgensen J, Papsdorf G, Furkert J, Schaefer M, Beyermann M, Rosenthal W, Oksche A. Ligand-dependent differences in the internalization of endothelin A and endothelin B receptor heterodimers. J Biol Chem 2004; 279:27679-87. (Pubitemid 38812609)
14. Sauvageau S, Thorin E, Caron A, Dupuis J. Endothelin-1-induced pulmonary vasoreactivity is regulated by ET(A) and ET(B) receptor interactions. J Vasc Res 2007; 44:375-81. (Pubitemid 47312658)
15. Shi-Wen X, Denton CP, Dashwood MR, Holmes AM, Bou-Gharios G, Pearson JD, Black CM, Abraham DJ. Fibroblast matrix gene expression and connective tissue remodeling: role of endothelin-1. J Invest Dermatol 2001; 116:417-25. (Pubitemid 32202907)
16. Porter KE, Olojugba DH, Masood I, Pemberton M, Bell PR, London NJ. Endothelin-B receptors mediate intimal hyperplasia in an organ culture of human saphenous vein. J Vasc Surg 1998; 28:695-701. (Pubitemid 28481225)
17. Clozel M, Gray GA. Are there different ETB receptors mediating constriction and relaxation? J Cardiovasc Pharmacol 1995; 26:262-4.
18. Iglarz M, Binkert C, Morrison K, Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther 2008; 327:736-45.
19. Sidharta PN, Dingemanse J. Multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the dual endothelin receptor antagonist act-064992 in healthy human subjects. J Clin Pharmacol 2008; 48:1114.
20. LeRoy EC, Black C, Fleischmajer R, et al. Scleroderma (systemic sclerosis): classification, subsets and pathogenesis. J Rheumatol 1988; 15:202-5. (Pubitemid 18073738)
21. Moulin V, Plamondon M. Differential expression of collagen integrin receptor on fetal vs. adult skin fibroblasts: implications in wound contraction during healing. Br J Dermatol 2002; 5:886-92. (Pubitemid 35365434)
22. Van Meerloo J, Kaspers GJ, Cloos J. Cell sensitivity assay: the MTT assay. Methods Mol Biol 2011; 731:237-45.
23. Bradford MM. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 1976; 72:48-254.
24. Laemmli UK. Cleavage of structural proteins during the assembly of the head of bacteriophage T4. Nature 1970; 227:680-5.
25. Harrison NK, Argent AC, McAnulty RJ, Black CM, Corrin B, Laurent GJ. Collagen synthesis and degradation by systemic sclerosis lung fibroblasts. Responses by transforming growth factor-beta. Chest 1991; 99:71-2.
26. Tomasek JJ, Gabbiani G, Hinz B, Chaponnier C, Brown RA. Myofibroblasts and mechano-regulation of connective tissue remodeling. Nat Rev Mol Cell Biol 2002; 3:349-63. (Pubitemid 34619269)
27. Giordano N, Papakostas P, Pecetti G, Nuti R. Cytokine modulation by endothelin-1 and possible therapeutic implications in systemic sclerosis. J Biol Regul Homeost Agents 2011; 25:487-92.
28. Nishibu A, Sakai E, Oyama N, Yamamoto T. Endothelin receptor antagonist bosentan improves the dermal sclerosis in a patient with systemic sclerosis. Australas J Dermatol 2012; 53:32-3.
29. Shi-Wen X, Chen Y, Denton CP, et al. Endothelin-1 promotes myofibroblast induction through the ETA receptor via a rac/phosphoinositide 3-kinase/Akt-dependent pathway and is essential for the enhanced contractile phenotype of fibrotic fibroblasts. Mol Biol Cell 2004; 15(6):2707-19. (Pubitemid 38691860)