Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: A comparison with leflunomide

Inflammation Research

Volumn 61, Issue 5, 2012, Pages 445-454

  Yamaguchi, Takayuki ^a   Kakefuda, Reina ^a   Tanimoto, Atsuo ^a   Watanabe, Yoshihiro ^a   Tajima, Nobuyuki ^a  

^a JAPAN TOBACCO INC   (Japan)

Author keywords

Adjuvant induced arthritis; Collagen induced arthritis; JTP 74057; Leflunomide; MEK ERK pathway; MEK1 2 inhibitor

Indexed keywords

COLLAGEN ANTIBODY; COLLAGEN TYPE 2; IMMUNOGLOBULIN G ANTIBODY; INTERLEUKIN 6; LEFLUNOMIDE; LIPOPOLYSACCHARIDE; MITOGEN ACTIVATED PROTEIN KINASE KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE KINASE 2; TRAMETINIB; TUMOR NECROSIS FACTOR ALPHA;

ADJUVANT ARTHRITIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBODY PRODUCTION; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CONTROLLED STUDY; CYTOKINE PRODUCTION; DISEASE MODEL; DRUG DOSE COMPARISON; EX VIVO STUDY; HUMAN; HUMAN CELL; IN VIVO STUDY; LYMPHOCYTE PROLIFERATION; MALE; MOUSE; NONHUMAN; PAW EDEMA; PERIPHERAL BLOOD MONONUCLEAR CELL; PROTEIN PHOSPHORYLATION; RAT; RHEUMATOID ARTHRITIS; T LYMPHOCYTE ACTIVATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ARTHRITIS, EXPERIMENTAL; COLLAGEN TYPE II; CYTOKINES; ENZYME INHIBITORS; HUMANS; INTERLEUKIN-6; ISOXAZOLES; LIPOPOLYSACCHARIDES; LYMPHOCYTE ACTIVATION; MAP KINASE KINASE 1; MAP KINASE KINASE 2; MICE; MICE, INBRED ICR; PYRIDONES; PYRIMIDINONES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84863109639     PISSN: 10233830     EISSN: 1420908X     Source Type: Journal    
DOI: 10.1007/s00011-011-0431-5     Document Type: Article

References (42)

1. Firestein GS. Evolving concepts of rheumatoid arthritis. Nature. 2003;423:356-61.
2. Arend WP, Dayer JM. Inhibition of the production and effects of interleukin-1 and tumor necrosis factor a in rheumatoid arthritis. Arthritis Rheum. 1995;38:151-60.
3. Feldmann M, Brennan FM, Maini RN. Rheumatoid arthritis. Cell. 1996;85:307-10.
4. van Vollenhoven RF. Treatment of rheumatoid arthritis: state of the art 2009. Nat Rev Rheumatol. 2009;5:531-41.
5. Gartlehner G, Hansen RA, Jonas BL, Thieda P, Lohr KN. The comparative efficacy and safety of biologics for the treatment of rheumatoid arthritis: a systematic review and metaanalysis. J Rheumatol. 2006;33:2398-408.
6. Morel J, Berenbaum F. Signal transduction pathways: new targets for treating rheumatoid arthritis. Joint Bone Spine. 2004;71: 503-10.
7. Thalhamer T, McGrath MA, Harnett MM. MAPKs and their relevance to arthritis and inflammation. Rheumatology. 2008;47: 409-14.
8. Sweeney SE, Firestein GS. Mitogen activated protein kinase inhibitors: where are we now and where are we going? Ann Rheum Dis. 2006; 65 SUPPL. 3:iii83-iii88.
9. Schett G, Tohidast-Akrad M, Smolen JS, Schmid BJ, Steiner CW, Bitzan P, et al. Activation, differential localization, and regulation of the stress-activated protein kinases, extracellular signal-regulated kinase, c-jun N-terminal kinase, and p38 mitogen-activated protein kinase, in synovial tissue and cells in rheumatoid arthritis. Arthritis Rheum. 2000;43:2501-12.
10. Scherle PA, Jones EA, Favata MF, Daulerio AJ, Covington MB, Nurnberg SA, et al. Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharidestimulated monocytes. J Immunol. 1998;161:5681-6.
11. Liu E, Thant AA, Kikkawa F, Kurata H, Tanaka S, Nawa A, et al. The Ras-mitogen-activated protein kinase pathway is critical for the activation of matrix metalloproteinase secretion and the invasiveness in v-crk-transformed 3Y1. Cancer Res. 2000;60:2361-4.
12. Thiel MJ, Schaefer CJ, Lesch ME, Mobley JL, Dudley DT, Tecle H, et al. Central role of the MEK/ERK MAP kinase pathway in a mouse model of rheumatoid arthritis: potential proinflammatory mechanisms. Arthritis Rheum. 2007;56:3347-57.
13. Ohori M, Takeuchi M, Maruki R, Nakajima H, Miyake H. FR180204, a novel and selective inhibitor of extracellular signalregulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007;374:311-6.
14. Yamaguchi T, Yoshida T, Kurachi R, Kakegawa J, Hori Y, Nanayama T, et al. Identification of JTP-70902, a p15INK4b- inductive compound, as a novel MEK1/2 inhibitor. Cancer Sci. 2007;98:1809-16.
15. Yamaguchi T, Kakefuda R, Tajima N, Sowa Y, Sakai T. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011;39:23-31.
16. Abe H, Kikuchi S, Hayakawa K, Iida T, Nagahashi N, Maeda K, et al. Discovery of a highly potent and selective MEK inhibitor: GSK1120212 (JTP-74057 DMSO solvate). ACS Med Chem Lett. 2011;2:320-4.
17. Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin Cancer Res. 2011;17:989-1000.
18. Sugimoto K, Ohata M, Miyoshi J, Ishizaki H, Tsuboi N, Masuda A, et al. A serine/threonine kinase, Cot/Tpl2, modulates bacterial DNA-induced IL-12 production and Th cell differentiation. J Clin Invest. 2004;114:857-66.
19. Dumitru CD, Ceci JD, Tsatsanis C, Kontoyiannis D, Stamatakis K, Lin JH, et al. TNF-α induction by LPS is regulated posttranscriptionally via a Tpl2/ERK-dependent pathway. Cell. 2000;103: 1071-83.
20. Sebolt-Leopold JS, Herrera R. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer. 2004;4: 937-47.
21. Feng D, Ling WH, Duan RD. Lycopene suppresses LPS-induced NO and IL-6 production by inhibiting the activation of ERK, p38MAPK, and NF-kB in macrophages. Inflamm Res. 2010;59: 115-21.
22. Hall JP, Kurdi Y, Hsu S, Cuozzo J, Liu J, Telliez JB, et al. Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. J Biol Chem. 2007;282:33295-304.
23. 3 integrin and macrophage colony stimulating factor-mediated signals on phospholipase Cc in prefusion osteoclasts. J Cell Biol. 2001;152:361-73.
24. Lee SE, Chung WJ, Kwak HB, Chung CH, Kwack KB, Lee ZH, et al. Tumor necrosis factor-a supports the survival of osteoclasts through the activation of Akt and ERK. J Biol Chem. 2001; 276:49343-9.
25. Lee ZH, Lee SE, Kim CW, Lee SH, Kim SW, Kwack K, et al. IL-1β stimulation of osteoclast survival through the PI 3-kinase/Akt and ERK pathways. J Biochem. 2002;131:161-6.
26. Breitkreutz I, Raab MS, Vallet S, Hideshima T, Raje N, Chauhan D, et al. Targeting MEK1/2 blocks osteoclast differentiation, function and cytokine secretion in multiple myeloma. Br J Haematol. 2007;139:55-63.
27. Nakamura H, Hirata A, Tsuji T, Yamamoto T. Role of osteoclast extracellular signal-regulated kinase (ERK) in cell survival and maintenance of cell polarity. J Bone Miner Res. 2003;18: 1198-205.
28. Seo SW, Lee D, Minematsu H, Kim AD, Shin M, Cho SK, et al. Targeting extracellular signal-regulated kinase (ERK) signaling has therapeutic implications for inflammatory osteolysis. Bone. 2010;46:695-702.
29. Myers LK, Rosloniec EF, Cremer MA, Kang AH. Collageninduced arthritis, an animal model of autoimmunity. Life Sci. 1997;61:1861-78.
30. + T cells in the early stage of collagen-induced arthritis and its arthritogenic role in DBA/1 J mice. J Clin Immunol. 2006;26:204-12.
31. Schattenkirchner M. The use of leflunomide in the treatment of rheumatoid arthritis: an experimental and clinical review. Immunopharmacology. 2000;47:291-8.
32. Vergne-Salle P, Léger DY, Bertin P, Trèves R, Beneytout JL, Liagre B. Effects of the active metabolite of leflunomide, A77 1726, on cytokine release and the MAPK signalling pathway in human rheumatoid arthritis synoviocytes. Cytokine. 2005;31: 335-48.
33. 2, matrix metalloproteinase 1 and interleukin 6 in human fibroblast-like synoviocytes. Rheumatology. 2003;42:89-96.
34. Cutolo M, Sulli A, Ghiorzo P, Pizzorni C, Craviotto C, Villaggio B. Anti-inflammatory effects of leflunomide on cultured synovial macrophages from patients with rheumatoid arthritis. Ann Rheum Dis. 2003;62:297-302.
35. Korn T, Magnus T, Toyka K, Jung S. Modulation of effector cell functions in experimental autoimmune encephalomyelitis by leflunomide- mechanisms independent of pyrimidine depletion. J Leukoc Biol. 2004;76:950-60.
36. Ohori M, Kinoshita T, Okubo M, Sato K, Yamazaki A, Arakawa H, et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005;336:357-63.
37. Graczyk PP. Gini coefficient: a new way to express selectivity of kinase inhibitors against a family of kinases. J Med Chem. 2007;50:5773-9.
38. INK4a senescence gene as a new therapeutic strategy for the treatment of rheumatoid arthritis. Nat Med. 1999;5:760-7.
39. Sekine C, Sugihara T, Miyake S, Hirai H, Yoshida M, Miyasaka N, et al. Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors. J Immunol. 2008;180:1954-61.
40. WAF1/Cip1expression. Arthritis Rheum. 2004;50:3365-76.
41. Bolon B, Stolina M, King C, Middleton S, Gasser J, Zack D, et al. Rodent preclinical models for developing novel antiarthritic molecules: comparative biology and preferred methods for evaluating efficacy. J Biomed Biotechnol. 2011;2011:569068.
42. Takagi N, Mihara M, Moriya Y, Nishimoto N, Yoshizaki K, Kishimoto T, et al. Blockage of interleukin-6 receptor ameliorates joint disease in murine collagen-induced arthritis. Arthritis Rheum. 1998;41:2117-21.