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

Content Provider	Springer Nature Link
Author	Yamaguchi, Takayuki Kakefuda, Reina Tanimoto, Atsuo Watanabe, Yoshihiro Tajima, buyuki
Copyright Year	2012
Abstract	To examine the effects of a mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2-inhibitor, JTP-74057, on inflammatory arthritis development, and compare its anti-arthritic effect with leflunomide.Human, mouse, and rat peripheral blood mononuclear cells (PBMCs) were used. Lewis rats and DBA/1J mice were used for animal models.JTP-74057 was tested between 0.1–100 nM in in-vitro studies. JTP-74057 (0.01–0.3 mg/kg) and leflunomide (2–10 mg/kg) were administered orally in vivo.PBMCs were stimulated with lipopolysaccharide. Adjuvant-induced arthritis (AIA) and type II collagen-induced arthritis (CIA) was induced in Lewis rats or DBA1/J mice, respectively.JTP-74057 blocked tumor necrosis factor-α and interleukin-6 production from PBMCs. AIA and CIA development were suppressed almost completely by 0.1 mg/kg of JTP-74057 or 10 mg/kg of leflunomide. In the CIA, JTP-74057, but not leflunomide, suppressed collagen-reactive T-cell proliferation ex vivo, whereas leflunomide, but not JTP-74057, suppressed anti-collagen antibody production.JTP-74057 exerts potent anti-arthritic effects with a different profile from leflunomide, suggesting that JTP-74057 may be useful as a new therapeutic reagent in the treatment of rheumatoid arthritis.
Starting Page	445
Ending Page	454
Page Count	10
File Format	PDF
ISSN	10233830
Journal	Inflammation Research
Volume Number	61
Issue Number	5
e-ISSN	1420908X
Language	English
Publisher	SP Birkhäuser Verlag Basel
Publisher Date	2012-01-14
Publisher Place	Basel
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	MEK–ERK pathway MEK1/2 inhibitor JTP-74057 Collagen-induced arthritis Adjuvant-induced arthritis Leflunomide Immunology Allergology Neurology Pharmacology/Toxicology Dermatology Rheumatology
Content Type	Text
Resource Type	Article
Subject	Pharmacology Immunology

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