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ERK inhibitors as a potential new therapy for rheumatoid arthritis.

Abstract
Rheumatoid arthritis (RA), a chronic and systemic autoimmune disease that leads to progressive articular destruction, is evoked by the concerted action of RA-related cells, such as T cells, synovial fibroblasts and macrophages. Although anticytokine biologics block the intercellular signal transduction of these RA-related cells and thereby exert a strong ameliorative effect on RA, there still remains a significant percentage of nonresponsive patients. In addition to these biologics that disrupt specific intercellular signals, extracellular signal-regulated kinase (ERK) inhibitors, which are believed to target the intracellular signals common to the diverse RA-related cells, are also used as a treatment for RA patients, including those who are nonresponsive to the anticytokine therapies. Recently, potent and selective inhibitors for ERK with the co-crystal structures have been reported. FR180204, an ERK inhibitor, has been shown to be effective against mouse collagen-induced arthritis, a representative animal model of RA. This compound also suppresses the antigen-specific activation of T cells, which play a central role in the initiation and progress of the disease. Information obtained from the co-crystal structures would contribute to the improvement of the chemical characteristics. Thus, with the discovery of new potential chemical entities, ERK inhibitors may emerge as a new therapeutic approach for the treatment of RA.
AuthorsMakoto Ohori
JournalDrug news & perspectives (Drug News Perspect) Vol. 21 Issue 5 Pg. 245-50 (Jun 2008) ISSN: 0214-0934 [Print] United States
PMID18596988 (Publication Type: Journal Article, Review)
CopyrightCopyright 2008 Prous Science, S.A.U. or its licensors. All rights reserved.
Chemical References
  • Antirheumatic Agents
  • Immunologic Factors
  • Extracellular Signal-Regulated MAP Kinases
Topics
  • Animals
  • Antirheumatic Agents (therapeutic use)
  • Arthritis, Rheumatoid (drug therapy)
  • Extracellular Signal-Regulated MAP Kinases (antagonists & inhibitors)
  • Humans
  • Immunologic Factors (therapeutic use)
  • Mice

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