Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity

@article{Hill2008PamapimodAN,
  title={Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity},
  author={R. J. Hill and K. Dabbagh and D. Phippard and Ching Li and Rebecca T. Suttmann and Mary Welch and E. Papp and K. W. Song and Kung-ching Chang and D. Leaffer and Y. Kim and R. T. Roberts and T. Zabka and D. Aud and J. Porto and A. Manning and S. Peng and D. Goldstein and B. Wong},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2008},
  volume={327},
  pages={610 - 619}
}
  • R. J. Hill, K. Dabbagh, +16 authors B. Wong
  • Published 2008
  • Medicine
  • Journal of Pharmacology and Experimental Therapeutics
  • P38α is a protein kinase that regulates the expression of inflammatory cytokines, suggesting a role in the pathogenesis of diseases such as rheumatoid arthritis (RA) or systemic lupus erythematosus. Here, we describe the preclinical pharmacology of pamapimod, a novel p38 mitogen-activated protein kinase inhibitor. Pamapimod inhibited p38α and p38β enzymatic activity, with IC50 values of 0.014 ± 0.002 and 0.48 ± 0.04 μM, respectively. There was no activity against p38δ or p38γ isoforms. When… CONTINUE READING
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    References

    SHOWING 1-10 OF 50 REFERENCES
    Inflammation-activated protein kinases as targets for drug development.
    • M. Karin
    • Biology, Medicine
    • Proceedings of the American Thoracic Society
    • 2005
    • 120
    • PDF
    A Selective p38α Mitogen-Activated Protein Kinase Inhibitor Reverses Cartilage and Bone Destruction in Mice with Collagen-Induced Arthritis
    • 71
    • Highly Influential
    A selective p38 alpha mitogen-activated protein kinase inhibitor reverses cartilage and bone destruction in mice with collagen-induced arthritis.
    • 46
    • Highly Influential
    Mitogen-activated protein kinase kinase 3 is a pivotal pathway regulating p38 activation in inflammatory arthritis.
    • T. Inoue, D. Boyle, +4 authors G. Firestein
    • Biology, Medicine
    • Proceedings of the National Academy of Sciences of the United States of America
    • 2006
    • 101
    • PDF
    Pathway to the clinic: inhibition of P38 MAP kinase. A review of ten chemotypes selected for development.
    • 138
    p38 Mitogen-Activated Protein Kinase Contributes to Autoimmune Renal Injury in MRL-Faslpr Mice
    • 73
    • PDF
    Generation and Characterization of p38β (MAPK11) Gene-Targeted Mice
    • 242
    • PDF
    R-130823, a novel inhibitor of p38 MAPK, ameliorates hyperalgesia and swelling in arthritis models.
    • 42
    p38 MAP kinases: key signalling molecules as therapeutic targets for inflammatory diseases
    • 1,094
    • Highly Influential
    p38 Mitogen-activated protein kinase contributes to autoimmune renal injury in MRL-Fas lpr mice.
    • 27